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Dive into the research topics where Sujay Basu is active.

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Featured researches published by Sujay Basu.


Bioorganic & Medicinal Chemistry Letters | 2012

Discovery of novel and potent heterocyclic carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors.

Sujay Basu; Uppuleti Viplava Prasad; Dinesh Barawkar; Siddhartha De; Venkata P. Palle; Suraj Menon; Meena Patel; Sachin Thorat; Umesh Prasad Singh; Koushik Das Sarma; Yogesh Waman; Sanjay Niranjan; Vishal Pathade; Ashwani Gaur; Satyanarayana Reddy; Shariq Ansari

A series of novel heterocyclic carboxylic acid based protein tyrosine phosphatase 1B (PTP1B) inhibitors with hydrophobic tail have been synthesized and characterized. Structure-activity relationship (SAR) optimization resulted in identification of several potent, selective (over the highly homologous T-cell protein tyrosine phosphatase, TCPTP) and metabolically stable PTP1B inhibitors. Compounds 7a, 19a and 19c showed favorable cell permeability and pharmacokinetic properties in mouse with moderate to very good oral (% F=13-70) bio-availability.


Bioorganic & Medicinal Chemistry Letters | 2011

Revisiting glitazars: Thiophene substituted oxazole containing α-ethoxy phenylpropanoic acid derivatives as highly potent PPARα/γ dual agonists devoid of adverse effects in rodents ☆

Preeti Raval; Mukul R. Jain; Amitgiri Goswami; Sujay Basu; Archana Gite; Atul Godha; Harikishore Pingali; Saurin Raval; Suresh Giri; Dinesh Suthar; Maanan Shah; Pankaj R. Patel

In an effort to develop safe and efficacious compounds for the treatment of metabolic disorders, novel thiophene substituted oxazole containing α-alkoxy-phenylpropanoic acid derivatives are designed as highly potent PPARα/γ dual agonists. These compounds were found to be efficacious at picomolar concentrations. Lead compound 18d has emerged as very potent PPARα/γ dual agonist demonstrating potent antidiabetic and lipid lowering activity at a very low dose and did not exhibit any significant signs of toxicity in rodents.


Bioorganic & Medicinal Chemistry Letters | 2008

Discovery of a highly orally bioavailable c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid as a potent hypoglycemic and hypolipidemic agent ☆

Harikishore Pingali; Mukul R. Jain; Shailesh R. Shah; Sujay Basu; Pankaj Makadia; Amitgiri Goswami; Pandurang Zaware; Pravin Patil; Atul Godha; Suresh Giri; Ashish Goel; M. N. Patel; Harilal Patel; Pankaj R. Patel

A series of novel 1,3-dioxane-2-carboxylic acid derivatives containing alkyl chain tether and substituted phenyl group as a lipophilic tail have been prepared as agonists of PPARalpha and gamma. c-5-[6-(4-Methanesulfonyloxyphenyl)hexyl]-2-methyl-1,3-dioxane-r-2-carboxylic acid 13c exhibited potent hypoglycemic and lipid lowering activity with high oral bioavailability in animal models.


Journal of Medicinal Chemistry | 2017

Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A2A Receptor Antagonists and Their Biological Evaluation

Sujay Basu; Dinesh Barawkar; Sachin Thorat; Yogesh Shejul; Meena V. Patel; Minakshi Naykodi; Vaibhav Jain; Yogesh Salve; Vandna Prasad; Sumit Chaudhary; Indraneel Ghosh; Ganesh Bhat; Azfar Quraishi; Harish Patil; Shariq Ansari; Suraj Menon; Vishal Unadkat; Rhishikesh Thakare; Madhav S. Seervi; Ashwinkumar V. Meru; Siddhartha De; Ravi K. Bhamidipati; Sreekanth R. Rouduri; Venkata Palle; Anita Chug; Kasim A. Mookhtiar

Our initial structure-activity relationship studies on 7-methoxy-4-morpholino-benzothiazole derivatives featured by aryloxy-2-methylpropanamide moieties at the 2-position led to identification of compound 25 as a potent and selective A2A adenosine receptor (A2AAdoR) antagonist with reasonable ADME and pharmacokinetic properties. However, poor intrinsic solubility and low to moderate oral bioavailability made this series unsuitable for further development. Further optimization using structure-based drug design approach resulted in discovery of potent and selective adenosine A2A receptor antagonists bearing substituted 1-methylcyclohexyl-carboxamide groups at position 2 of the benzothiazole scaffold and endowed with better solubility and oral bioavailability. Compounds 41 and 49 demonstrated a number of positive attributes with respect to in vitro ADME properties. Both compounds displayed good pharmacokinetic properties with 63% and 61% oral bioavailability, respectively, in rat. Further, compound 49 displayed oral efficacy in 6-OHDA lesioned rat model of Parkinson diseases.


Bioorganic & Medicinal Chemistry | 2017

Rational design, synthesis, and structure-activity relationships of 5-amino-1H-pyrazole-4-carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors

Sujay Basu; Philip Prathipati; Sachin Thorat; Shariq Ansari; Meena V. Patel; Vaibhav Jain; Ramana R. Jinugu; Sanjay Niranjan; Siddhartha De; Satyanarayana Reddy

A series of novel amino-carboxylic based pyrazole as protein tyrosine phosphatase 1B (PTP1B) inhibitors were designed on the basis of structure-based pharmacophore model and molecular docking. Compounds containing different hydrophobic tail (1,2-diphenyl ethanone, oxdiadizole and dibenzyl amines) were synthesized and evaluated in PTP1B enzymatic assay. Structure-activity relationship based optimization resulted in identification of several potent, metabolically stable and cell permeable PTP1B inhibitors.


Bioorganic & Medicinal Chemistry | 2017

Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A1 receptor antagonists and their biological evaluation

Summon Koul; Vidya Ramdas; Dinesh Barawkar; Yogesh Waman; Neela Prasad; Santosh Kumar Madadi; Yogesh Shejul; Rajesh Bonagiri; Sujay Basu; Suraj Menon; Srinivasa B. Reddy; Sandhya Chaturvedi; Srinivas Rao Chennamaneni; Gaurav Bedse; Rhishikesh Thakare; Jayasagar Gundu; Sumit Chaudhary; Siddhartha De; Ashwinkumar V. Meru; Venkata Palle; Anita Chugh; Kasim A. Mookhtiar

Multipronged approach was used to synthesize a library of diverse C-8 cyclopentyl hypoxanthine analogs from a common intermediate III. Several potent and selective compounds were identified and evaluated for pharmacokinetic (PK) properties in Wistar rats. One of the compounds 14 with acceptable PK parameters was selected for testing in in vivo primary acute diuresis model. The compound demonstrated significant diuretic activity in this model.


ACS Medicinal Chemistry Letters | 2017

Discovery of Potent and Selective A2A Antagonists with Efficacy in Animal Models of Parkinson’s Disease and Depression

Sujay Basu; Dinesh Barawkar; Vidya Ramdas; Minakshi Naykodi; Yogesh Shejul; Meena V. Patel; Sachin Thorat; Anil Panmand; K. Kashinath; Rajesh Bonagiri; Vandna Prasad; Ganesh Bhat; Azfar Quraishi; Sumit Chaudhary; Amol Magdum; Ashwinkumar V. Meru; Indraneel Ghosh; Ravi K. Bhamidipati; Amol A. Raje; Vamsi Madgula; Siddhartha De; Sreekanth R. Rouduri; Venkata Palle; Anita Chugh; Narayanan Hariharan; Kasim A. Mookhtiar

Adenosine A2A receptor (A2AAdoR) antagonism is a nondopaminergic approach to Parkinsons disease treatment that is under development. Earlier we had reported the therapeutic potential of 7-methoxy-4-morpholino-benzothiazole derivatives as A2AAdoR antagonists. We herein described a novel series of [1,2,4]triazolo[5,1-f]purin-2-one derivatives that displays functional antagonism of the A2A receptor with a high degree of selectivity over A1, A2B, and A3 receptors. Compounds from this new scaffold resulted in the discovery of highly potent, selective, stable, and moderate brain penetrating compound 33. Compound 33 endowed with satisfactory in vitro and in vivo pharmacokinetics properties. Compound 33 demonstrated robust oral efficacies in two commonly used models of Parkinsons disease (haloperidol-induced catalepsy and 6-OHDA lesioned rat models) and depression (TST and FST mice models).


Archive | 2008

2,2,2-tri-substituted acetamide derivatives as glucokinase activators, their process and pharmaceutical application

Kasim A. Mookhtiar; Debnath Bhuniya; Bhavesh Dave; Gobind Singh Kapkoti; Sujay Basu; Anita Chugh; Siddhartha De; Venkata P. Palle


Archive | 2002

Novel pyrroles having hypolipidemic hypocholesteremic activities, process for their preparation and pharmaceutical compositions containing them and their use in medicine

Braj Bhushan Lohray; Vidya Bhushan Lohray; Vijay Kumar Gajubhai Barot; Saurin Raval; Preeti Raval; Sujay Basu


Archive | 2009

Heterocyclic compounds as adenosine receptor antagonist

Venkata P. Palle; Sujay Basu; Yogesh Waman; Vidya Ramdas; Dinesh Barawkar

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Yogesh Waman

Takeda Pharmaceutical Company

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Anil Panmand

Takeda Pharmaceutical Company

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Preeti Raval

Maharaja Sayajirao University of Baroda

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Braj Bhushan Lohray

Indian Institute of Technology Kanpur

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