Design, synthesis and antifungal activities in vitro of novel tetralin compounds

Autor:	Can Hui Zheng, Hui Tang, Ju Zhu, Jia Guo Lv, Jun Chen, You Jun Zhou, Yao Wu Li
Rok vydání:	2008
Předmět:	chemistry.chemical_classification Antifungal biology Stereochemistry medicine.drug_class Active site General Chemistry biology.organism_classification In vitro Amino acid chemistry.chemical_compound chemistry biology.protein medicine Tetralin Candida albicans Lead compound Heme
Zdroj:	Chinese Chemical Letters. 19:264-268
ISSN:	1001-8417
Popis:	Novel chiral tetralin compounds were designed and synthesized, and their antifungal activities in vitro were tested. The results showed that all of target compounds had potent antifungal activities, and were stronger than that of control compounds tetrahydroisoquinolines. The binding model of lead molecules in the active site of CYP51 of Candida albicans showed that lead compound specifically interacted with the amino acids residues in the active site, without binding with the heme of CYP51, which was different from azole antifungal drugs. The present study might afford a novel lead molecule to develop non-azole CYP51 inhibitors of fungi.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::dec67cc8c4e2bca10f928680fc83dbe0 https://doi.org/10.1016/j.cclet.2007.12.031 Zobrazit plný text záznamu Full Text from ScienceDirect