Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity-Reference-Cited by-同舟云学术

Biphenyl scaffold for the design of NMDA-receptor negative modulators: molecular modeling, synthesis, and biological activity

Published:2022 Issue:7 Volume:13 Page:822-830
ISSN:2632-8682
Container-title:RSC Medicinal Chemistry
language:en
Short-container-title:RSC Med. Chem.

Author:

Karlov Dmitry S.¹^ORCID,Temnyakova Nadezhda S.²,Vasilenko Dmitry A.²,Barygin Oleg I.³,Dron Mikhail Y.³,Zhigulin Arseniy S.³,Averina Elena B.²^ORCID,Grishin Yuri K.²,Grigoriev Vladimir V.⁴,Gabrel'yan Alexey V.⁴,Aniol Viktor A.⁵,Gulyaeva Natalia V.⁵,Osipenko Sergey V.¹,Kostyukevich Yury I.¹,Palyulin Vladimir A.²^ORCID,Popov Petr A.¹^ORCID,Fedorov Maxim V.¹⁶

Affiliation:

1. Skolkovo Institute of Science and Technology, Skolkovo Innovation Center, 143026 Moscow, Russian Federation

2. Department of Chemistry, Lomonosov Moscow State University, 119991 Moscow, Russian Federation

3. I. M. Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, 194223 St. Petersburg, Russian Federation

4. Institute of Physiologically Active Compounds, Russian Academy of Sciences, 142432 Chernogolovka, Moscow Region, Russian Federation

5. Institute of Higher Nervous Activity and Neurophysiology, Russian Academy of Sciences, 117485 Moscow, Russian Federation

6. Sirius University of Science and Technology, 1 Olympic ave, 354340 Sochi, Russian Federation

Abstract

The activity of biphenyl-based NMDA receptor allosteric modulator identified in virtual screening (IC50 = 5 μM) was improved 100 times (IC50 = 50 nM); SAR is consistent with ifenprodil analogs.

Funder

Russian Science Foundation

Russian Academy of Sciences

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2022/MD/D2MD00001F

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