| Design, synthesis, and evaluation of novel ethambutol analogues. | |
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MedLine Citation:
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PMID: 18242089 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Ethambutol is one of the front-line agents recommended by the World Health Organization for the treatment of tuberculosis. In an effort to develop more potent therapies to treat tuberculosis, novel unsymmetrical ethambutol analogues were successfully synthesized by a new route utilizing novel building blocks synthesized using Ellman's sulfinyl chemistry. The resulting analogues were tested for anti-tuberculosis activity yielding compounds with comparable anti-tuberculosis activity to ethambutol and increased lipophilicity that may instill better tissue penetration and serum half-life. |
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Authors:
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Raghunandan Yendapally; Richard E Lee |
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Publication Detail:
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Type: Journal Article; Research Support, N.I.H., Extramural Date: 2008-01-19 |
Journal Detail:
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Title: Bioorganic & medicinal chemistry letters Volume: 18 ISSN: 1464-3405 ISO Abbreviation: Bioorg. Med. Chem. Lett. Publication Date: 2008 Mar |
Date Detail:
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Created Date: 2008-03-10 Completed Date: 2008-05-19 Revised Date: 2010-09-29 |
Medline Journal Info:
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Nlm Unique ID: 9107377 Medline TA: Bioorg Med Chem Lett Country: England |
Other Details:
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Languages: eng Pagination: 1607-11 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutical Sciences, The University of Tennessee Health Science Center, 847 Monroe Ave Rm327, Memphis, TN 38163, USA. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Antitubercular Agents
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chemistry*,
pharmacology* Drug Design Ethambutol / analogs & derivatives*, chemistry*, pharmacology Microbial Sensitivity Tests Molecular Structure Mycobacterium tuberculosis / drug effects Structure-Activity Relationship |
| Grant Support | |
ID/Acronym/Agency:
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AI057836/AI/NIAID NIH HHS; P01 AI057836-010001/AI/NIAID NIH HHS |
| Chemical | |
Reg. No./Substance:
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0/Antitubercular Agents; 74-55-5/Ethambutol |
| Comments/Corrections | |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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