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.
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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)
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Chemical References |
- Anti-Bacterial Agents
- Anti-HIV Agents
- Nevirapine
- Isoniazid
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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)
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