Synthesis of 4-alkoxy-2-phenylquinoline derivatives as potent antiplatelet agents
2001; Elsevier BV; Volume: 11; Issue: 3 Linguagem: Inglês
10.1016/s0960-894x(00)00652-1
ISSN1464-3405
AutoresTing-Chia Ko, Mann‐Jen Hour, Jin‐Cherng Lien, Che‐Ming Teng, K H Lee, Sheng-Chu Kuo, Li‐Jiau Huang,
Tópico(s)Synthesis of β-Lactam Compounds
ResumoIn our continuing search for novel antiplatelet agents, 4-alkoxy derivatives of 2-phenylquinoline as well as related compounds were prepared. Through biological screening, a preliminary structure–antiplatelet activity relationship was established. Compounds 5-ethyl-4-methoxy-2-phenylquinoline (8), 4-ethoxy-5-ethyl-2-phenylquinoline (9), 4-ethoxycarbonylmethoxy-5-ethyl-2-phenylquinoline (10), 4-ethoxycarbonylbutoxy-5-ethyl-2-phenylquinoline (12) and 5-ethyl-4-(N-ethylcarboxido)methoxy-2-phenylquinoline (17) all demonstrated potent antiplatelet activity. Among them, compound 8 was the most potent with an IC50 value of 0.08 μM and was about 3-fold more active than indomethacin. The mechanism of antiplatelet action of 8 is possibly through its inhibition on cyclooxygenase or thromboxane synthetase.
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