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更新于：2025-03-20

Tolciclate

托西拉酯

更新于：2025-03-20

概要

基本信息

药物类型

小分子化药

别名

Tolciclate (JAN/USAN/INN)

+ [2]

靶点

Ergosterol

作用方式-

作用机制

麦角固醇生物合成抑制剂

治疗领域

感染皮肤和肌肉骨骼疾病

在研适应症

传染性皮肤病

非在研适应症-

原研机构-

在研机构-

非在研机构-

最高研发阶段批准上市

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C20H21NOS

InChIKeyCANCCLAKQQHLNK-UHFFFAOYSA-N

CAS号50838-36-3

关联

100 项与托西拉酯相关的临床结果

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100 项与托西拉酯相关的转化医学

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100 项与托西拉酯相关的专利（医药）

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项与托西拉酯相关的文献（医药）

2020-03-31·Journal of Pure and Applied Microbiology

Topological Polar Surface Area, Molecular Weight, and Rotatable Bond Count Account for the Variations in the Inhibitory Potency of Antimycotics against Microsporum canis

作者: Villarante, Nelson R. ; Agapito, Josephine D. ; Gloriani, Nina G. ; Asaad, Abubakar S. ; Sumalapao, Derick Erl P.

Multivariate statistical models were utilized to identify the interaction between the inhibitory activity and the mol. properties of the different antimycotics against Microsporum canis.Information on the inhibitory potency against M. canis and mol. properties of antifungal agents were obtained from literature.The relationship between the inhibitory potency and the mol. properties of the different antimycotics against M. canis was established using multiple linear regression anal. (MLRA) and principal component anal. (PCA).Three major descriptors: topol. polar surface area, mol. weight, and rotatable bond count of the antimycotics were identified to confer inhibitory action against M. canis using MLRA (r2 = 0.8968, p<0.0001) and PCA (95.86% total contribution rate).Both MLRA and PCA as statistical approaches demonstrate their potential as tools in computational structure design and for possible synthesis of next generation antimycotics as more effective treatments of fungal infections.

2016-10-24·Angewandte Chemie International Edition1区 · 化学

Synthesis of Bridged Cyclopentane Derivatives by Catalytic Decarbonylative Cycloaddition of Cyclobutanones and Olefins

1区 · 化学

Article

作者: Zhou, Xuan ; Ko, Haye Min ; Dong, Guangbin

AbstractHerein, we report an intramolecular rhodium‐catalyzed decarbonylative coupling between cyclobutanones and alkenes that proceeds by C−C activation and provides a distinct approach to a diverse range of saturated bridged cyclopentane derivatives. In this reaction, cyclobutanones serve as cyclopropane surrogates, reacting in a formal (4+2−1) transformation. To demonstrate the efficacy of this method, it was applied in a concise synthesis of the antifungal drug Tolciclate.

2012-09-01·Current Drug Safety

QSAR Study for Carcinogenicity in a Large Set of Organic Compounds

Article

作者: Castro, Eduardo A. ; Comelli, Nieves C. ; Duchowicz, Pablo R. ; Ortiz, Erlinda V.

In our continuing efforts to find out acceptable Absorption, Distribution, Metabolization, Elimination and Toxicity (ADMET) properties of organic compounds, we establish linear QSAR models for the carcinogenic potential prediction of 1464 compounds taken from the "Galvez data set", that include many marketed drugs. More than a thousand of geometry-independent molecular descriptors are simultaneously analyzed, obtained with the softwares E-Dragon and Recon. The variable subset selection method employed is the Replacement Method, and also the improved version Enhanced Replacement Method. The established models are properly validated through an external test set of compounds, and by means of the Leave-Group-Out Cross Validation method. In addition, we apply the Y-Randomization strategy and analyze the Applicability Domain of the developed model. Finally, we compare the results obtained in present study with the previous ones from the literature. The novelty of present work relies on the development of an alternative predictive structure-carcinogenicity relationship in a large heterogeneous set of organic compounds, by only using a reduced number of geometry independent molecular descriptors.

100 项与托西拉酯相关的药物交易

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