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

C Sahlberg; R Noréen; P Engelhardt; M Högberg; J Kangasmetsä; L Vrang; H Zhang

doi:10.1016/s0960-894x(98)00249-2

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.

Authors

C Sahlberg¹, R Noréen, P Engelhardt, M Högberg, J Kangasmetsä, L Vrang, H Zhang

Affiliation

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

PMID: 9873380
DOI: 10.1016/s0960-894x(98)00249-2

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.

MeSH terms

Anti-HIV Agents / chemical synthesis*
Anti-HIV Agents / metabolism
Anti-HIV Agents / pharmacology*
Blood Proteins / metabolism
Cell Line
HIV-1 / drug effects*
Humans
Microbial Sensitivity Tests
Protein Binding
Reverse Transcriptase Inhibitors / chemical synthesis*
Reverse Transcriptase Inhibitors / metabolism
Reverse Transcriptase Inhibitors / pharmacology*
Structure-Activity Relationship
Thiazoles / chemistry
Thiazoles / metabolism
Thiazoles / pharmacology*
Triazoles / chemistry
Triazoles / metabolism
Triazoles / pharmacology*

Substances

Anti-HIV Agents
Blood Proteins
Reverse Transcriptase Inhibitors
Thiazoles
Triazoles
2-phenyl-6-(2'-(4'-(ethoxycarbonyl)thiazolyl))thiazolo(3,2-b)(1,2,4)triazole