BI-RG-587对齐多夫定耐药的1型人类免疫缺陷病毒具有活性，并与齐多夫定具有协同作用。
BI-RG-587 is active against zidovudine-resistant human immunodeficiency virus type 1 and synergistic with zidovudine.
作者信息
Richman D, Rosenthal A S, Skoog M, Eckner R J, Chou T C, Sabo J P, Merluzzi V J
机构信息
University of California, San Diego 92161.
出版信息
Antimicrob Agents Chemother. 1991 Feb;35(2):305-8. doi: 10.1128/AAC.35.2.305.
Abstract
A series of dipyridodiazepinones have been shown to be potent inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. The lead compound, BI-RG-587, had a 50% inhibitory concentration of 84 nM against HIV-1 reverse transcriptase activity. This compound reduced plaque formation of HIV-1 in HeLa cells expressing the CD4 receptor by 50% at 15 nM. BI-RG-587 at comparable concentrations inhibited the production of p24 antigen following the acute infection of CEM T-lymphoblastoid cells or primary human monocyte-derived macrophages with HIV-1. No inhibitory effects against HIV-2 or against three picornaviruses were detected. Zidovudine (3'-azido-3'-deoxythymidine [AZT])-susceptible and AZT-resistant isolates of HIV-1 were equally susceptible to BI-RG-587. AZT and BI-RG-587 exhibited synergistic inhibition of HIV-1BRU at all concentrations examined.
摘要
一系列二吡啶并二氮杂卓酮已被证明是人类免疫缺陷病毒1型（HIV-1）逆转录酶的有效抑制剂。先导化合物BI-RG-587对HIV-1逆转录酶活性的50%抑制浓度为84 nM。该化合物在15 nM时可使表达CD4受体的HeLa细胞中HIV-1的噬斑形成减少50%。在CEM T淋巴母细胞或原代人单核细胞衍生巨噬细胞被HIV-1急性感染后，同等浓度的BI-RG-587可抑制p24抗原的产生。未检测到对HIV-2或三种微小核糖核酸病毒的抑制作用。对齐多夫定（3'-叠氮-3'-脱氧胸苷[AZT]）敏感和耐药的HIV-1分离株对BI-RG-587同样敏感。在所有检测浓度下，AZT和BI-RG-587对HIV-1BRU均表现出协同抑制作用。
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