85561-97-3Relevant academic research and scientific papers
5-SULFAMOYL-2-HYDROXYBENZAMIDE DERIVATIVES
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Page/Page column 159, (2017/09/27)
The invention is directed to substituted salicylamide derivatives. Specifically, the invention is directed to compounds according to Formula (I): wherein R, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof. The compounds of the invention are inhibitors of CD73 and can be useful in the treatment of cancer, pre-cancerous syndromes and diseases associated with CD73 inhibition, such as AIDS, the treatment of HIV, autoimmune diseases, infections, atherosclerosis, and ischemia–reperfusion injury. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CD73 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
2-aminobenzimidazole derivatives strongly inhibit and disperse Pseudomonas aeruginosa biofilms
Frei, Reto,Breitbach, Anthony S.,Blackwell, Helen E.
supporting information; experimental part, p. 5226 - 5229 (2012/07/03)
Bacterial biofilms are exceptionally difficult to clear using traditional antibiotics and constitute a significant health threat. 2-Aminobenzimidazole derivatives (see scheme) are capable of strongly inhibiting the growth of and dispersing Pseudomonas aeruginosa biofilms. These molecules were found to modulate quorum sensing in reporter strains, and represent some of strongest P. aeruginosa biofilm inhibitors known. Copyright
The design, synthesis and biological evaluation of 7-alkoxy-4-heteroarylamino-3-cyanoquinolines as dual inhibitors of c-Src and iNOS
Cao, Xin,You, Qi-Dong,Li, Zhi-Yu,Liu, Xiao-Rong,Xu, Dan,Guo, Qing-Long,Shang, Jing,Chern, Ji-Wang,Chen, Meng-Ling
scheme or table, p. 6206 - 6209 (2009/07/18)
Because both c-Src and iNOS are key regulatory enzymes in tumorigenesis, a new series of 4-heterocycle amine-3-quinolinecarbonitriles as potent dual inhibitors of both enzymes were designed, synthesized and evaluated as multiple targets agents in cancer therapy. All compounds were evaluated by two related enzyme inhibition assays and an anti-proliferation assay in vitro. The results showed that most compounds inhibited c-Src and iNOS well. The best compound 8 inhibited both enzymes with the IC50 values of 34.8 nM and 26.7 μM. Several compounds also showed moderate anti-proliferation at 10 μM against colon and liver cancer cell lines.
Novel benzimidazole-based MCH R1 antagonists
Carpenter, Andrew J.,Al-Barazanji, Kamal A.,Barvian, Kevin K.,Bishop, Michael J.,Britt, Christy S.,Cooper, Joel P.,Goetz, Aaron S.,Grizzle, Mary K.,Hertzog, Donald L.,Ignar, Diane M.,Morgan, Ronda O.,Peckham, Gregory E.,Speake, Jason D.,Swain, Will R.
, p. 4994 - 5000 (2007/10/03)
The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity.
Polyamide analogs
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, (2008/06/13)
This invention is directed to novel antibacterial/antifungal/antiparasitic agents of Formula (I): pharmaceutical compositions containing them, methods for their use and methods for preparing these compound
Method of inhibiting the advanced glycosylation of proteins using 1,2-disubstituted-benzimidazoles
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, (2008/06/13)
The present invention relates to compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, composition is disclosed which comprises 1,2-disubstituted benzimidazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
