3^rd International Conference on Biopharmaceutics and Biologic Drugs August 30-31, 2017 Philadelphia, USA
(10 Plenary Forums - 1Event)

Dixit (graduate from University of Illinois) is a scholastic personality with several patents and publications to his credit and with more than 25 years of rich experience in pharmaceuticals, biopharmaceutical and CRO industries in the area of drug discovery and bio-analytical services. He has extensively worked on method development and validation of various assay platforms such as LC-MS, ELISA, MSD, SPR, RIA/RIPA and Cell based assays for Immunogenicity and pharmacokinetics evaluation of non-clinical and clinical study samples under GLP and GCLP compliant practices for regulatory submission studies. As a test facility management and head of bioanalytical laboratory he has successfully faced multiple sponsor’s and regulatory audits. Dr. Dixit with his expertise is currently guiding the team biologics in the delivery of quality compliant bioanalytical and Characterization services for biologics and biosimilars for submission studies

With the advent of Biotechnology more and more human recombinant protein biotherapeutics have replaced the animal derived drug products. Th is has helped in global availability of quality drug products at a competitive price. Th e advantages of the recombinant protein biotherapeutics are high purity, high specifi c activity, steady supply and batch-to-batch consistency. All protein biotherapeutics are potentially immunogenic and hence could elicit immunogenicity response. Th ese responses could be of diff erent types such as binding antibodies or neutralizing antibodies. Immunogenicity of protein biotherapeutics is a major concern especially when the biological function of the drug and the endogenous counterpart are neutralized by antidrug antibodies (ADA). Hence the regulatory agencies insist that the immunogenicity response should be assessed by validated sensitive assay formats during the diff erent stages of drug development and the antibody response be characterized. An effort has been made in this presentation to discuss on immunogenicity to protein biotherapeutics, regulatory concerns, strategy to evaluate the immunogenicity, overview of methods available, factors infl uencing immunogenicity and to share the experience of developing an ADA method using ELISA and GYROS assay format to assess immunogenicity of two drug products

Nayanabhirama Udupa was at Manipal University as Professor and Head of the institution, Manipal College of Pharmaceutical Sciences for couple of tenures since his joining as Professor from 1987. He has published more than 510 papers peer reviewed journals, presented 411 papers in different conferences throughout the world, contributed 12 books in pharmacy fi eld and gave more than 125 lectures. He has received more than 57 research grants having 9 patents. He has guided 36 PhD candidates and 80 M pharm students for the completion of their thesis.

Diabetes mellitus is a metabolic disorder, is becoming a serious threat to mankind health. Among all types of diabetes, type

2 diabetes is main complication which can be controlled with diet, exercise and oral medications. Oral medications are not insulin pills, rather four classes of drugs designed to improve the body’s utilization of what insulin is still present. These are sulfonylurea, metformin, troglitazone and acarbose but these oral medications will not be eff ective when islets of pancreas stop

making suffi cient insulin. So we have come with a dietary supplement which can be used as a soup for management of diabetes.

Th e composition of the supplement includes all dietary ingredients such as wheat fl our commonly known as bread wheat, barley powder, guar gum it’s a polysaccharide of galactose and mannose, which is water soluble polymer, exhibits a viscosifying

eff ect in water, onion powder commonly known as bulb onion, which contains quercetin, allicin, allinin and salt as required and turmeric powder that are harmless when given to patients. Our preliminary in vitro studies suggested good activity in modifying glucose absorption from the gut and we also carried out a prospective observational pilot study, to study the eff ect of dietary supplement on glycemic control in pre-diabetes (PD) and mildly uncontrolled diabetics (MUCD) and the results have shown that the dietary supplementation could be an adjuvant therapy which is safe, healthy and economic alternative for DM patients to control blood glucose levels and also that can minimize even the dose of OHAs.

Santosh K Singh obtained his Master’s in Botany from Veer Bahadur Singh Purvanchal University, Jaunpur in India in 1992. He was awarded a PhD degree in Botany from Banaras Hindu University, Varanasi, India in 1998. He is currently appointed as Senior Research Offi cer in Centre of Experimental Medicine and Surgery, IMS, BHU and leading the center which have facilities for cell culture, natural product research, molecular biology research, plant endophytes research and animal house also for animal study works. He is working on traditionally used herbal medicines, bio-fabrication of highly structured nanomaterials and their evaluation for anti-cancer activity.

Cancer is one of the second most leading causes of death in India and around the world aft er cardiovascular disease while breast cancer is the most common cancer in women worldwide, with nearly 1.67 million new cases diagnosed in 2012. It was projected that the burden of breast cancer will increase by 50% in 2030. Chemotherapy continues to be the most common pharmacological approach for the treatment and most of the chemotherapeutic drugs for cancer treatment are molecules isolated or derived from plants. More new drugs are needed for the treatment because of the development of chemo-resistance. Natural products have continued to receive an increasing attention for their potential as novel cancer preventive and therapeutic agents which show the importance of traditionally used medicinal plants as the prime sources for development of anticancer drugs. Amoora rohituka WA is a well-known medicinal plant which possesses numerous therapeutic actions including antiinflammatory, sedative, hypnotic and narcotic. It was evaluated for anticancer activity in this study. Th e hydro-alcoholic (1:1) crude extract of the plant bark (100 g) was fractionated using column chromatography using benzene, ethyl acetate and methanol solvents respectively. The fractions were dried under vacuum in rotary evaporator and evaluated for their anticancer activity using MTT assay against human breast cancer cell line, MCF-7. Mode of cell death was evaluated by ethidium bromide and acridine orange double-staining. Th is study show that ethyl acetate fraction of bark extract (RBEA) induces cytotoxicity in a dose-dependent manner in cancer cell lines. Ethidium bromide and acridine orange double-staining demonstrated that RBEA potentiate apoptosis rather than necrosis in cancer cells.

Yesenia Elizabeth Cevallos Villacrés is an Electronic and Telecommunication Engineer from National Polytechnic in Ecuador, 2001. She has an Information Technology Master’s degree from Technical University of Ambato in Ecuador, 2010. She is an Associate Professor at National University of Chimborazo, Ecuador. Currently, she is a PhD student at University of Calabria, Italy. She has articles published in network and digital communications area in journals in Ecuador. Her main publications as PhD student is: A digital communication analysis of gene expression of proteins in biological systems: A layered network model view.

In this study, we propose the design of a protocol stack network model to explain gene expression. Gene expression is the process by which information carried by deoxyribonucleic acid (DNA) is transformed into proteins. Proteins are produced in the cell and excreted to perform a biological function. Th e nucleus of eukaryotic cells is the source of biological information, which must be modifi ed via intracellular communication to reach an adequate cellular or extracellular destination. This process implies that information is transferred through a biological path, and aft er it is received, a biological function is performed.

The transmission of proteins (specifi cally peptide hormones) to a target organ through blood stream involves the golgi apparatus, which is similar to the digital communication process wherein a transmitter in a network sends information to a destination device in another network through a router. Th e modeling that we have proposed is supported by very well know theories in communications as Shannon’s theorem, and network characteristics (e.g., independent functions of layers in a stack, addressing, fl ow control, error control, and traffi c control). Our analysis is focused in the importance of the addressing in networks applied to biological systems to reduce the incidence of side eff ects of drugs used to treat disease. Th e objective is to improve the quality of treatment for patients from health and socio-economic perspectives.

Shyam B Mehta is a PhD student in Pharmaceutical Sciences with expertise in areas specifi c to biologic drugs. His work focuses on drug product development, fi ll-fi nish manufacturing of drug product, formulation development including protein stability and biophysical characterization of protein molecules

Despite the popularity and advent of liquid formulations for biological therapeutic products, lyophilized presentations

continue to be a robust alternative, especially for products in early stages of development or with in-adequate liquid stability. In this context, there continues to be on-going interest in the pharmaceutical industry about understanding potential failure modes and mitigations for lyophilized products. Here, we present a real life case study of observations of “product on stopper” for a lyophilized product and provide further analysis if this constitutes only a cosmetic/ pharmaceutical elegance issue or can potentially be product quality impacting. Th e primary failure modes that were the focus of this investigation were potentially improper protein recovery during reconstitution and/or sterility concerns due to container closure integrity compromise. In this context, we also discuss potential mitigations. Methods: Filling of product in vials was carried out using a peristaltic pump fi lling unit and subsequently the product was lyophilized. Post lyophilization, upon visual inspection, around 40% of vials had cosmetic defect with residual product around stopper of the vial and the remaining 60% vials with no cosmetic defect were called ‘acceptable vials’. Within the product group that had product on stopper, there were diff erent degrees of this event observed. Hence for this evaluation, the lyophilized vials with the worst case product on stopper profi les were evaluated along with “acceptable vials”. Testing performed were protein concentration (UV absorbance at 280), residual moisture (Karl Fischer), sterility (membrane fi ltration) and container closure integrity (using blue dye ingress). Results & Conclusion: Product quality attributes such as sterility, residual moisture, protein concentration were also similar

between the two groups of vials. However, container closure integrity of the ‘product on stopper’ vials was compromised due to the presence of product around stopper of the vial. Th e results of this study provides two important fi ndings- 1) Defects such as “product on stopper” under certain worst case conditions may pose product quality concerns and not just cosmetic quality concerns, and 2) Container closure integrity test methods may be more sensitive in such cases compared to sterility, which also explains the regulatory agencies preference for this method for assessing sterility assurance. As an outcome of this investigation, the following corrective actions were implemented for this case: use of larger sized vial that can potentially mitigate the product handling issues.

Hong Ngoc Thuy Pham has graduated with a BSc in Food Technology from Nha Trang University, Vietnam in 2004 and then completed her Master’s degree in Postharvest Technology from Nha Trang University, Vietnam in 2009. She is currently a Lecturer of Nha Trang University, Vietnam and a PhD student at the University of Newcastle, Australia. She has published 10 papers in domestic and international journals. She is now working on the research project: Extraction of anticancer compounds from selected medicinal plants as novel agents against pancreatic cancer cells at the University of Newcastle, Australia.

Catharanthus roseus (L.) G Don (C. roseus) is traditionally known as a medicinal plant; however only its leaf has been investigated for its bioactive compounds. Other plant components, such as the stem and the root have not been studied. Our previous study conducted on the stem revealed a high level of saponins, which have been linked with various biological activities such as antimicrobial, ant herbivore and/or cytotoxic activities. Ultrasound-assisted extraction (UAE) is known as an advanced extraction method because of its eff ectiveness, simplicity and up-scale capability, thus UAE shows potential for the eff ective extraction of saponins from the stem of C. roseus. Response surface methodology (RSM) has been commonly applied to optimize extraction conditions as it can show the interactive eff ects between the tested parameters. Th is study aimed to optimize UAE conditions including temperature, time and power in combination with ratio of sample-to-solvent for the effi cient extraction of saponins from stem of C. roseus using RSM with Box-Behnken design. Th e results indicated that either ultrasonic temperature or sample-to-solvent ratio had a signifi cant infl uence on saponin yield, DPPH and ABTS radical scavenging activities (p<0.05). With the exception of ultrasonic power, the other three parameters (UAE temperature, sampleto- solvent ratio and time) statistically aff ected ferric reducing antioxidant power (FRAP) and cupric ion reducing antioxidant capacity (CUPRAC). A maximized saponin yield (138.21 mg ESE/g) and high levels of antioxidant activity (8.34, 12.06, 10.53 and 19.15 mg TE/g ABTS, DPPH scavenging capacity, FRAP and CUPRAC respectively) could be obtained under the optimal extraction conditions (ultrasonic temperature of 55°C, ultrasonic time of 35 min, sample-to-solvent ratio of 1/100 (g/mL) and ultrasonic power of 150W). Th e saponin-enriched extract from C. roseus stem can be potentially used for further investigation and application in the nutraceutical and pharmaceutical industries.

Rubi Mahato received her interdisciplinary Ph.D. in Pharmaceutical Sciences and Chemistry from University of Missouri-Kansas City in 2014. After that, she joined as an assistant professor at the school of Pharmacy at Fairleigh Dickinson University. She has authored several research and review articles and book chapters. She also serves as a regular reviewer for many prestigious journals, as well as editorial board member for various journals. Her research interests include drug release analysis from transdermal patch, development of targeted delivery systems, ayurvedic treatment for arthritis, and pedagogical research

Kamna Srivastava has completed her B Pharm, M Pharm and PhD from Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, India. She held her Post-doctoral positions in National Institute of Immunology, All India Institute of Medical Sciences, New Delhi. Presently, she is working as an Assistant Professor in Molecular Cardiology Lab in Dr. B R Ambedkar Centre for Biomedical Research, Delhi University. Her on-going project is focused on the identifying the potential biomarkers for cardiovascular diseases. She has more than 30 research publications to her credit and recipient of grants from DST, CSIR and ICMR India.

Background: Hypertension is one of the major risk factors for cardiovascular diseases. It has been suggested that genetic backgrounds, which have an association with essential hypertension, may also determine the responsiveness to ACE inhibitor. We determined the association of angiotensinogen gene polymorphism with essential hypertension and the relationship between polymorphism in the angiotensinogen (M235T) gene and blood pressure response to ACE inhibitor (enalapril) in patients with essential hypertension. Th e present study is also about a particular genetic polymorphism (A1166C), gene expression and protein expression of the angiotensin II type I receptor (AT1R) and its association with essential hypertension in a Northern Indian population. Methods: 250 patients with essential hypertension and 250 normal healthy controls from Delhi and surrounding areas were recruited for the investigation. Blood pressure was recorded before and aft er 6 weeks of treatment with ACE inhibitors, Enalapril. Genotyping were carried out by PCR and RFLP technique and expression analysis at mRNA levels by real-time PCR. Results and Conclusions: Statistically signifi cant association of T allele was observed with essential hypertension [x2=14.67, p=0.00013, Odds ratio=1.76 (1.3-2.32) at 95% CI]. Th e decrease in systolic blood pressure and diastolic blood pressure after six weeks of treatment of the patients carrying TT genotype were greater than the groups carrying MT and MM genotypes. Th e angiotensinogen (M235T) gene polymorphism is signifi cantly associated with essential hypertension. Patients carrying TT genotype had higher blood pressure lowering response when treated with ACE inhibitor, Enalapril than those carrying MM and MT genotypes suggesting that the T allele may be a possible genetic marker for essential hypertension. Our findings also suggest that C allele of A1166C polymorphism in the angiotensin II type 1 receptor gene is associated with essential

hypertension and its upregulation could play an important role in essential hypertension

Xiping Zhan has his expertise in neuropharmacology. His lab uses multiple interdisciplinary approaches to study neural circuits and underlying functional implications. He applies behavior measures to evaluate the neuropharmacology of small molecular drugs on tinnitus, tremor or mood behavior, and uses patch clamping or single unit in vivo recording to address the molecular mechanisms. In addition, he uses human iPS cell derived dopamine neurons to model pharmacology in human. He has been focused on tinnitus and tremor for years in research and teaching

Essential tremor is one of the most common neurological disorders characterized by uncontrollable shaking and tremors throughout the body. Well known to aff ect adults, it can also aff ect children. Harmaline induced tremor is an established animal model for human essential tremor, but its underlying mechanism and eff ects on mood behavior are still elusive. This study aims to use pharmacological and behavioral methods to investigate the pharmacology in harmaline-induced tremor and the auditory startle response. Mice tremors and auditory startle responses were recorded by the Kinder Startle Monitor System. Harmaline (12.5 mg/kg) reliably induced tremor, and that can be attenuated by ethanol (1.5 mg/kg) and sulpiride (20 mg/kg). In addition, it caused the startle response to decrease signifi cantly. Prepulse inhibition and gap responses also decreased upon harmaline injection and increased the following day, but not signifi cantly from the controls. Supplemental administration following recovery can signifi cantly attenuate gap detection without affecting prepulse inhibition. Our data confi rms the frequency of the tremor was from 10 -15 Hz, and the ethanol eff ect, which indicates validity as novel tremor assay. We also found that harmaline attenuates the auditory startle refl ex by causing the reflex and gap detection to be suppressed, but did not aff ect prepulse inhibition signifi cantly. Th ese fi ndings suggest harmaline not only specifi cally modulates sensory-motor integration, but also the timing of gap detection. Our data provides additional information that D2 receptors are involved in harmaline-induced tremor.

Lúzio G B Flauzino has completed his Graduation in Industrial Chemistry from the University of Franca (year 2011). During his graduation, he undertook a scientific initiation phase with the group of Natural Products (GPNUF) developing the project- Molecules of interest: isolation, identifi cation, structural modifi cations and evaluation in several biological tests with FAPESP technical training grant (Proc. FAPESP (Proc. No. 2014 / 08404-6), which develops the project phytochemical studies of Villa elliptica and Vellozia variabilis and evaluation in tests against neglected tropical diseases.

Schistosomiasis is a neglected tropical disease that infects over 200 million people worldwide and it is caused by schistosomes (parasitic trematodes). Its treatment relies only on Praziquantel, a drug which shows toxic side eff ects, lack of eff ectiveness against young worms and it may be less useful in the future due to the drug-resistance of schistosomes. Th us, alternative drugs for the treatment are required. Th e crude ethanolic stem extract from Vellozia variabillis (Velloziaceae) has shown in vitro schistosomicidal activity against adult worms of Schistosoma mansoni. Further, the fl avoliganan hydnocarpin D (Figure 1) was isolated from stem extract by chromatographic fractionation plus preparative HPLC; identifi ed by ¹H- NMR, ¹³C-NMR, mass spectrometry methods and evaluated in vitro against S. mansoni. Adult worms of S. mansoni LE strain was recovered from the mesenteric veins of the infected mice and cultured in 24-well plates at 37°C in RPMI1640 media. Hydnocarpin D was dissolved in 10% DMSO and diluted into the medium to give 12.5, 25, 50, 100 and 200 μM. Adult worms were kept for 72 hours and the viability was monitored every 24 hours. As negative control was used adult worms treated with 10% DMSO. Th e biological assay has shown that Hydnocarpin D caused the death of the S. mansoni adult worms (100% at 200 and 100 μM, and 75% at 50 μM aft er 48 hours; 100% at 25 μM aft er 72 hours) and reduced the motor activity signifi cantly of 100% of the adult worms (25, 50, 100, 200 μM aft er 24 hours and at 12,5μM aft er 72 hours). It was also registered a partial tegument alteration at 50, 100 and 200μM. Hydnocarpin D showed good results and can be a good choice to futures studies for the seeking of alternative drugs to schistosomiasis treatment.

Bhabani Sankar Satapathy has 6 years of experience in drug delivery research. He has worked as a Senior Research Fellow in the Dept. of Pharm. Tech., Jadavpur University, India under DST/Inspire fellowship, Govt. of India. His basic research area includes novel approaches like nanoparticles, nanosclae liposomes for targeted drug delivery in the treatment of various cancers like breast and liver. Currently, his research focuses on the brain targeted nanodrug delivery systems for treatment of brain cancer.

Eff ective management of brain related ailments continues to be the challenging area in neuroscience research. Lipid based nanosize carriers owing to their structural uniqueness possess the ability to cross blood-brain barrier (BBB); the major hurdle for the successful transport of therapeutic agents into brain. Th e present study aimed for the development of a phospholipid based nanosize carrier encapsulating a plant derived therapeutic agent and investigation of its BBB crossing potential in vivo. Th e optimized formulation had a size range between 20-50 nm with smooth surface morphology. The formulation showed a narrow size distribution pattern with nearly 8% drug loading capacity. Cryo-transmission electron microscopy study revealed stable formation without any perforation on the outer surface. A sustained drug release profi le was observed for the experimental formulation up to 24 hours study period. Pharmacokinetic and biodistribution data showed an enhanced residence time of the experimental nanocarrier in brain as compared to the free drug. Gamma scintigraphy studies clearly evidenced an

efficient permeation of the nanocarriers through the BBB, as compared to the free drug. Further investigations are warranted to establish its future use in clinical practice.

Saif S Abbas is pursuing his Master’s degree in Pharmaceutics/Pharmacokinetics at Al-Ahliyya Amman University in Jordan. He has completed his graduation from Faculty of Pharmacy and Medical Sciences in Al-Ahliyya Amman University/Jordan in 2013. He worked as a Senior Pharmacist in retail pharmacies and drug stores in Amman/Jordan.

Ivabradine is a new hyperpolarization-activated cyclic nucleotide-gated channel blocker. It has been approved by the FDA in 2015 in management of stable angina and congestive heart failure. Th e aim of this study was to investigate the possibility of pharmacokinetic interaction of a proposed combination of ivabradine and the β-blocker carvedilol in rats using spectroscopy technique. A simple, rapid and sensitive method for validation and determination of ivabradine and carvedilol in the rat’s plasma was developed using HPLC/MS. The method was successfully developed and validated in terms of linearity, precision and accuracy which were within the values accepted by EMEA and ICH. Ivabradine and carvedilol were given both intravenously and orally each alone and as oral combination to fasted Sprague-Dawley rats. Blood samples were withdrawn on scheduled time intervals up to 36 hours and analyzed for each drug. Both compartmental and non-compartmental kinetic analysis was performed on plasma level-time data and the kinetic parameters were calculated from non-compartmental analysis. Results showed signifi cant increase in bioavailability of both drugs in combination (94% for carvedilol and 58% for ivabradine). Also, Cmax was changed signifi cantly from by 165% for carvedilol and 56% for ivabradine when given in combination. There was also a signifi cant decrease in elimination of both drugs expressed as 48% decrease in clearance and 41% increase in the halflife for carvedilol and 32% decrease in clearance and 37% increase of the half-life of ivabradine when given in combination. These changes suggested an interaction on metabolic function of the liver on both drugs by enzyme inhibition. Also, the rate of absorption of ivabradine was slowed by concomitant administration of carvedilol suggesting an interaction on absorption level. In conclusion, a signifi cant kinetic interaction occurred when ivabradine was given orally with carvedilol which makes

dose adjustment of both drugs of much importance.

Osama M Al-Quteimat has completed his Master’s degree in Clinical Pharmacy from University of Jordan. He is a board-certifi ed Oncology Pharmacist working as Senior Inpatient Pharmacist in Cleveland Clinic Abu Dhabi, a leading healthcare institution providing high-quality tertiary healthcare, education and research in United Arab Emirates. His main interests include pharmaceutical care, oncology pharmacy and patient education. He has published many papers in the field of clinical pharmacy in reputed journals.

Pharmacy is a very dynamic profession and the role of the pharmacist is improving with the expansion of the scope of services and the introduction of new subspecialties over time. Moving from being medication dispensers to outcomeoriented and patient-focused care providers; pharmacists will carry more responsibility and commitment to improve their knowledge and practice. Being updated and evidence-based is a key tool to achieve eff ective pharmaceutical care services. The primary purpose of this article is to highlight the concept of “evidence based pharmaceutical care” as professional practice to improve the quality of pharmaceutical care. Th ere is strong data showing that pharmaceutical care lead to improvement in health outcomes and cost-eff ective therapy. More eff orts, policies and qualifi ed staff are needed to establish the “evidencebased pharmaceutical care” as new daily professional practice. Evidence to support pharmacists in their emerging role as care providers is available to improve the effi cacy and quality of pharmaceutical care. Education and specialized training practicing evidence based approach are vital to prepare pharmacists to provide high quality pharmaceutical care. As care providers, pharmacists are eff ective in providing high quality patient care and being members in multidisciplinary clinical teams is needed to give them the opportunity. Evidence based pharmaceutical care is a natural and logical emerging concept in the modern pharmacy practice to achieve high quality and more eff ective pharmaceutical care but still more eff orts and resources are needed to promote new attitude toward more professional career

Krishna Gajjar is a Pharma Student, having Bachelors and Master degree in Pharmacy and currently pursuing PhD as Research Fellow (in Pharmaceutical Sciences- specialization in Medicinal Chemistry) from Nirma University, Ahmedabad, (Gujarat) India, under the guidance of Prof. Anuradha K. Gajjar.

Free fatty-acid receptor 1, is a G-protein-coupled receptor that binds long chain free fatty acids to enhance glucose-dependent insulin secretion and are therefore viable targets for diabetes and metabolic disorders. In the course of the research work, QSAR study, Pharmacophore generation, Molecular Docking, in-silico ADME studies and synthesis was performed to explore the molecular determinants responsible for the agonist action at GPR40. Th e generation of ligand & structure based pharmacophore using the standard tools within Catalyst from diff erent training sets consisted of Hydrophobic, Hydrogen Bond Acceptor and Aromatic ring features as essential aspects. Th e most representative features were selected and included in

the pharmacophore model which was further validated and utilized as a query tool to search 3D databases. CoMFA, CoMSIA and HQSAR were performed on series of 3-aryl-3-ethoxypropanoic acid derivatives to build 3D-QSAR models. Contour maps provided signifi cant insights which gave hints for the modifi cation required to design new molecules with improved biological activity. Molecular docking studies were carried out on designed molecules using Sybyl-X soft ware. Out of these the best Heteroaryl systems, specifi cally the fi ve membered pyrazole ring system was being explored and some of the virtual structures were synthetically explored, and 3-[3-(4-methoxyphenyl)-4-(phenoxymethyl)-1H-pyrazol-1-yl] acetic acid derivative class of compounds were synthesized taking into the account of sustainability and feasibility of the chemistry, which may act as a starting point for the in-house discovery program.