NONNUCLEOSIDE INHIBITORS OF HIV-1 REVERSE-TRANSCRIPTASE - MOLECULAR MODELING AND X-RAY STRUCTURE INVESTIGATIONS

被引：145

作者：

SCHAFER, W ^{[1
]}

FRIEBE, WG ^{[1
]}

LEINERT, H ^{[1
]}

MERTENS, A ^{[1
]}

POLL, T ^{[1
]}

VONDERSAAL, W ^{[1
]}

ZILCH, H ^{[1
]}

NUBER, B ^{[1
]}

ZIEGLER, ML ^{[1
]}

机构：

[1] UNIV HEIDELBERG,INST ANORGAN CHEM,W-6900 HEIDELBERG,GERMANY

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 06期

关键词：

D O I：

10.1021/jm00058a009

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The structural features of a new class of non-nucleoside HIV-1 reverse transcriptase inhibitors (3) are presented. Comparison of the structural and electronic properties with those of TIBO (1) and Nevirapine (2) yields a common three-dimensional model. This model permits the improvement of the lead compound 3 by chemical modification (5, 6). Additionally, two new types of inhibitors (4, 7) with similar biological activity can be derived from this model. The structures of the new compounds, including their absolute configuration, are determined by X-ray crystallography.

引用

页码：726 / 732

页数：7

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