ChemInform Abstract: Synthesis and Bioactivity of Novel Bis(heteroaryl)piperazine (BHAP) Reverse Transcriptase Inhibitors: Structure-Activity Relationships and Increased Metabolic Stability of Novel Substituted Pyridine Analogues.
✍ Scribed by M. J. GENIN; T. J. POEL; Y. YAGI; C. BILES; I. ALTHAUS; B. J. KEISER; L. A. KOPTA; J. M. FRIIS; F. REUSSER; W. J. ADAMS; R. A. OLMSTED; R. L. VOORMAN; R. C. THOMAS; D. L. ROMERO
- Publisher
- John Wiley and Sons
- Year
- 2010
- Weight
- 33 KB
- Volume
- 28
- Category
- Article
- ISSN
- 0931-7597
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✦ Synopsis
Synthesis and Bioactivity of Novel Bis(heteroaryl)piperazine (BHAP) Reverse Transcriptase Inhibitors: Structure-Activity Relationships and Increased Metabolic Stability of Novel Substituted Pyridine Analogues.
-Piperazine-containing compounds such as (VII) (11 examples) and piperidine containing analogues such as (X) (10 examples) are synthesized and tested for HIV-1 RT inhibitory activity. The active analogues are further evaluated to determine their metabolic stability in vitro. In general, a 3-ethoxy or 3-isopropoxy substituent on the pyridine ring results in enhanced stability. The nature of the indole substitution sometimes plays a significant role in the metabolic stability, particularly in the series of compounds (VII). -(GENIN, M.