38239-45-1Relevant articles and documents
Design, synthesis, and structure-activity relationship studies of novel thienopyrrolidone derivatives with strong antifungal activity against Aspergillus fumigates
Cao, Xufeng,Xu, Yuanyuan,Cao, Yongbing,Wang, Ruilian,Zhou, Ran,Chu, Wenjing,Yang, Yushe
, p. 471 - 476 (2015/09/01)
In order to further enhance the anti-Aspergillus efficacy of our previously discovered antifungal lead compounds (I), two series of novel azoles featuring thieno[2,3-c]pyrrolidone and thieno[3,2-c]pyrrolidone nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using molecular docking, along with SARs of antifungal triazoles. Most of target compounds exhibited excellent activity against Candida and Cryptococcus spp., with MIC values in the range of 0.0625 μg/ml to 0.0156 μg/ml. The thieno[3,2-c]pyrrolidone unit was more suited for improving activity against Aspergillus spp. The most potent compound, 18a, was selected for further development due to its significant in vitro activity against Aspergillus spp. (MIC Combining double low line 0.25 μg/ml), as well as its high metabolic stability in human liver microsomes.
PYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
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Page/Page column 98; 99, (2010/04/28)
The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, Formula Ia, R4, R5, Formula Ib, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.
Novel thienopyridine compounds, and methods of use thereof
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Page/Page column 22, (2008/06/13)
The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).