98436-74-9Relevant academic research and scientific papers
Mur ligases inhibitors with azastilbene scaffold: Expanding the structure–activity relationship
Hrast, Martina,Frlan, Rok,Knez, Damijan,Zdovc, Irena,Barreteau, Hélène,Gobec, Stanislav
supporting information, (2021/05/10)
Antibiotic resistance represents one of the biggest public health challenges in the last few years. Mur ligases (MurC–MurF) are involved in the synthesis of UDP-N-acetylmuramyl-pentapeptide, the main building block of bacterial peptidoglycan polymer. They are essential for the survival of bacteria and therefore important antibacterial targets. We report herein the synthesis and structure–activity relationships of Mur ligases inhibitors with an azastilbene scaffold. Several compounds showed promising inhibitory potencies against multiple ligases and one compound also possessed moderate antibacterial activity. These results represent a solid ground for further development and optimization of structurally novel antimicrobial agents to combat the rising bacterial resistance.
HETEROARYL OREXIN RECEPTOR ANTAGONISTS
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Page/Page column 37, (2016/07/05)
The present invention is directed to heteroaryl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
METABOTROPIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS OF USE THEREOF
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Page/Page column 80, (2013/02/27)
Compounds that modulate GluR5 activity and methods of using the same are disclosed.
2-CARBOXAMIDE-7-PIPERAZINYL-BENZOFURAN DERIVATIVES 774
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Page/Page column 25, (2011/01/05)
The present invention relates to compounds of formula (I), wherein R1 is heteroaryl or heterocyclyl, optionally substituted;R2 is C1-4alkyl, heterocyclyl, C1-4alkylaryl, C1-4alkylheteroaryl, carbocycl
