636581-61-8Relevant academic research and scientific papers
BENZIMIDAZOLES DERIVATIVES AS ANTI-TUBERCULOSIS AGENTS
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Page/Page column 10, (2020/10/09)
The present invention provides novel compounds of benzimidazole derivatives as anti-tubercular agents and their pharmaceutically acceptable salts for use as bactericidal therapeutics. The invention also provides a pharmaceutical composition comprising a c
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity
Manjunatha,Shandil, Radha,Panda, Manoranjan,Sadler, Claire,Ambady, Anisha,Panduga, Vijender,Kumar, Naveen,Mahadevaswamy, Jyothi,Sreenivasaiah,Narayan, Ashwini,Guptha, Supreeth,Sharma, Sreevalli,Sambandamurthy, Vasan K.,Ramachandran, Vasanthi,Mallya, Meenakshi,Cooper, Christopher,Mdluli, Khisi,Butler, Scott,Tommasi, Ruben,Iyer, Pravin S.,Narayanan, Shridhar,Chatterji, Monalisa,Shirude, Pravin S.
supporting information, p. 1480 - 1485 (2019/10/19)
We report a novel benzimidazole (BI) based DprE1 inhibitor that resulted from scaffold morphing of a 1,4-azaindole series. The clinical progression of the 1,4-azaindole series from our previous work validates the potential of exploring newer chemical enti
1, 4, 6-TRISUBSTITUTED-2-ALKYL-1H-BENZO[D]IMIDAZOLE DERIVATIVES AS DIHYDROOROTATE OXYGENASE INHIBITORS
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, (2018/09/19)
The present invention provides 1, 4, 6-trisubstituted-2-alkyl-1H-benzo[d]imidazole derivatives as dihydroorotate oxygenase inhibitor compounds of formula (I), which may be therapeutically useful as DHODH inhibitors, in which R1 to R3
COMPOUNDS FOR TREATMENT OF IMMUNE AND INFLAMMATORY DISORDERS
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Paragraph 0751, (2017/03/14)
Compounds, methods of use, and processes for making inhibitors of complement Factor D are provided comprising Formula I, I" and I'" or a pharmaceutically acceptable salt or composition thereof. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.
SUBSTITUTED QUINOXALINE DERIVATIVES
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Page/Page column 347; 348, (2016/12/01)
The present invention relates to substituted quinoxaline derivatives. These compounds are useful for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases.
DIHYDROOROTATE DEHYDROGENASE INHIBITORS
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Page/Page column 73, (2010/11/03)
The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: Intelligent design and evolution through the judicious use of structure-guided design and stucture-activity relationships
Charifson, Paul S.,Grillot, Anne-Laure,Grossman, Trudy H.,Parsons, Jonathan D.,Badia, Michael,Bellon, Steve,Deininger, David D.,Drumm, Joseph E.,Gross, Christian H.,LeTiran, Arnaud,Liao, Yusheng,Mani, Nagraj,Nicolau, David P.,Perola, Emanuele,Ronkin, Steven,Shannon, Dean,Swenson, Lora L.,Tang, Qing,Tessier, Pamela R.,Tian, Ski-Kai,Trudeau, Martin,Wang, Tiansheng,Wei, Yunyi,Zhang, Hong,Stamos, Dean
experimental part, p. 5243 - 5263 (2009/07/01)
The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA gyrase and topoisomerase IV are well-characterized clinically validated targets of the fluoroquinolone antibiotics which exert their antibacterial activity through inhibition of the catalytic subunits. Inhibition of these targets through interaction with their ATP sites has been less clinically successful. The discovery and characterization of a new class of low molecular weight, synthetic inhibitors of gyrase and topoisomerase IV that bind to the ATP sites are presented. The benzimidazole ureas are dual targeting inhibitors of both enzymes and possess potent antibacterial activity against a wide spectrum of relevant pathogens responsible for hospital- and community-acquired infections. The discovery and optimization of this novel class of antibacterials by the use of structure-guided design, modeling, and structure-activity relationships are described. Data are presented for enzyme inhibition, antibacterial activity, and in vivo efficacy by oral and intravenous administration in two rodent infection models.
ANTIBACTERIAL COMPOSITIONS
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, (2008/06/13)
Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1 ; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (-O-), thioether (-S-) or amino (-NR)- link, wherein R is hydrogen, -CN or C1-C3 alkyl; X is -C(=O)NR6-, -S(O)NR6-, -C(=O)O- or -S(=O)O- wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or -( C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
ORGANIC COMPOUNDS
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Page/Page column 27, (2008/06/13)
Compounds of formula (I) in free or salt form, where Y, R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the CXCR2 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
2-UREIDO-6-HETEROARYL-3H-BENZOIMIDAZOLE-4-CARBOXYLIC ACID DERIVATIVES AND RELATED COMPOUNDS AS GYRASE AND/OR TOPOISOMERASE IV INHIBITORS FOR THE TREATMENT OF BACTERIAL INFECTIONS
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Page 48, (2010/02/05)
The present invention relates to compounds of formula I, wherein X, Q, W, R1, R2 and R3 are as defined in the claims, which inhibit bacterial gyrase and/or Topo IV and pharmaceutically acceptable compositions comprising said compounds. These compounds, and compositions thereof, are useful in treating bacterial infection. Accordingly, the present invention also relates to methods for treating bacterial infections in, mammals. The present invention also relates to a method for preparing these compounds.
