S
Siddhartha De
Publications - 17
Citations - 288
Siddhartha De is an academic researcher. The author has contributed to research in topics: Chemistry & Acetamide. The author has an hindex of 10, co-authored 15 publications receiving 230 citations.
Papers
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Journal ArticleDOI
Discovery of a potent and selective small molecule hGPR91 antagonist.
Debnath Bhuniya,Dhananjay N. Umrani,Bhavesh Dave,Deepak B. Salunke,Gagan Kukreja,Jayasagar Gundu,Minakshi Naykodi,Nadim S. Shaikh,Prasad Shitole,Santosh Kurhade,Siddhartha De,Sreemita Majumdar,Srinivasa B. Reddy,Suhas Tambe,Yogesh D. Shejul,Anita Chugh,Venkata P. Palle,Kasim A. Mookhtiar,Doris F. Cully,Joseph P. Vacca,Prasun K. Chakravarty,Ravi P. Nargund,Samuel D. Wright,Michael P. Graziano,Sheo B. Singh,Sophie Roy,Tian-Quan Cai +26 more
TL;DR: A rat pharmacodynamic assay was developed to characterize the antagonists in vivo using succinate induced increase in blood pressure, and the GPR91 target engagement was subsequently demonstrated using the designed pharmacodynamics assay.
Journal ArticleDOI
Design and synthesis of novel xanthine derivatives as potent and selective A 2B adenosine receptor antagonists for the treatment of chronic inflammatory airway diseases.
Sujay Basu,Dinesh A. Barawkar,Vidya Ramdas,Meena Patel,Yogesh Waman,Anil Panmand,Santosh Kumar,Sachin Thorat,Minakshi Naykodi,Arnab Goswami,B. Srinivasa Reddy,Vandna Prasad,Sandhya Chaturvedi,Azfar Quraishi,Suraj Menon,Shalini Paliwal,Abhay Kulkarni,Vikas Karande,Indraneel Ghosh,Syed Mustafa,Siddhartha De,Vaibhav Jain,Ena Ray Banerjee,Sreekanth R. Rouduri,Venkata P. Palle,Anita Chugh,Kasim A. Mookhtiar +26 more
TL;DR: Several prop-2-ynylated C8-aryl or heteroaryl substitutions on xanthine chemotype were explored and found that 1-prop-2 -ynyl-1H-pyrazol-4-yl moiety was better tolerated at the C8 position and provided better selectivity for A2BAdoR compared to that of para-substituted analogs.
Patent
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 +7 more
TL;DR: In this paper, 2,2,2-tri-substituted acetamide derivatives of formula (I), its polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts and formulations thereof, useful as Glucokinase activator.
Journal ArticleDOI
Discovery of novel and potent heterocyclic carboxylic acid derivatives as protein tyrosine phosphatase 1B inhibitors
Sujay Basu,Uppuleti Viplava Prasad,Dinesh A. Barawkar,Siddhartha De,Venkata P. Palle,Suraj Menon,Meena Patel,Sachin Thorat,Umesh Prasad Singh,Koushik Das Sarma,Yogesh Waman,Sanjay Niranjan,Vishal V Pathade,Ashwani Gaur,Satyanarayana Reddy,Shariq S. Ansari +15 more
TL;DR: A series of novel heterocyclic carboxylic acid based protein tyrosine phosphatase 1B (PTP1B) inhibitors with hydrophobic tail showed favorable cell permeability and pharmacokinetic properties in mouse with moderate to very good oral bio-availability.
Journal ArticleDOI
Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.
Debnath Bhuniya,Rajendra K. Kharul,Hajare Atul Kashinath,Nadim S. Shaikh,Sandeep Bhosale,Sandip Balwe,Fouzia Begum,Siddhartha De,Sonalee Athavankar,Dhananjay Joshi,Vamsi Madgula,Kaushal Joshi,Amol A. Raje,Ashwinkumar V. Meru,Amol Magdum,Kasim A. Mookhtiar,Rashmi Barbhaiya +16 more
TL;DR: Based on comparative profile of FAAH potency, metabolic stability in liver microsome, liability of inhibiting major hCYP450 isoforms, rat PK, and brain penetration ability, two SAR optimized compounds were selected for efficacy study in rat model of chemotherapy-induced peripheral neuropathy (CIPN).