Novel 1,3-diarylpyrazole acrylamides: synthesis, antiplatelet activity screening, and in silico evaluation studies

• Published in: Medicinal chemistry research Vol. 22; no. 12; pp. 5922 - 5933
• Main Authors: Baytas, Sultan Nacak, Inceler, Nazan, Ozkan, Yesim, Unlu, Serdar, Fethi Sahin, M.
• Format: Journal Article
• Language: English
• Published: New York Springer US 01-12-2013
• Subjects: Biochemistry; Biomedical and Life Sciences; Biomedicine; Cell Biology; Original Research; Pharmacology/Toxicology; 1,3-Diarylpyrazoles; Acryl amides; Arachidonic acid; Collagen; Antiplatelet activity
• ISSN: 1054-2523; 1554-8120
• DOI: 10.1007/s00044-013-0580-x

(
E
)-3-[3-(pyridin-4-yl)-1-phenyl-1
H
-pyrazole-4-yl]acryl amides were evaluated for their antiplatelet activities. Compounds
4o
and
4r
were found as active derivatives showing a potent inhibitory activity on the arachidonic acid-induced aggregation, with IC
50
of 20.2 and 30.3 μM, respectively. Compounds
4j
,
4k
, and
4u
presented significant inhibitor effect on collagen-induced platelet aggregation (73.1, 82.5, and 86.7 %, respectively). All synthesized compounds demonstrated good drug-likeness and drug-score values in silico evaluations.