引用本文:
Hui Tang, You Jun Zhou, Yao Wu Li, Jia Guo Lv, Can Hui Zheng, Jun Chen, Ju Zhu. Design, synthesis and antifungal activities in vitro of novel tetralin compounds[J]. Chinese Chemical Letters,
2008, 19(3): 264-268.
doi:
10.1016/j.cclet.2007.12.031
Citation: Hui Tang, You Jun Zhou, Yao Wu Li, Jia Guo Lv, Can Hui Zheng, Jun Chen, Ju Zhu. Design, synthesis and antifungal activities in vitro of novel tetralin compounds[J]. Chinese Chemical Letters, 2008, 19(3): 264-268. doi: 10.1016/j.cclet.2007.12.031
Citation: Hui Tang, You Jun Zhou, Yao Wu Li, Jia Guo Lv, Can Hui Zheng, Jun Chen, Ju Zhu. Design, synthesis and antifungal activities in vitro of novel tetralin compounds[J]. Chinese Chemical Letters, 2008, 19(3): 264-268. doi: 10.1016/j.cclet.2007.12.031
Design, synthesis and antifungal activities in vitro of novel tetralin compounds
摘要:
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.
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关键词:
- Antifungal
- / Chiral tetralins
- / Lanosterol 14α-demethylase
- / Design
- / Synthesis
English
Design, synthesis and antifungal activities in vitro of novel tetralin compounds
Abstract:
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.
-
Key words:
- Antifungal
- / Chiral tetralins
- / Lanosterol 14α-demethylase
- / Design
- / Synthesis
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