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


BAYTAŞ S. , Inceler N., ÖZKAN Y. , Unlu S., Sahin M. F.

MEDICINAL CHEMISTRY RESEARCH, cilt.22, sa.12, ss.5922-5933, 2013 (SCI İndekslerine Giren Dergi) identifier identifier

  • Cilt numarası: 22 Konu: 12
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1007/s00044-013-0580-x
  • Dergi Adı: MEDICINAL CHEMISTRY RESEARCH
  • Sayfa Sayıları: ss.5922-5933

Özet

(E)-3-[3-(pyridin-4-yl)-1-phenyl-1H-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 IC50 of 20.2 and 30.3 mu M, 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.