- Important Hydrogen Bond Networks in Indoleamine 2,3-Dioxygenase 1 (IDO1) Inhibitor Design Revealed by Crystal Structures of Imidazoleisoindole Derivatives with IDO1
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Indoleamine 2,3-dioxygenase 1 (IDO1), promoting immune escape of tumors, is a therapeutic target for the cancer immunotherapy. A number of IDO1 inhibitors have been identified, but only limited structural biology studies of IDO1 inhibitors are available t
- Peng, Yi-Hui,Ueng, Shau-Hua,Tseng, Chen-Tso,Hung, Ming-Shiu,Song, Jen-Shin,Wu, Jian-Sung,Liao, Fang-Yu,Fan, Yu-Shiou,Wu, Mine-Hsine,Hsiao, Wen-Chi,Hsueh, Ching-Cheng,Lin, Shu-Yu,Cheng, Chia-Yi,Tu, Chih-Hsiang,Lee, Lung-Chun,Cheng, Ming-Fu,Shia, Kak-Shan,Shih, Chuan,Wu, Su-Ying
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Read Online
- Synthesis of 4,4'-biimidazoles
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The palladium(0) catalysed coupling reaction of 4-iodo-1-triphenylmethylimidazole (7) or its 2-methyl analogue 8 afforded the 4,4'-biimidazoles 9 and 10, respectively. Treatment of these compounds with 60% aqueous trifluoroacetic acid gave 4,4'-biimidazole and 2,2'-dimethyl-4,4'-biimidazole as their bistrifluoroacetate salts 11 and 12, respectively.
- Cliff,Pyne
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- Direct synthesis of pyrroles via a silver-promoted three-component reaction involving unusual imidazole ring opening
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A novel silver-promoted three-component reaction toward the synthesis of multifunctionalized pyrroles has been developed. This reaction involves an unusual imidazole ring decomposition, presumably via 1,5-isomerization and subsequent hydrolysis.
- Zeng, Jing,Bai, Yaguang,Cai, Shuting,Ma, Jimei,Liu, Xue-Wei
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supporting information; experimental part
p. 12855 - 12857
(2012/02/03)
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- Discovery of MK-5046, a potent, selective bombesin receptor subtype-3 agonist for the treatment of obesity
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We report the development and characterization of compound 22 (MK-5046), a potent, selective small molecule agonist of BRS-3 (bombesin receptor subtype-3). In pharmacological testing using diet-induced obese mice, compound 22 caused mechanism-based, dose-
- Sebhat, Iyassu K.,Franklin, Christopher,Lo, Michael M.-C.,Chen, David,Jewell, James P.,Miller, Randy,Pang, Jianmei,Palyha, Oksana,Kan, Yanqing,Kelly, Theresa M.,Guan, Xiao-Ming,Marsh, Donald J.,Kosinski, Jennifer A.,Metzger, Joseph M.,Lyons, Kathryn,Dragovic, Jasminka,Guzzo, Peter R.,Henderson, Alan J.,Reitman, Marc L.,Nargund, Ravi P.,Wyvratt, Matthew J.,Lin, Linus S.
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supporting information; experimental part
p. 43 - 47
(2011/04/17)
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- Substituted inmidazoles as bombesin receptor subtype-3 modulators
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Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.
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Page/Page column 27-28
(2010/02/17)
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