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 shu

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

Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China

Received Date: 13 September 2007

Fund Project: We thank Professor YongBin Cao of The Second Military Medical University for determining in vitro antifungal activities. This work was supported by the National Natural Science Foundation of China (No. 30572257).

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.
- Antifungal,
- Chiral tetralins,
- Lanosterol 14α-demethylase,
- Design,
- Synthesis
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