Stampidine: a selective oculo-genital microbicide.

Abstract	Adenoviruses (ADVs) are causative agents of severe and extremely contagious ocular and genital infections associated with conjunctivitis, genital ulcers and urethritis. Yet, no functional antiviral compounds are currently available against adenoviral infections. We discovered halogen-substituted phenyl phosphoramidate derivatives of stavudine (STV/d4T) as a new class of dual-function anti-human immunodeficiency virus (HIV) agents with potent and selective anti-ADV activity. The lead compound, stampidine [5'-(4-bromophenyl methoxyalaninylphosphate)-2',3'-didehydro-3'-deoxythymidine], was the most potent non-toxic dual-function antiviral agent. Stampidine displayed remarkable in vitro and in vivo anti-HIV activity against drug-sensitive and drug-resistant HIV strains. Stampidine was non-cytotoxic and nonirritating to mucosal epithelial cells. Several preclinical studies conducted thus far, suggest that stampidine has clinical potential as a dual-function topical agent for the prevention and/or effective treatment of oculo-genital ADV/HIV infections.
Authors	Osmond J D'Cruz, Fatih M Uckun
Journal	The Journal of antimicrobial chemotherapy (J Antimicrob Chemother) Vol. 56 Issue 1 Pg. 10-9 (Jul 2005) ISSN: 0305-7453 [Print] England
PMID	15919769 (Publication Type: Journal Article, Research Support, N.I.H., Extramural, Research Support, U.S. Gov't, P.H.S., Review)
Chemical References	Anti-HIV Agents Antiviral Agents Dideoxynucleotides Receptors, Virus adenovirus receptor stampidine Thymidine Monophosphate Stavudine
Topics	Adenoviridae (classification, drug effects) Animals Anti-HIV Agents (pharmacology) Antiviral Agents (pharmacology) Dideoxynucleotides Drug Stability Eye Infections, Viral (drug therapy) Genitalia (virology) Humans Receptors, Virus (analysis) Serotyping Solubility Stavudine (analogs & derivatives, pharmacology) Thymidine Monophosphate (analogs & derivatives, pharmacology) Urethritis (drug therapy)

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