79508-09-1Relevant articles and documents
Design, synthesis, biological evaluation and in silico studies of pyrazole‐based nh2‐acyl oseltamivir analogues as potent neuraminidase inhibitors
Ye, Jiqing,Lin, Lin,Xu, Jinyi,Chan, Paul Kay-Sheung,Yang, Xiao,Ma, Cong
, (2021/05/05)
Oseltamivir represents one of the most successful neuraminidase (NA) inhibitors in the current anti‐influenza therapy. The 150‐cavity of NA was identified as an additional binding pocket, and novel NA inhibitors have been designed to occupy the 150‐cavity
Pyrazole derivatives as inhibitors of arachidonic acid-induced platelet aggregation
Levent, Serkan,?ali?kan, Burcu,?ift?i, Murat,?zkan, Ye?im,Yenicesu, Idil,ünver, Hüseyin,Banoglu, Erden
, p. 42 - 53 (2013/07/27)
Antiplatelet drugs are promising therapeutics to intervene with platelet aggregation in arterial thrombosis, most prominently in myocardial infarction and ischemic stroke. Here, we describe the synthesis and structure-activity relationships of potent inhibitors of platelet aggregation based on the 1,5-diarylpyrazol-3-carboxamide scaffold. Analogs from this series demonstrated potent anti-aggregatory activities against arachidonic acid-induced platelet aggregation, as measured by turbidimetric method of Born. 1,5-Diarylpyrazole-3- carboxamides obtained with small-basic amines (7, 8, 50, 51, 61, 62) displayed the strongest activity with IC50 values in low nanomolar range (5.7-83 nM). On the basis of their high potency in cellular environment, these straightforward pyrazole derivatives may possess potential in the design of more potent compounds for intervention with cardiovascular diseases.