Premium
Synthesis, Characterization, and Biological Evaluation of Novel 3‐(4‐Chlorophenyl)‐2‐(substituted)quinazolin‐4(3 H )‐one Derivatives as Multi‐target Anti‐inflammatory Agents
Author(s) -
Raghu M. S.,
Pradeep Kumar C. B.,
Yogesh Kumar K.,
Prashanth M. K.,
Jayanna B. K.
Publication year - 2019
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3585
Subject(s) - chemistry , anti inflammatory , cyclooxygenase , in vitro , proinflammatory cytokine , stereochemistry , biological activity , inhibitory postsynaptic potential , enzyme , combinatorial chemistry , pharmacology , biochemistry , inflammation , medicine , neuroscience , biology
A novel class of 3‐(4‐chlorophenyl)‐2‐(substituted)quinazolin‐4(3 H )‐one derivatives were synthesized, and the structure of synthesized compounds was characterized by IR, 1 H NMR, and mass spectroscopy. The newly synthesized compounds ( 4a–g and 6a–g ) were tested for their in vitro cyclooxygenase (COX) inhibition activity. The compounds have inhibitory profile against both COX‐1 and COX‐2, and some of the compounds are found to be selective against COX‐2. The compound 6g showed distinct inhibitory activity on COXs. The synthesized compounds were evaluated for their potential anti‐inflammatory activity as inhibitors of the proinflammatory cytokines IL‐6. Compounds 4d – g showed the highest level of inhibition among all the tested compounds. Thus, our data suggested that these compounds may represent a new class of potent anti‐inflammatory agents.