Document Detail


New AZT conjugates as potent anti-HIV agents.
MedLine Citation:
PMID:  16440984     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
In an attempt to discover anti-HIV agents with much reduced cytotoxicity from the currently available HIV-reverse transcriptase inhibitors, AZT conjugates of cholanic acids, 2-imidazolidone-4-carboxylic acid and its derivatives, and N,N'-disubstituted 5-hydroxy-tetrahydropyrimidin-2-ones have been synthesized and their anti-HIV profiles determined with CEM-SS cell line. The AZT conjugates with 2-imidazolidone-4-carboxylic acid and 2-pyrrolidone-5-carboxylic acid through an ester linkage, and with N,N'-diphenyl-5-hydroxy-tetrahydropyrimidin-2-one through a succinate tether showed significantly higher therapeutic indexes than AZT while they also retained or enhanced AZT's anti-HIV activity. Thus, structural features that favor the desired therapeutic profile of the conjugates appear to include a five-membered ring cyclic urea or lactam, and six-membered ring cyclic urea with N,N'-diphenyl substitution.
Authors:
Zhengqing You; Henry Young Lee
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural    
Journal Detail:
Title:  Nucleosides, nucleotides & nucleic acids     Volume:  25     ISSN:  1525-7770     ISO Abbreviation:  Nucleosides Nucleotides Nucleic Acids     Publication Date:  2006  
Date Detail:
Created Date:  2006-01-30     Completed Date:  2006-04-03     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  100892832     Medline TA:  Nucleosides Nucleotides Nucleic Acids     Country:  United States    
Other Details:
Languages:  eng     Pagination:  37-54     Citation Subset:  IM    
Affiliation:
College of Pharmacy and Pharmaceutical Sciences, Florida A & M University, Tallahassee, Florida, USA.
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MeSH Terms
Descriptor/Qualifier:
Anti-HIV Agents / chemistry*,  pharmacology*,  toxicity
Cell Line
Molecular Structure
Zidovudine / chemistry*
Grant Support
ID/Acronym/Agency:
AI 20360/AI/NIAID NIH HHS; AM 21627/AM/NIADDK NIH HHS; RR 02660/RR/NCRR NIH HHS; RR 08111/RR/NCRR NIH HHS
Chemical
Reg. No./Substance:
0/Anti-HIV Agents; 30516-87-1/Zidovudine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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