Academic Journal
Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives
العنوان: | Synthesis and antifungal activity of a new series of 2-(1H-imidazol-1-yl)-1-phenylethanol derivatives |
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المؤلفون: | DE VITA, DANIELA, SCIPIONE, Luigi, TORTORELLA, Silvano, MELLINI, PAOLO, DI RIENZO, Barbara, SIMONETTI, Giovanna, D'AURIA, Felicia Diodata, PANELLA, SIMONA, DI SANTO, Roberto, PALAMARA, ANNA TERESA, Roberto Cirilli |
المساهمون: | DE VITA, Daniela, Scipione, Luigi, Tortorella, Silvano, Mellini, Paolo, DI RIENZO, Barbara, Simonetti, Giovanna, D'Auria, Felicia Diodata, Panella, Simona, Roberto, Cirilli, DI SANTO, Roberto, Palamara, ANNA TERESA |
بيانات النشر: | ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER |
سنة النشر: | 2012 |
المجموعة: | Sapienza Università di Roma: CINECA IRIS |
مصطلحات موضوعية: | non-albicans candida specie, human monocytic cell line, enantiomers separation, antifungal imidazole, candida albicans species |
الوصف: | A new series of aromatic ester and carbamate derivatives of 2-(1H-imidazol-1-yl)-1-phenylethanol were synthesized and evaluated for their antifungal activity towards Candida albicans and non-albicans Candida species strains. The aromatic biphenyl ester derivatives 6a-c were more active than the reference compound fluconazole. 6c possesses a MIC mean values of 1.7 ± 1.4 μg mL -1 vs C. albicans and 1.9 ± 2.0 μg mL -1 vs non-albicans Candida species strains. The racemic mixtures of 6a, b were purified to afford the pure enantiomers. The (-) isomers were up to 500 times more active than (+) isomers. (-)-6a and (-)-6b were thirty and ninety times more active than fluconazole towards C. krusei strain respectively. The racemates of 6a-c showed low cytotoxicity against human monocytic cell line (U937) with 6a demonstrating a CC 50 greater than 128 μg mL -1. © 2012 Elsevier Masson SAS. All rights reserved. |
نوع الوثيقة: | article in journal/newspaper |
وصف الملف: | STAMPA |
اللغة: | English |
Relation: | info:eu-repo/semantics/altIdentifier/pmid/22321993; info:eu-repo/semantics/altIdentifier/wos/WOS:000302033300033; volume:49; firstpage:334; lastpage:342; numberofpages:9; journal:EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; http://hdl.handle.net/11573/434328; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-84857239066; http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=000302033300033&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=0c7ff228ccbaaa74236f48834a34396a; http://www.ncbi.nlm.nih.gov/pubmed/22321993; http://www.scopus.com/inward/record.url?eid=2-s2.0-84857239066&partnerID=65&md5=29fd080864bc4de3c238a1abd6c413f0 |
DOI: | 10.1016/j.ejmech.2012.01.034 |
الاتاحة: | http://hdl.handle.net/11573/434328 https://doi.org/10.1016/j.ejmech.2012.01.034 http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=000302033300033&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=0c7ff228ccbaaa74236f48834a34396a http://www.ncbi.nlm.nih.gov/pubmed/22321993 http://www.scopus.com/inward/record.url?eid=2-s2.0-84857239066&partnerID=65&md5=29fd080864bc4de3c238a1abd6c413f0 |
رقم الانضمام: | edsbas.F2F2DF77 |
قاعدة البيانات: | BASE |
DOI: | 10.1016/j.ejmech.2012.01.034 |
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