A new series of [4-(4'-substituted-phenyl)thiazol-2-yl]hydrazine derivatives were synthesized in good yield (86-99%) and characterized by elemental analysis, IR, (1)H NMR, and mass spectral studies. The compounds were assayed for their in vitro broad-spectrum antifungal activity, compared to clotrimazole and fluconazole, against 20 clinical isolates of pathogenic Candida spp., representing five different species. The results showed that the presence of heterocyclic or bicyclic rings on hydrazone moiety in position C2 of thiazole revealed a promising selective inhibitory activity especially against Candida albicans and Candida glabrata. (C) 2010 Elsevier Masson SAS. All rights reserved,
Synthesis and biological evaluation of novel 2,4-disubstituted-1,3-thiazoles as anti-Candida spp. agents / Franco, Chimenti; Bizzarri, Bruna; Bolasco, Adriana; Secci, Daniela; Chimenti, Paola; Granese, Arianna; Simone, Carradori; Melissa, D'Ascenzio; Lilli, Daniela; Rivanera, Daniela. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 46:1(2011), pp. 378-382. [10.1016/j.ejmech.2010.10.027]
Synthesis and biological evaluation of novel 2,4-disubstituted-1,3-thiazoles as anti-Candida spp. agents
BIZZARRI, Bruna;BOLASCO, Adriana;SECCI, DANIELA;CHIMENTI, Paola;GRANESE, ARIANNA;LILLI, Daniela;RIVANERA, Daniela
2011
Abstract
A new series of [4-(4'-substituted-phenyl)thiazol-2-yl]hydrazine derivatives were synthesized in good yield (86-99%) and characterized by elemental analysis, IR, (1)H NMR, and mass spectral studies. The compounds were assayed for their in vitro broad-spectrum antifungal activity, compared to clotrimazole and fluconazole, against 20 clinical isolates of pathogenic Candida spp., representing five different species. The results showed that the presence of heterocyclic or bicyclic rings on hydrazone moiety in position C2 of thiazole revealed a promising selective inhibitory activity especially against Candida albicans and Candida glabrata. (C) 2010 Elsevier Masson SAS. All rights reserved,I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
