Anti-HIV-1 activities and pharmacokinetics of new arylpiperazinyl fluoroquinolones

Anti-HIV-1 activities and pharmacokinetics of new arylpiperazinyl fluoroquinolones
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DOI:
10.1016/s0960-894x(02)00003-3
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发表时间:
2002-03-11
影响因子:
2.7
通讯作者:
Yamashita, M
Yamashita, M
中科院分区:
医学4区
文献类型:
--
作者:
Ohmine, T;Katsube, T;Yamashita, M

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报道了一系列新型芳基哌嗪基氟喹诺酮类药物的抗hiv -1活性和药代动力学。在C-8位点用三氟甲基修饰比用二氟甲氧基修饰更能获得更高的抗hiv -1活性。所研究的两种化合物在猴子中显示出相当高的抗hiv -1活性(IC50为90%)。(C) 2002 Elsevier Science Ltd.版权所有。
Anti-HIV-1 activities and pharmacokinetics of a series of novel arylpiperazinyl fluoroquinolones are reported. Modification at the C-8 position with a trifluoromethyl group was superior to that with a difluoromethoxy group to achieve higher anti-HIV-1 activity. Two compounds studied exhibited quite high anti-HIV-1 activities (IC50 90%) in monkeys. (C) 2002 Elsevier Science Ltd. All rights reserved.