Preclinical Studies on Aryl Phosphate Derivatives of Bromo-Methoxy Zidovudine (Compounds WHI-05 and WHI-07): Novel Contraceptives with Anti-HIV Activity

Abstract

Objectives: Aryl phosphate derivatives of bromo-methoxy zidovudine are a new class of potent anti-HIV agents with selective spermicidal activity. We investigated the in vivo contraceptive efficacy and safety of two lead compounds, WHI-05 [5-bromo-6-methoxy-5,6-dihydro-3′-azidothymidine-5′-(p-methoxyphenyl) methoxyalaninyl phosphate], and WHI-07 [5-bromo-6-methoxy-5,6-dihydro-3′-azidothymidine-5′-(p-bromophenyl) methoxyalaninyl phosphate] in a lipophilic gel-microemulsion formulation.