Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
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.
Gouveia
Frederico L
FL
Departamento de Ciências Farmacêuticas, Universidade Federal de Pernambuco, Recife 50670-901, Brazil.
de Oliveira
Renata M B
RM
de Oliveira
Tatiane B
TB
da Silva
Ivanildo M
IM
do Nascimento
Silene C
SC
de Sena
Kêsia X F R
KX
de Albuquerque
Julianna F C
JF
D000890:Anti-Infective Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D018432:Drug Resistance, Multiple; D004354:Drug Screening Assays, Antitumor; D006094:Gram-Positive Bacteria / Q000187:drug effects; D006801:Humans; D007659:Ketones; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000494:pharmacology
D000890:Anti-Infective Agents; D000970:Antineoplastic Agents; D007659:Ketones; D053778:Thiazolidines