Search

Your search keyword '"Goel, Rajan N."' showing total 4 results
Start Over Author "Goel, Rajan N."
4 results on '"Goel, Rajan N."'

1. LL-00066471, a novel positive allosteric modulator of α7 nicotinic acetylcholine receptor ameliorates cognitive and sensorimotor gating deficits in animal models: Discovery and preclinical characterization

Author

Verma, Mahip K., Goel, Rajan N., Bokare, Anand M., Dandekar, Manoj P., Koul, Sarita, Desai, Sagar, Tota, Santoshkumar, Singh, Nilendra, Nigade, Prashant B., Patil, Vinod B., Modi, Dipak, Mehta, Maneesh, Gundu, Jayasagar, Walunj, Sameer S., Karche, Navnath P., Sinha, Neelima, Kamboj, Rajender K., and Palle, Venkata P.

Published
2021
Full Text
View/download PDF

2. Dual PI3Kδγ inhibition demonstrates potent anticancer effects in diffuse large B-cell lymphoma models: Discovery and preclinical characterization of LL-00084282

Author

Verma, Mahip K., primary, Samant, Charudatt, additional, Kale, Ramesh, additional, Patra, Sukanya, additional, Mahajan, Nilesh, additional, Gholve, Milind K., additional, Marisetti, Ajitkumar, additional, Sunkara, Brahmam, additional, Naik, Aditya, additional, Shingare, Manisha, additional, Reddy, Madhusudhan, additional, Bokare, Anand M., additional, Akarte, Atul, additional, Koul, Sarita, additional, Nigade, Prashant B., additional, Patil, Vinod B., additional, Modi, Dipak, additional, Ahirrao, Prajakta, additional, Pawar, Shashikant, additional, Kuldharan, Sandip, additional, Dinchhana, Lal, additional, Mehta, Maneesh, additional, Gundu, Jayasagar, additional, Jana, Nirmal, additional, Vidhate, Prashant, additional, Mahangare, Sachin Jaysing, additional, Shukla, Manojkumar R., additional, Goel, Rajan N., additional, Bhonde, Mandar, additional, Kamboj, Rajender Kumar, additional, and Palle, Venkata P., additional

Published
2022
Full Text
View/download PDF

3. Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure–Activity Relationship and Preclinical Characterization

Author

Sinha, Neelima, primary, Karche, Navnath P., additional, Verma, Mahip Kalyan, additional, Walunj, Sameer S., additional, Nigade, Prashant B., additional, Jana, Gourhari, additional, Kurhade, Sanjay P., additional, Hajare, Anil K., additional, Tilekar, Ajay R., additional, Jadhav, Ganesh R., additional, Thube, Baban R., additional, Shaikh, Javed S., additional, Balgude, Sudhakar, additional, Singh, Lairikyengbam Bikramjit, additional, Mahimane, Vijaya, additional, Adurkar, Shridhar K., additional, Hatnapure, Girish, additional, Raje, Firoj, additional, Bhosale, Yogesh, additional, Bhanage, Dnyaneshwar, additional, Sachchidanand, Sachchidanand, additional, Dixit, Ruchi, additional, Gupta, Rajesh, additional, Bokare, Anand M., additional, Dandekar, Manoj, additional, Bharne, Ashish, additional, Chatterjee, Manavi, additional, Desai, Sagar, additional, Koul, Sarita, additional, Modi, Dipak, additional, Mehta, Maneesh, additional, Patil, Vinod, additional, Singh, Minakshi, additional, Gundu, Jayasagar, additional, Goel, Rajan N., additional, Shah, Chirag, additional, Sharma, Sharad, additional, Bakhle, Dhananjay, additional, Kamboj, Rajender Kumar, additional, and Palle, Venkata P., additional

Published
2019
Full Text
View/download PDF

4. Discovery of Novel, Potent, Brain-Permeable, and Orally Efficacious Positive Allosteric Modulator of α7 Nicotinic Acetylcholine Receptor [4-(5-(4-Chlorophenyl)-4-methyl-2-propionylthiophen-3-yl)benzenesulfonamide]: Structure–Activity Relationship and Preclinical Characterization

Author

Sinha, Neelima, Karche, Navnath P., Verma, Mahip Kalyan, Walunj, Sameer S., Nigade, Prashant B., Jana, Gourhari, Kurhade, Sanjay P., Hajare, Anil K., Tilekar, Ajay R., Jadhav, Ganesh R., Thube, Baban R., Shaikh, Javed S., Balgude, Sudhakar, Singh, Lairikyengbam Bikramjit, Mahimane, Vijaya, Adurkar, Shridhar K., Hatnapure, Girish, Raje, Firoj, Bhosale, Yogesh, Bhanage, Dnyaneshwar, Sachchidanand, Sachchidanand, Dixit, Ruchi, Gupta, Rajesh, Bokare, Anand M., Dandekar, Manoj, Bharne, Ashish, Chatterjee, Manavi, Desai, Sagar, Koul, Sarita, Modi, Dipak, Mehta, Maneesh, Patil, Vinod, Singh, Minakshi, Gundu, Jayasagar, Goel, Rajan N., Shah, Chirag, Sharma, Sharad, Bakhle, Dhananjay, Kamboj, Rajender Kumar, and Palle, Venkata P.

Abstract

The discovery of a series of thiophenephenylsulfonamides as positive allosteric modulators (PAM) of α7 nicotinic acetylcholine receptor (α7 nAChR) is described. Optimization of this series led to identification of compound 28,a novel PAM of α7 nicotinic acetylcholine receptor (α7 nAChR). Compound 28showed good in vitro potency, with pharmacokinetic profile across species with excellent brain penetration and residence time. Compound 28robustly reversed the cognitive deficits in episodic/working memory in both time-delay and scopolamine-induced amnesia paradigms in the novel object and social recognition tasks, at very low dose levels. Additionally, compound 28has shown excellent safety profile in phase 1 clinical trials and is being evaluated for efficacy and safety as monotherapy in patients with mild to moderate Alzheimer’s disease.

Published
2020
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results