1. Academic Validation
  2. Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors

Synthesis and anti-HIV activities of urea-PETT analogs belonging to a new class of potent non-nucleoside HIV-1 reverse transcriptase inhibitors

  • Bioorg Med Chem Lett. 1998 Jun 16;8(12):1511-6. doi: 10.1016/s0960-894x(98)00249-2.
C Sahlberg 1 R Noréen P Engelhardt M Högberg J Kangasmetsä L Vrang H Zhang
Affiliations

Affiliation

  • 1 Medivir AB, Huddinge, Sweden. christer.sahlberg@medivir.se
Abstract

A series of potent specific HIV-1 RT inhibitory compounds is described. The compounds are urea analogs of PETT (PhenylEthylThiazoleThiourea) derivatives and the series includes derivatives with an ethyl linker (1-6) and conformationally restricted analogs (7-13). The Antiviral activity is determined both at the RT level and in Cell Culture on both native and mutant forms of HIV-1. Many compounds display activity in the nM range against wt-RT.

Figures