In this paper, we report on the synthesis of a novel series of 2-thiazolylhydrazone derivatives and the influence of the substituents on the thiazole ring on antifungal activity. All synthesized compounds were screened for their in vitro activities against 22 clinical isolates of Candida spp., representing six different species, compared to clotrimazole as a reference compound. Some of the tested compounds were found to possess significant antifungal activity when compared to clotrimazole, in particular compound 14 which exhibited higher potency against most of the Candida spp. considered. The compounds that were most active as anti-Candida agents were also Submitted to cytotoxic screening by the Trypan Blue dye exclusion assay and in general they were shown to induce low cytotoxic effects. (c) 2007 Elsevier Ltd. All rights reserved.
Synthesis and in vitro activity of 2-thiazolylhydrazone derivatives compared with the activity of clotrimazole against clinical isolates of Candida spp / Chimenti, Franco; Bizzarri, Bruna; Elias, Maccioni; Secci, Daniela; Bolasco, Adriana; Fioravanti, Rossella; Chimenti, Paola; Granese, Arianna; Carradori, Simone; Rivanera, Daniela; Lilli, Daniela; Zicari, Alessandra; Simona, Distinto. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - 17:16(2007), pp. 4635-4640. [10.1016/j.bmcl.2007.05.078]
Synthesis and in vitro activity of 2-thiazolylhydrazone derivatives compared with the activity of clotrimazole against clinical isolates of Candida spp.
CHIMENTI, Franco;BIZZARRI, Bruna;SECCI, DANIELA;BOLASCO, Adriana;FIORAVANTI, Rossella;CHIMENTI, Paola;GRANESE, ARIANNA;CARRADORI, Simone;RIVANERA, Daniela;LILLI, Daniela;ZICARI, Alessandra;
2007
Abstract
In this paper, we report on the synthesis of a novel series of 2-thiazolylhydrazone derivatives and the influence of the substituents on the thiazole ring on antifungal activity. All synthesized compounds were screened for their in vitro activities against 22 clinical isolates of Candida spp., representing six different species, compared to clotrimazole as a reference compound. Some of the tested compounds were found to possess significant antifungal activity when compared to clotrimazole, in particular compound 14 which exhibited higher potency against most of the Candida spp. considered. The compounds that were most active as anti-Candida agents were also Submitted to cytotoxic screening by the Trypan Blue dye exclusion assay and in general they were shown to induce low cytotoxic effects. (c) 2007 Elsevier Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
