253192-29-9Relevant academic research and scientific papers
SUBSTITUTED N-(2-(AMINO)-2-OXOETHYL)BENZAMIDE INHIBITORS OF AUTOTAXIN AND THEIR PREPARATION AND USE IN THE TREATMENT OF LPA-DEPENDENT OR LPA-MEDIATED DISEASES
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, (2015/12/17)
The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancer, lymphocyte homing, chronic inflammation, neuropathic pain, fibrotic diseases, thrombosis, and cholestatic pruritus, mediated at least in part by ATX.
Structure-activity relationships of novel 2-substituted quinazoline antibacterial agents
Kung, Pei-Pei,Casper, Martin D.,Cook, Kimberley L.,Wilson-Lingardo, Laura,Risen, Lisa M.,Vickers, Timothy A.,Ranken, Ray,Blyn, Lawrence B.,Wyatt, Jacqueline R.,Cook, P. Dan,Ecker, David J.
, p. 4705 - 4713 (2007/10/03)
High-throughput screening of in-house compound libraries led to the discovery of a novel antibacterial agent, compound 1 (MIC: 12-25 μM against S. pyogenes). In an effort to improve the activity of this active compound, a series of 2-substituted quinazolines was synthesized and evaluated in several antibacterial assays. One such compound (22) displayed improved broad- spectrum antibacterial activity against a variety of bacterial strains. This molecule also inhibited transcription/translation of bacterial RNA, suggesting a mechanism for its antibiotic effects. Structure-activity relationship studies of 22 led to the synthesis of another 24 compounds. Although some of these molecules were found to be active in bacterial growth assays, none were as potent as 22. Compound 22 was tested for its ability to cure a systemic K. pneumonia infection in the mouse and displayed moderate effects compared with a control antibiotic, gentamycin.
