Research article summary (published 30 Jan 2009):

N-benzylsalicylthioamides: highly active potential antituberculotics.

Full Abstract

A gseries of 29 new derivatives of N-benzylsalicylthioamides was synthesized and the compounds were tested for in-vitro antimycobacterial activity against Mycobacterium tuberculosis, Mycobacterium kansasii, and Mycobacterium avium. The activity was analyzed by quantitative structure-activity relationship (QSAR). Activity increased with increasing lipophilicity and electron donating effect of the substituents in the acyl moiety and decreased with the electrophilic superdelocalizability of the molecules. The most active compounds are more active than isoniazid (INH) and are active against INH-resistant potential pathogenic strains of mycobacterium.

Author information

Author/s: Dolezal, Rafael (R); Waisser, Karel (K); Petrlíková, Eva (E); Kunes, Jirí (J); Kubicová, Lenka (L); Machácek, Milos (M); Kaustová, Jarmila (J); Dahse, Hans Martin (HM);

Affiliation: Department of Inorganic and Organic Chemistry, Faculty of Pharmacy in Hradec Králové, Charles University in Prague, Hradec Králové, Czech Republic.

Journal and publication information

Publication Type: Journal Article; Research Support, Non-U.S. Gov't

Journal: Archiv der Pharmazie (Arch Pharm (Weinheim)), published in Germany. (Language: eng)

Reference: 2009-Feb; vol 342 (issue 2) : pp 113-9

Dates: Created 2009/02/12; Completed 2009/04/20; Revised 2009/05/20;

PMID: 19137534, status: MEDLINE (last retrieved date: 5/20/2009)

Sourced from the National Library of Medicine. Abstract text and other information may be subject to copyright.

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MeSH headings (categories)

This article was linked to the MeSH Headings (categories) shown below.

Antitubercular Agents - chemical synthesis; chemistry; pharmacology; toxicity Cell Line Cell Proliferation - drug effects Cell Survival Dose-Response Relationship, Drug Humans Microbial Sensitivity Tests

Molecular Structure Mycobacterium - drug effects Mycobacterium avium - drug effects Mycobacterium kansasii - drug effects Mycobacterium tuberculosis - drug effects Structure-Activity Relationship Thioamides - chemical synthesis; chemistry; pharmacology; toxicity

Note: Bold headings indicate primary MeSH headings or qualifiers.

Associated Chemicals: Antitubercular Agents (0) ; Thioamides (0)

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