RESUMEN

Four types of piscidinol A derivatives were synthesized and evaluated their ability to inhibit HIV-1 protease to understand their structure-activity relationships. Of these tirucallane-type triterpene derivatives, an A-seco derivative (1b) moderately inhibited human immunodeficiency virus (HIV) protease (IC50 38.2 µM). The 2,2-dimethyl succinic acid (DMS) acylated tirucallane derivatives (4b, 6a, and 7b, 50 < IC50 < 100 µM) were more inhibitory against HIV-1 PR than the others (PA, 2a, 4a, 4c-4d, 5a, 6b-6d, and 7a, IC50 > 100 µM). These findings indicated that the 2,3-seco-2,3-dioic acid (1b) and DMS-acylated tirucallane-type derivatives preferably inhibited HIV viral protease.

Asunto(s)

Fármacos Anti-VIH/síntesis química , Fármacos Anti-VIH/farmacología , Proteasa del VIH/efectos de los fármacos , VIH-1/efectos de los fármacos , Triterpenos/síntesis química , Triterpenos/farmacología , Fármacos Anti-VIH/química , VIH-1/enzimología , Humanos , Estructura Molecular , Relación Estructura-Actividad , Triterpenos/química