“SECOND GENERATION” OF TSAO COMPOUNDS DIRECTED AGAINST HIV-1 TSAO-RESISTANT STRAINS

Abstract

A “second generation” of TSAO molecules directed against TSAO-resistant strains have been prepared. The presence of two neighboring carbonyl groups at the 4″ position of the 3′-spiro moiety seems to be important for the anti-HIV-1 activity against both wild type and TSAO-resistant strains. NMR conformational studies in solution and theoretical calculations of the novel compounds have also been carried out.

ACKNOWLEDGMENT

We thank the Spanish CICYT (Project SAF2000-0153-C02-01), the Spanish Comunidad de Madrid (Project 08.2/0031.1/1999) and the European Commission (Project QLRT-1999-30291) for financial support. Esther Lobatón thanks Janssen-Cylag S.A. for an award to young researchers for the present work.