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新型非核苷类逆转录酶抑制剂色满酮衍生物12-氧代卡拉诺内酯A的体外抗人免疫缺陷病毒(HIV)活性

In vitro anti-human immunodeficiency virus (HIV) activity of the chromanone derivative, 12-oxocalanolide A, a novel NNRTI.

作者信息

Xu Z Q, Buckheit R W, Stup T L, Flavin M T, Khilevich A, Rizzo J D, Lin L, Zembower D E

机构信息

MediChem Research Inc., Lemont, IL 60439, USA.

出版信息

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2179-84. doi: 10.1016/s0960-894x(98)00380-1.

Abstract

The three chromanone derivatives, (+)-, (-)-, and (+/-)-12-oxocalanolide A (2), were evaluated for in vitro antiviral activities against HIV and simian immunodeficiency virus (SIV). The compounds were determined to be inhibitors of HIV-1 reverse transcriptase (RT) and exhibited activity against a variety of viruses selected for resistance to other HIV-1 nonnucleoside RT inhibitors. They are the first reported calanolide analogues capable of inhibiting SIV.

摘要

对三种色满酮衍生物,即(+)-、(-)-和(+/-)-12-氧代卡拉诺内酯A(2)进行了抗HIV和猿猴免疫缺陷病毒(SIV)的体外抗病毒活性评估。这些化合物被确定为HIV-1逆转录酶(RT)抑制剂,并对多种对其他HIV-1非核苷RT抑制剂耐药的病毒表现出活性。它们是首次报道的能够抑制SIV的卡拉诺内酯类似物。

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