Site-specific enzymatic activation of the anti-HIV agent stampidine

Arzneimittel-Forschung/Drug Research

Volumn 56, Issue 2 A, 2006, Pages 167-175

  Venkatachalam, Taracad K ^a,b   Qazi, Sanjive ^a,b   Uckun, Fatih M ^a,b,c  

^a PARKER HUGHES INSTITUTE   (United States)

^b Paradigm Pharmaceuticals   (United States)

^c Ikaros Enterprises   (United States)

Author keywords

Anti HIV agents; Antiretroviral therapy; CAS 217178 62 6; DDE 113; HI 113; N p (4 bromophenyl) 2',3' didehydro 3' deoxy 5' thymidylyl L alanine methyl ester; Stampidine, enzymatic activation

Indexed keywords

CAS 217178 62 6; DDE 113; ESTERASE; HI 113; PROTEINASE; RNA DIRECTED DNA POLYMERASE INHIBITOR; STAMPIDINE; TRIACYLGLYCEROL LIPASE; UNCLASSIFIED DRUG;

ARTICLE; DRUG ACTIVATION; DRUG HYDROLYSIS; DRUG METABOLISM; DRUG SYNTHESIS; ENZYME ACTIVATION; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN IMMUNODEFICIENCY VIRUS INFECTION;

EID: 33645100316     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1296804     Document Type: Article

References (6)

1. Uckun, F. M., Chen, C. L., Lisowski, E. et al., Toxicity and Pharmacokinetics of Stampidine in Mice and Rats. Arzneim.-Forsch./Drug Res. 53, 357 (2003)
2. Venkatachalam, T. K. Li, G, Samuel, P et al., Lipase-mediated Stereoselective Hydrolysis of Stampidine and Other Phosphoramidate Derivatives of Stavudine. Bioorg. Med. Chem. 12, 3371 (2004)
3. Venkatachalam, T. K., Samuel, P., Qazi, S. et al., Protease Mediated Enzymatic Hydrolysis and Activation of Aryl Phosphoramidate Derivatives of Stavudine. Eur. J. Med. Chem. 40, 452 (2005)
4. Venkatachalam, T. K., Samuel, P., Qazi, S. et al., Effects of change in nucleoside structure on the activation and antiviral of phosphoramidate derivatives. Bioorg. Med. Chem. 13, 5408 (2005)
5. Venkatachalam, T. K. Samuel, P., Uckun, F. M., Stereochemical influence on lipase-mediated hydrolysis and biological activity of Stampidine and other Stavudine phosphoramidates. Bioorg. Med. Chem. 13, 1763 (2005)
6. Venkatachalam, T. K., Li, G., Samuel, P. et al., A comparative study of the hydrolysis pathways of substituted aryl phosphoramidate versus aryl thiophosphoramidate derivatives of stavudine. Eur. J. Med. Chem. 39, 665 (2004)