Design, synthesis, and structure-activity relationship studies of novel tetrazole antifungal agents with potent activity, broad antifungal spectrum and high selectivity

doi:10.1016/j.bmcl.2017.12.040

	Design, synthesis, and structure-activity relationship studies of novel tetrazole antifungal agents with potent activity, broad antifungal spectrum and high selectivity
	Qian, Anran 3,4; Zheng, Yazhou 5; Wang, Ruilian 1; Wei, Jianhai 2; Cui, Yongmei 5; Cao, Xufeng 3,4; Yang, Yushe3,4
刊名	BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
	2018-02-01
卷号	28 期号:3 页码:344-350
关键词	Triazoles Antifungal activity Drug-drug interactions Tetrazole CYP3A4
ISSN号	0960-894X
DOI	10.1016/j.bmcl.2017.12.040
文献子类	Article
英文摘要	In this letter, we report our efforts to design, synthesize and evaluate biological activities of a series of novel hybridized compounds containing 1-tetrazole and 4-pyridinyl-1,2,4-triazole-3-one. An analysis of structure-activity data indicates that the target compounds with bulky and hydrophobic side chains exhibited stronger activities against the Candida spp and Cryptococcus neoformans tested than those of fluconazole and racemic VT-1161. Furthermore, 13k and 13ad were active against Microsporum gypseum, which was resistant to racemic VT-1161. In addition, 13k, 13ac and 13ad, with good in vitro activities against all of pathogenic fungi tested except for Aspergillus fumigatus, had no inhibition of human CYP3A4, suggesting a low risk of drug-drug interactions. (C) 2017 Elsevier Ltd. All rights reserved.
资助项目	National Natural Science Foundation of China[21402223]
WOS关键词	INVASIVE FUNGAL-INFECTIONS ; HYBRIDS ; MANAGEMENT ; INHIBITORS ; TRIAZOLE ; CYP51
WOS研究方向	Pharmacology & Pharmacy ; Chemistry
语种	英语
出版者	PERGAMON-ELSEVIER SCIENCE LTD
WOS记录号	WOS:000424285600022
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279931]
专题	药物化学研究室中科院受体结构与功能重点实验室新药研究国家重点实验室
通讯作者	Yang, Yushe
作者单位	1.Second Mil Med Univ, Sch Pharm, 325 Guohe Rd, Shanghai 200433, Peoples R China; 2.East China Normal Univ, Sch Chem & Mol Engn, Shanghai Engn Res Ctr Mol Therapeut & New Drug De, North Zhongshan Rd 3663, Shanghai, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China; 4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China; 5.Shanghai Univ, Coll Sci, Dept Chem, Shanghai 200444, Peoples R China;
推荐引用方式 GB/T 7714	Qian, Anran,Zheng, Yazhou,Wang, Ruilian,et al. Design, synthesis, and structure-activity relationship studies of novel tetrazole antifungal agents with potent activity, broad antifungal spectrum and high selectivity[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2018,28(3):344-350.
APA	Qian, Anran.,Zheng, Yazhou.,Wang, Ruilian.,Wei, Jianhai.,Cui, Yongmei.,...&Yang, Yushe.(2018).Design, synthesis, and structure-activity relationship studies of novel tetrazole antifungal agents with potent activity, broad antifungal spectrum and high selectivity.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,28(3),344-350.
MLA	Qian, Anran,et al."Design, synthesis, and structure-activity relationship studies of novel tetrazole antifungal agents with potent activity, broad antifungal spectrum and high selectivity".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 28.3(2018):344-350.