| Aminopyrimidinimino isatin analogues: design and synthesis of novel non- nucleoside HIV-1 reverse transcriptase inhibitors with broad-spectrum anti-microbial properties. | |
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MedLine Citation:
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PMID: 16787323 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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HIV is the most significant risk factor for many opportunistic infections like tuberculosis, bacterial infections etc. In this paper, we designed aminopyrimidinimino isatin lead compound as a novel non-nucleoside reverse transcriptase inhibitor with broad-spectrum chemotherapeutic properties for the effective treatment of AIDS and AIDS-related opportunistic infections. Compound 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7[[N(4)-[3'-(4'-amino-5'-chloroben-zylpyrimidin-2'-yl)imino-1'-(5-methylisatinyl)] methyl]N(1)-piperazinyl]-3-quinoline carboxylic acid (10) emerged as the most potent broad-spectrum chemotherapeutic agent active against HIV-1 replication (EC(50): 9.4 microg /ml), M. tuberculosis (MIC: 3.13 microg /ml) and various pathogenic bacteria (MIC's: 1.22 microg /ml). |
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Authors:
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Dharmarajan Sriram; Tanushree Ratan Bal; Perumal Yogeeswari |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't |
Journal Detail:
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Title: Medicinal chemistry (Shāriqah (United Arab Emirates)) Volume: 1 ISSN: 1573-4064 ISO Abbreviation: - Publication Date: 2005 May |
Date Detail:
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Created Date: 2006-06-21 Completed Date: 2006-08-28 Revised Date: 2008-02-26 |
Medline Journal Info:
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Nlm Unique ID: 101240303 Medline TA: Med Chem Country: United Arab Emirates |
Other Details:
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Languages: eng Pagination: 277-85 Citation Subset: IM |
Affiliation:
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Medicinal Chemistry Research Laboratory, Pharmacy group, Birla Institute of Technology and Science, Pilani, 333031, India. dsriram@bits-pilani.ac.in |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Anti-Infective Agents
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chemical synthesis,
chemistry*,
pharmacology Bacteria / drug effects Cells, Cultured Drug Design* HIV Reverse Transcriptase / antagonists & inhibitors* HIV-1 / drug effects, enzymology Humans Imines / chemistry Indoles / chemical synthesis, chemistry*, pharmacology Isatin / chemistry Lead / chemistry Mycobacterium tuberculosis / drug effects Pyrimidines / chemistry Quinolines / chemical synthesis, chemistry*, pharmacology Reverse Transcriptase Inhibitors / chemical synthesis, chemistry*, pharmacology Virus Replication / drug effects |
| Chemical | |
Reg. No./Substance:
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0/1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-((N4-(3'-(4'-amino-5'-chlorobenzylpyrimidin-2'-yl)imino-1'-(5-methylisatinyl))methyl)-N1-piperazinyl)-3-quinolinecarboxylic acid; 0/Anti-Infective Agents; 0/Imines; 0/Indoles; 0/Pyrimidines; 0/Quinolines; 0/Reverse Transcriptase Inhibitors; 7439-92-1/Lead; 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
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