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Piperazine and piperidine‐substituted 7‐hydroxy coumarins for the development of anti‐inflammatory agents
Author(s) -
Buran Kerem,
Reis Rengin,
Sipahi Hande,
Önen Bayram F. Esra
Publication year - 2021
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.202000354
Subject(s) - coumarin , piperazine , chemistry , carbonic anhydrase , piperidine , anti inflammatory , antimicrobial , drug , benzopyran , stereochemistry , enzyme , in vitro , pharmacology , combinatorial chemistry , biochemistry , organic chemistry , medicine
Coumarins (2 H ‐1‐benzopyran‐2‐one), derivatives that can be isolated from several plants, have been reported for their anticoagulant, antimicrobial, anti‐inflammatory, or anticancer activity. Some of these structures are currently approved for the treatment of cardiovascular diseases, as antibiotics or as an anticancer drug. Given the great potential of this structure and the limited number of studies that focus on molecules derived from carbon 8 of the benzopyranone heterocycle, we synthesized in this project 38 coumarin derivatives by substituting carbon 8 of the benzopyran ring with some aromatic and aliphatically substituted piperidines and piperazines. As a few of these structures were already shown to exhibit some carbonic anhydrase (CA) inhibition and as CA enzymes are reported to be closely related to inflammation, the synthesized derivatives were evaluated for their anti‐inflammatory activity in vitro. The results indicated that compounds 20 and 31 revealed promising anti‐inflammatory activity, as they demonstrated better activity than the reference drugs.