Synthesis and biological evaluation of novel 2,4-disubstituted-1,3-thiazoles as anti-Candida spp. agents

被引：94
作者：
Chimenti, Franco [1 ]
Bizzarri, Bruna [1 ]
Bolasco, Adriana [1 ]
Secci, Daniela [1 ]
Chimenti, Paola [1 ]
Granese, Arianna [1 ]
Carradori, Simone [1 ]
D'Ascenzio, Melissa [1 ]
Lilli, Daniela [2 ]
Rivanera, Daniela [2 ]
机构：
[1] Univ Roma La Sapienza, Dipartimento Chim & Tecnol Farm, I-00185 Rome, Italy
[2] Univ Roma La Sapienza, Dipartimento Sci Sanita Pubbl & Malattie Infett, I-00185 Rome, Italy
来源：
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2011年 / 46卷 / 01期
关键词：
Thiazole; Hydrazone; Candida spp; Hantzsch reaction; IN-VITRO ACTIVITY; MONOAMINE-OXIDASE; ANTIMICROBIAL ACTIVITY; CANDIDA SPP; DERIVATIVES; ANTIBACTERIAL; THIAZOLE; PATTERNS;
D O I：
10.1016/j.ejmech.2010.10.027
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
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, H-1 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,
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收藏
页码：378 / 382
页数：5
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