56934-77-1Relevant academic research and scientific papers
Design, synthesis, and biological activity evaluation of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives as broad-spectrum antifungal agents
Zhao, Liyu,Sun, Yin,Yin, Wenbo,Tian, Linfeng,Sun, Nannan,Zheng, Yang,Zhang, Chu,Zhao, Shizhen,Su, Xin,Zhao, Dongmei,Cheng, Maosheng
, (2021/11/22)
To discover antifungal compounds with broad-spectrum and stable metabolism, a series of 2-(benzo[b]thiophen-2-yl)-4-phenyl-4,5-dihydrooxazole derivatives was designed and synthesized. Compounds A30-A34 exhibited excellent broad-spectrum antifungal activity against Candida albicans with MIC values in the range of 0.03–0.5 μg/mL, and against Cryptococcus neoformans and Aspergillus fumigatus with MIC values in the range of 0.25–2 μg/mL. In addition, compounds A31 and A33 showed high metabolic stability in human liver microsomes in vitro, with the half-life of 80.5 min and 69.4 min, respectively. Moreover, compounds A31 and A33 showed weak or almost no inhibitory effect on the CYP3A4 and CYP2D6. The pharmacokinetic evaluation in SD rats showed that compound A31 had suitable pharmacokinetic properties and was worthy of further study.
PRODUCTION METHOD OF BENZOTHIAZOLE DERIVATIVE
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, (2020/06/18)
PROBLEM TO BE SOLVED: To provide: a production method of a benzothiazole derivative; as well as a production method of a polymerizable compound produced from the benzothiazole derivative; a polymerizable composition including the polymerizable compound; a polymer obtained by polymerizing the polymerizable composition; and an optical isomer utilizing the polymer. SOLUTION: A production method of a compound represented by the following general formula (III) is provided, and also a production method of a polymerizable compound produced from the compound represented by the general formula (III), a polymerizable composition, a polymer obtained by polymerizing the polymerizable composition, and an optical isomer utilizing the polymer are provided. When the polymerizable composition containing the compound is polymerized and the obtained film-like polymer is irradiated with ultraviolet light, change of color and change of phase difference scarcely take place. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT
MANUFACTURING INTERMEDIATE AND MANUFACTURING METHOD OF POLYMERIZABLE COMPOUND
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Paragraph 0172; 0174; 0189-0190, (2020/04/09)
PROBLEM TO BE SOLVED: To provide a manufacturing intermediate hardly generating discoloration and change of haze, when ultraviolet is radiated to a film-shaped polymer obtained by manufacturing a polymerizable compound and polymerizing a polymerizable composition containing the compound, and a manufacturing method of the manufacturing intermediate. SOLUTION: There are provided a compound represented by the formula (II), a manufacturing method of the compound, a polymerizable compound manufactured from the compound, a polymerizable composition, a polymer obtained by polymerizing the polymerizable composition, and an optical isomer using the polymer. In the formula, R1, R2 and L1 represent organic groups, n1 represents an integer of 1 to 4, when a plurality of L1 exist, it may be same or different, and neighboring L1 each other may form a condensed ring. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT
Acylaminoimidazole derivative and use thereof
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, (2016/10/07)
The invention belongs to the technical field of medicines and relates to an acylaminoimidazole derivative shown in the general formula I and its stereisomer and pharmaceutical acceptable salt, hydrate, solvate or prodrug. In the formula I, substituents R, R1, Ar, M and X are defined in the specification. The invention also relates to a method for preparing the compound shown in the formula I, a medicinal composition containing the compound and a use of the compound and the medicinal composition in preparation of drugs for treating and/or preventing cancers and other skin proliferative diseases. An antifungal experiment proves that the compound has strong resistance to shallow and deep fungi and can be used for preparation of an antibacterial drug.
Design, synthesis, and biological evaluation of amide imidazole derivatives as novel metabolic enzyme CYP26A1 inhibitors
Sun, Bin,Liu, Kai,Han, Jing,Zhao, Li-Yu,Su, Xiao,Lin, Bin,Zhao, Dong-Mei,Cheng, Mao-Sheng
, p. 6763 - 6773 (2015/10/20)
All-trans-retinoic acid (ATRA) as a physiological metabolite of vitamin A is widely applied in the treatment of cancer, skin, neurodegenerative and autoimmune diseases. CYP26A1 enzyme, induced by ATRA in liver and target tissues, metabolizes ATRA into 4-hydroxyl-RA. Inhibition of CYP26A1 metabolic enzyme represents a promising strategy for discovery of new specific anticancer agents. Herein, we describe the design, synthesis and biological evaluation of a series of new amide imidazole derivatives as retinoic acid metabolism blocking agents (RAMBAs) toward CYP26A1 enzyme. First, based on the recent theoretical models (Sun et al., J. Mol. Graph. Model., 2015, 56, 10-19) a series of RAMBAs with novel scaffolds were designed using fragment-based drug discovery approach. Subsequently, the new RAMBAs were synthesized and evaluated for their biological activities. All the compounds demonstrated appropriate enzyme activities and cell activities. The promising inhibitors 20 and 23 with IC50 value of 0.22 μM and 0.46 μM toward CYP26A1, respectively, were further evaluated for CYP selectivity and the metabolic profile of ATRA. Both compounds 20 and 23 showed higher selectivity for CYP26A1 over other CYPs (CYP2D6, CYP3A4) when compared to liarozole. They also showed better inhibitory activities for the metabolism of ATRA when also compared to liarozole. These studies further validated the pharmacophore and structure-activity relationship models obtained about CYP26A1 inhibitors and highlighted the promising activities of the new series of CYP26A1 inhibitors designed from such models. They also paved the way for future development of those candidates as potential drugs.
