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Eur J Med Chem ; 44(5): 2038-43, 2009 May.
Article in English | MEDLINE | ID: mdl-19027993

ABSTRACT

Several 5-arylidene-4-thioxo-thiazolidine-2-ones (3a-n) were synthesized and evaluated as antimicrobial agents against representative strains, including multidrug-resistant strains of clinical isolates. Also, the antiproliferative activity was evaluated against two human carcinoma cell lines (NCI-H292 and HEp-2). The compounds containing the 5-arylidene subunit presented greater antimicrobial activities against Gram positive bacteria, including the multidrug-resistant clinical isolates, than the 4-thioxo-thiazolidine-2-one. Important SAR information was also gathered, such as the contribution of thiocarbonyl attached at 4-position on the thiazolidine heterocyclic for antimicrobial properties. None of the derivatives exhibited significant antiproliferative activity against the human carcinoma cell lines.


Subject(s)
Anti-Infective Agents/chemical synthesis , Thiazolidines/chemical synthesis , Anti-Infective Agents/pharmacology , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Cell Line, Tumor , Cell Proliferation/drug effects , Drug Resistance, Multiple , Drug Screening Assays, Antitumor , Gram-Positive Bacteria/drug effects , Humans , Ketones , Microbial Sensitivity Tests , Structure-Activity Relationship , Thiazolidines/pharmacology
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