876710-76-8Relevant articles and documents
Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents
Alasmary, Fatmah A.S.,Snelling, Anna M.,Zain, Mohammed E.,Alafeefy, Ahmed M.,Awaad, Amani S.,Karodia, Nazira
supporting information, p. 15206 - 15223 (2015/09/21)
A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the others are derivatives of one 2-(chloromethyl)-1Hbenzo[ d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications.
NITROGEN HETEROCYCLIC COMPOUNDS USEFUL AS PDE10 INHIBITORS
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Page/Page column 138, (2011/12/02)
Unsaturated nitrogen heterocyclic compounds of formula (I): (I), as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
CARBAMATE COMPOUND OR SALT THEREOF
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Page/Page column 14, (2011/08/08)
[Problems] A compound useful as an active ingredient for a pharmaceutical composition for treating FAAH-related diseases is provided. [Means for Solution] The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that a piperazine-1-carboxylate compound, in which benzimidazol-2-ylcarbonyl, benzofuran-2-ylcarbonyl or the like binds to the 4-position of the piperazine, has an excellent FAAH inhibitory activity and further has an action to increase the effective bladder capacity, an action to ameliorate sleep disorders, an anti-diuretic action, and an analgesic activity on lower urinary tract pain including bladder pain and the like, thereby completed the present invention. The carbamate compound of the present invention has an excellent FAAH inhibitory activity and can be used as an agent for preventing and/or treating FAAH-related diseases, particularly nocturia, interstitial cystitis, painful bladder syndrome, or chronic non-bacterial prostatitis/chronic pelvic pain syndrome.
