1918-78-1Relevant articles and documents
Synthesis and antimicrobial activity of some netropsin analogues
Khalaf, Abedawn I.,Ebrahimabadi, Abdolrasoul H.,Drummond, Allan J.,Anthony, Nahoum G.,Mackay, Simon P.,Suckling, Colin J.,Waigh, Roger D.
, p. 3119 - 3127 (2004)
Nine novel lexitropsins were synthesized by linking two netropsin-like moieties through three different dicarboxylic acids; 9, 10-dihydro-2, 7-phenanthrenedicarboxylic acid; [(3- {[(carboxymethyl)amino]carbonyl}benzoyl) amino]acetic acid and indole-2,5-di
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
supporting information, 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.
NOVEL THIOPHENECARBOXAMIDE DERIVATIVE AND PHARMACEUTICAL USE THEREOF
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Page/Page column 14, (2012/05/04)
The object of the present invention is to provide a compound having a glucokinase-activating effect. A pharmaceutical composition comprising a compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof as an active ingredient: wherein X means a nitrogen atom or CR6, wherein R6 means a hydrogen atom or a halogen atom; R1 means a hydrogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 alkylthio group; R2 means a hydrogen atom or a fluorine atom; R3 means a hydrogen atom or a C1-C6 alkyl group; and one of R4 and R5 means a hydrogen atom or a C1-C6 alkyl group, and the other means a C1-C6 alkylenecarboxylic acid, a C1-C6 alkylsulfonyl group, a C1-C6 alkylcarbonyl group, or CONH2.