| Synthesis, anti-HIV and antitubercular activities of isatin derivatives. | |
| | |
MedLine Citation:
|
PMID: 16649536 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
|
HIV is the most significant risk factor for many opportunistic infections like tuberculosis. In this study, we designed an isatinimino lead compound as a novel non-nucleoside reverse transcriptase inhibitor with antimycobacterial properties for the effective treatment of AIDS and AIDS-related tuberculosis. Among the compounds sythesized, 1-cyclopropyl-6-fluoro-8-methoxy-1,4-dihydro-4-oxo-7[[N4-[3'-[(4,6-dimethylpyrimidin-2-yl)benzenesulfonamido-4-yl]imino-1'-(5-fluoroisatinyl)]methyl]-3-methyl N1-piperazinyl]-3-quinoline carboxylic acid (9) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV (EC50: 12.1 microg/ml), and Mycobacterium tuberculosis (MIC: 1.22 microg/ml). |
| | |
Authors:
|
D Sriram; P Yogeeswari; K Meena |
Related Documents
:
|
22163386 - A bankruptcy problem approach to load-shedding in multiagent-based microgrid operation. 12125816 - Bacterial bioinformatics: pathogenesis and the genome. 17300556 - Development of ethnic disparities in internalizing and externalizing problems from adol... 890116 - The goldenhar syndrome: a natural history. 17054746 - Community response to intermittent preventive treatment delivered to infants (ipti) thr... 12636216 - Cytokine manipulation of the wound. |
Publication Detail:
|
Type: Journal Article |
Journal Detail:
|
Title: Die Pharmazie Volume: 61 ISSN: 0031-7144 ISO Abbreviation: Pharmazie Publication Date: 2006 Apr |
Date Detail:
|
Created Date: 2006-05-02 Completed Date: 2006-05-30 Revised Date: 2007-11-15 |
Medline Journal Info:
|
Nlm Unique ID: 9800766 Medline TA: Pharmazie Country: Germany |
Other Details:
|
Languages: eng Pagination: 274-7 Citation Subset: IM |
Affiliation:
|
Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, Pilani 333031, India. dsriram@bits-pilani.ac.in |
Export Citation:
|
APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
|
Anti-HIV Agents
/
chemical synthesis*,
pharmacology* Antitubercular Agents / chemical synthesis*, pharmacology* Cell Line HIV Reverse Transcriptase / metabolism HIV-1 / metabolism Humans Isatin / analogs & derivatives*, chemical synthesis, pharmacology* Mannich Bases Mycobacterium tuberculosis / drug effects, growth & development Reverse Transcriptase Inhibitors / pharmacology Stereoisomerism Structure-Activity Relationship Virus Replication / drug effects |
| Chemical | |
Reg. No./Substance:
|
0/Anti-HIV Agents; 0/Antitubercular Agents; 0/Mannich Bases; 0/Reverse Transcriptase Inhibitors; 91-56-5/Isatin; EC 2.7.7.49/HIV Reverse Transcriptase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
Previous Document: New tacrine-hydrazinonicotinamide hybrids as acetylcholinesterase inhibitors of potential interest f...
Next Document: Thieno[3,2-c]quinoline-4-yl-amines--synthesis and investigation of activity against malaria