Novel N-3 Substituted TSAO-T Derivatives: Synthesis and Anti-HIV-Evaluation.
Novel N-3 Substituted TSAO-T Derivatives: Synthesis and Anti-HIV-Evaluation.
Novel derivatives of the anti-HIV-1 agent, TSAO-T, bearing at the N-3 position alkylating groups or photoaffinity labels were prepared and evaluated for their anti-HIV activity. All of these compounds demonstrated pronounced anti-HIV-1 activity and inhibited HIV-1 RT; however, we were unable to detect stable covalent linkages between inhibitor and enzyme. In addition, compounds with an alcohol functional group connected to the N-3 position through a cis or trans double bond have been prepared. These compounds have been useful to study how the conformational restriction of the linker affects in the interaction between the N-3 substituent and the HIV-1 RT enzyme.
Bonache MC, Quesada E, Sheen CW, Balzarini J, Sluis-Cremer N, Pérez-Pérez MJ, Camarasa MJ, San-Félix A.
Instituto de QuÃmica Médica (C.S.I.C.), Madrid, Spain.