Nevirapine derivatives with broad-spectrum chemotherapeutic properties for the effective treatment of HIV/AIDS.

Abstract

A series of nevirapine derivatives has been synthesized in an effort to enhance the spectrum of chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections. The nevirapine derivative bearing isoniazid moiety (3a) was found to be the most potent compound with EC50 of<0.0636 microM, CC50 of>1000 microM and selectivity index of>15,723 which also exhibited 90% inhibition against Mycobacterium tuberculosis at 6.25 microg/ml. Compound 3c showed 100% inhibition against M. tuberculosis and also exhibited potent antibacterial activity against 24 pathogenic bacteria with MIC less than 1 microg/ml.

• Authors: Dharmarajan Sriram, Narasimharaghavan Srichakravarthy, Tanushree R Bal, Perumal Yogeeswari
• Journal: Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie (Biomed Pharmacother) Vol. 59 Issue 8 Pg. 456-9 (Sep 2005) ISSN: 0753-3322 [Print] France
• PMID: 16140495 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Anti-Bacterial Agents
• Anti-HIV Agents
• Nevirapine
• Isoniazid

Topics

• AIDS-Related Opportunistic Infections (prevention & control)
• Anti-Bacterial Agents (chemical synthesis, pharmacology)
• Anti-HIV Agents (chemical synthesis, pharmacology)
• Cell Line
• Cell Survival (drug effects)
• Dose-Response Relationship, Drug
• HIV-1 (drug effects, physiology)
• Humans
• Isoniazid (analogs & derivatives, chemical synthesis, pharmacology)
• Microbial Sensitivity Tests
• Mycobacterium tuberculosis (drug effects)
• Nevirapine (analogs & derivatives, chemical synthesis, pharmacology)
• Structure-Activity Relationship
• Virus Replication (drug effects)