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Your search keyword '"Laxmikant, Datrange"' showing total 4 results
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4 results on '"Laxmikant, Datrange"'

1. Discovery of Potent, Selective, and State-Dependent NaV1.7 Inhibitors with Robust Oral Efficacy in Pain Models: Structure–Activity Relationship and Optimization of Chroman and Indane Aryl Sulfonamides

Author

Shreyas Deshpande, Rashmi Talwar, Ganesh Navinchandra Gote, Jayasagar Gundu, Rupali Vyawahare, Shashikant Pawar, Akshaya Wagh, Talha Khan, Anil Kalia, Venkata P. Palle, Usha Dhayagude, M. K. Singh, Pradeep Patil, Ganesh Chaure, Praveen Kumar Gupta, Amit Das, Vijay Kanoje, Sharad Sharma, Vidya Ramdas, Vinod Patil, Rajesh Yeshodharan, Prashant B. Nigade, Dipak Modi, Dnyaneshwar Warude, Dilip Pandey, Jagadeesh Daler, Mahammad Azhar, Arun Nayak, Sneha Joshi, Sudipto Das, Rajender Kumar Kamboj, Javed S Shaikh, Maneesh Mehta, Deepak Sahebrao Walke, Rajesh V. Gupta, Himani Pareek, Kumar V S Nemmani, Parag Joshi, Mahip Verma, Vinod Mali, Laxmikant Datrange, Santosh Parkale, Rajesh Loriya, Vaibhav Kalhapure, Geetika Sharma, Ravindra R. Pal, Sagar Budhe, Gautam Agarwal, Sachin Suravase, Sagar Darekar, Mark G. Bock, Advait Arun Joshi, Moloy Banerjee, Smita Bhoskar, Amitesh Kishore, and Dhananjay Bakhle

Subjects
0303 health sciences, Bicyclic molecule, Sulfonamide (medicine), Indane, Pharmacology, 01 natural sciences, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, 03 medical and health sciences, chemistry.chemical_compound, chemistry, Pharmacokinetics, Drug Discovery, Neuropathic pain, medicine, Molecular Medicine, Structure–activity relationship, Thiazole, CYP2C9, 030304 developmental biology, medicine.drug
Abstract

Voltage-gated sodium channel NaV1.7 is a genetically validated target for pain. Identification of NaV1.7 inhibitors with all of the desired properties to develop as an oral therapeutic for pain has been a major challenge. Herein, we report systematic structure-activity relationship (SAR) studies carried out to identify novel sulfonamide derivatives as potent, selective, and state-dependent NaV1.7 inhibitors for pain. Scaffold hopping from benzoxazine to chroman and indane bicyclic system followed by thiazole replacement on sulfonamide led to identification of lead molecules with significant improvement in solubility, selectivity over NaV1.5, and CYP2C9 inhibition. The lead molecules 13, 29, 32, 43, and 51 showed a favorable pharmacokinetics (PK) profile across different species and robust efficacy in veratridine and formalin-induced inflammatory pain models in mice. Compound 51 also showed significant effects on the CCI-induced neuropathic pain model. The profile of 51 indicated that it has the potential for further evaluation as a therapeutic for pain.

Published
2020
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2. Discovery of Potent, Selective, and State-Dependent Na

Author

Vidya, Ramdas, Rashmi, Talwar, Vijay, Kanoje, Rajesh M, Loriya, Moloy, Banerjee, Pradeep, Patil, Advait Arun, Joshi, Laxmikant, Datrange, Amit Kumar, Das, Deepak Sahebrao, Walke, Vaibhav, Kalhapure, Talha, Khan, Ganesh, Gote, Usha, Dhayagude, Shreyas, Deshpande, Javed, Shaikh, Ganesh, Chaure, Ravindra R, Pal, Santosh, Parkale, Sachin, Suravase, Smita, Bhoskar, Rajesh V, Gupta, Anil, Kalia, Rajesh, Yeshodharan, Mahammad, Azhar, Jagadeesh, Daler, Vinod, Mali, Geetika, Sharma, Amitesh, Kishore, Rupali, Vyawahare, Gautam, Agarwal, Himani, Pareek, Sagar, Budhe, Arun, Nayak, Dnyaneshwar, Warude, Praveen Kumar, Gupta, Parag, Joshi, Sneha, Joshi, Sagar, Darekar, Dilip, Pandey, Akshaya, Wagh, Prashant B, Nigade, Maneesh, Mehta, Vinod, Patil, Dipak, Modi, Shashikant, Pawar, Mahip, Verma, Minakshi, Singh, Sudipto, Das, Jayasagar, Gundu, Kumar, Nemmani, Mark G, Bock, Sharad, Sharma, Dhananjay, Bakhle, Rajender Kumar, Kamboj, and Venkata P, Palle

Subjects
Male, Voltage-Gated Sodium Channel Blockers, Mice, Inbred BALB C, Sulfonamides, NAV1.7 Voltage-Gated Sodium Channel, Drug Evaluation, Preclinical, Disease Models, Animal, Mice, Structure-Activity Relationship, Drug Design, Animals, Cytochrome P-450 CYP3A, Neuralgia, Protein Isoforms, Chromans, Cytochrome P-450 CYP2C9, Half-Life
Abstract

Voltage-gated sodium channel Na

Published
2020

3. An Enantiospecific Route to (+)-(1R,3S)-cis-Chrysanthemic Acid from (-)-d-Pantolactone¹

Author

D. Srinivasa Reddy, Hajare Atul Kashinath, Laxmikant Datrange, Debnath Bhuniya, and Yellajyosula Lakshmi Narasimha Murthy

Subjects
chemistry.chemical_classification, Grob fragmentation, Stereochemistry, Alkene, Organic Chemistry, Metathesis, Chemical synthesis, Catalysis, Chrysanthemic acid, chemistry.chemical_compound, chemistry, Wittig reaction, Cyclopentene, Stereoselectivity
Abstract

In this paper, a novel route for the synthesis of (+)-(1R,3S)-cis-chrysanthemic acid is described. The use of readily available (-)-D-pantolactone as a starting point, application of ring-closing metathesis to form the cyclopentene intermediate, and Haller-Bauer/Grob-type fragmentation to form the target compound are the highlights of the present synthesis.

Published
2011
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4. Enantiospecific synthesis of sex pheromone of the obscure mealybug from pantolactone via tandem conjugate addition/cyclization

Author

Laxmikant Datrange, Debnath Bhuniya, D. Srinivasa Reddy, Samir Vyas, and Hajare Atul Kashinath

Subjects
chemistry.chemical_classification, Tandem, Double bond, Chemistry, Stereochemistry, Organic Chemistry, Biochemistry, Cascade reaction, Sex pheromone, Drug Discovery, Pheromone, Stereoselectivity, Enantiomer, Conjugate
Abstract

An efficient synthesis of an enantiomer of insect’s natural pheromone is reported starting from chiral pool d-(−)-pantolactone. Highly stereoselective tandem conjugate addition/cyclization sequence and hydrogenation of exocyclic double bond are the key steps in the present synthesis.

Published
2010
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