20 Feb

Aryl Phosphate Derivatives of Bromo-Methoxy-Azidothymidine: DISCUSSION(1)


The development of a new class of aryl phosphate derivatives of bromo-methoxy-AZT as dual-function spermicides with potent anti-HIV activity was reported. CASA based on centroid-derived movement characteristics revealed that the observed spermicidal activity of these novel anti-HIV drugs and prodrugs of AZT was proportional to their effects on the track speed, path velocity, and straight-line velocity of sperm. The concentrations of the lead compound, WHI-07, required for 50% inhibition of HIV replication were 439-fold lower than that for the currently used detergent-based virucidal spermicide, N-9. The spermicidal activity of WHI-07 was 13.5-fold more potent than that of N-9 and was not mediated by membrane disruption. proventil inhaler

With the most potent AZT derivatives described herein, sperm motility loss was complete within 30 min. Results of our structure-activity relationship studies clearly establish that addition of the bromo-methoxy functional groups was essential for, and the aryl phosphate derivatization contributory to, the spermicidal activity of two classes of AZT derivatives. The SIA of AZT derivatives was irreversible. The potent spermicidal and anti-HIV activity of bromo-meth-oxy-substituted aryl phosphate derivatives of bromo-meth-oxy-AZT may provide the basis for the development of new and effective vaginal microbicides.

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