244126-64-5Relevant 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.
Enantioselective Synthesis of Five-Membered-Ring Atropisomers with a Chiral Rh(III) Complex
Shaaban, Saad,Li, Houhua,Otte, Felix,Strohmann, Carsten,Antonchick, Andrey P.,Waldmann, Herbert
supporting information, p. 9199 - 9202 (2020/11/30)
Axially chiral atropisomeric compounds are widely applied in asymmetric catalysis and medicinal chemistry, and efficient methods for their synthesis are in high demand. This applies in particular to atropisomers derived from five-membered aromatic rings because their lower barrier for rotation among the biaryl axis limits their asymmetric synthesis. We report here an enantioselective C-H functionalization method using our chiral RhJasCp complex for the synthesis of the biaryl atropisomer types that can be accessed from three different five-membered-ring heterocycles.
Benzo[b]thiophene-2-carboxamide derivatives as potent urotensin-II receptor antagonists
Lim, Chae Jo,Woo, Seong Eun,Ko, Su Ik,Lee, Byung Ho,Oh, Kwang-Seok,Yi, Kyu Yang
, p. 4684 - 4686 (2016/09/13)
Members of a series of benzo[b]thiophene-2-carboxamide derivatives, possessing an N-(1-(3-bromo-4-(piperidin-4-yloxy)benzyl)piperidin-4-yl) group, were synthesized and evaluated as urotensin-II receptor antagonists. The results show that these substances have potent UT binding affinities. Observations made in a systematic SAR investigation of the effects of a variety of substituents (R1and R2) at the 5- and 6-positions in the benzo[b]thiophene-2-carboxamide moiety on UT binding affinities led to identification of the 5-cyano analog 7f as a highly potent UT antagonist with an IC50value of 25?nM. Despite having a good metabolic stability, 7f is a potent inhibitor of CYP isozyme and displays an unsuitable PK profile.
METHOD FOR PROMOTING PLANT GROWTH
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Page/Page column 24, (2012/12/13)
Disclosed is a method for promoting the growth of a plant, comprising treating the plant with an effective amount of a compound represented by the following formula (1):, wherein any one of R1, R2, R3 and R4 represents a trifluoromethyl group, the others represent a hydrogen atom, and R5 represents a methyl group or an ethyl group.
METHOD FOR PROMOTING PLANT GROWTH
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Page/Page column 21-22, (2012/12/13)
Disclosed is a method for promoting the growth of a plant, comprising treating the plant with an effective amount of a compound represented by the following formula (1):, wherein any one of R1, R2, R3 and R4 represents a trifluoromethyl group, and the others represent a hydrogen atom, or an agriculturally acceptable salt thereof.
