作者
Anna C Cunha, Juliana M Figueiredo, Jorge LM Tributino, Ana LP Miranda, Helena C Castro, Russolina B Zingali, Carlos AM Fraga, Maria Cecı́lia BV de Souza, Vitor F Ferreira, Eliezer J Barreiro
发表日期
2003/5/1
期刊
Bioorganic & medicinal chemistry
卷号
11
期号
9
页码范围
2051-2059
出版商
Pergamon
简介
This paper describes the design, synthesis and pharmacological evaluation of new N-acylhydrazone (NAH) compounds, belonging to the N-substituted-phenyl-1,2,3-triazole-4-acylhydrazone class (2a–p). Classical heteroaromatic ring bioisosterism strategies were applied to the previously reported N-phenylpyrazolyl-4-acylhydrazone derivative 1, elected as lead-compound due to its important anti-aggregating profile on arachidonic acid induced platelet aggregation (IC50=24±0.5μM), from which emerge this new series 2. These new compounds 2a–p were readily synthesized, characterized and tested on platelet aggregation assays induced by collagen (5μg/mL), ADP (5μM) and arachidonic acid (100μM) in rabbit citrated platelet-rich plasma. Compounds 2b, 2d, and 2h were found to be the most potent, exhibiting a significant antiplatelet activity on arachidonic acid- and collagen-induced platelet aggregation. In …
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