%0 Journal Article
%T Pyrazoles as Anti-inflammatory and Analgesic Agents: In-vivo and In-silico Studies.
%A Chahal G
%A Monga J
%A Rani I
%A Saini S
%A Devgun M
%A Husain A
%A Lal Khokra S
%J Antiinflamm Antiallergy Agents Med Chem
%V 23
%N 1
%D 2024
%M 38828869
暂无%R 10.2174/0118715230275741231207115011
%X <B>BACKGROUND: </B>Pyrazole is a well-known nucleus in the pharmacy field with a wide range of other activities in addition to anti-inflammatory and analgesic, i.e., anticonvulsant, antiviral, and anticancer activities. There are well-known marketed drugs having pyrazole moiety as celecoxib, and lonazolac as COX-II inhibitors.<BR><B>OBJECTIVE: </B>We aim to synthesize better anti-inflammatory than existing ones. Thiophene is also known for its analgesic and anti-inflammatory action. Thus, the fusion of both gives better anti-inflammatory agents. In the present studies, derivatives from two series of pyrazole were prepared by reacting substituted chalcone (3a-3f) derivatives prepared from 2-acetyl thiophene. They substituted aromatic aldehydes with phenyl hydrazine to form (5a-5f) and with 2, 4-dinitro phenyl hydrazine giving compounds (6a-6f) separately.<BR><B>METHODS: </B>Purified and characterized pyrazoles have been analyzed for in-vivo analgesic and anti-inflammatory activities by using standard methods. Compounds 5e, 5f, and 6d were proved to be potent analgesics and series (5a-5f) was found to have anti-inflammatory action, which was further validated using docking and ADME studies.<BR><B>RESULTS: </B>The ADME profile of synthesized compounds was found to be satisfactory.<BR><B>CONCLUSIONS: </B>The synthesized compounds can serve as lead for further drug designing.