Synthesis and in vitro activity of 2-thiazolylhydrazone derivatives compared with the activity of clotrimazole against clinical isolates of Candida spp.
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.
Chimenti
Franco
F
Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive Università degli Studi di Roma La Sapienza, P.le A. Moro 5, 00185 Rome, Italy.
Bizzarri
Bruna
B
Maccioni
Elias
E
Secci
Daniela
D
Bolasco
Adriana
A
Fioravanti
Rossella
R
Chimenti
Paola
P
Granese
Arianna
A
Carradori
Simone
S
Rivanera
Daniela
D
Lilli
Daniela
D
Zicari
Alessandra
A
Distinto
Simona
S
D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology; D002175:Candida / Q000187:drug effects*; D003022:Clotrimazole / Q000737:chemistry* / Q000494:pharmacology*; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology*; D015394:Molecular Structure; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D006835:Hydrazones; D003022:Clotrimazole