- New analogues of N-(2-aminoethyl)-4-chlorobenzamide (Ro 16-6491). Some of the most potent monoamine oxidase-B inactivators
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A series of halo- and nitro-substituted analogues of N-(2- aminoethyl)benzamide has been synthesized. All of the compounds are competitive, time-dependent inhibitors of monoamine oxidase-B (MAO-B), but upon dialysis complete return of enzyme activity is observed for all compounds. Therefore, these are mechanism-based reversible inhibitors of MAO- B. The relative potencies of the compounds are rationalized in terms of steric and hydrophobic effects.
- Annan,Silverman
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- Discovery and optimization of adamantane carboxylic acid derivatives as potent diacylglycerol acyltransferase 1 inhibitors for the potential treatment of obesity and diabetes
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Abstract We have developed a series of adamantane carboxylic acid derivatives exhibiting potent diacylglycerol acyltransferase 1 (DGAT1) inhibitory activities. Optimization of the series led to the discovery of E-adamantane carboxylic acid compound 43c, which showed excellent in vitro activity with an IC50 value of 5 nM against human and mouse DGAT1, also good druggability as well as microsomal stability and safety profiles such as hERG, CYP and cytotoxicity. Compound 43c significantly reduced plasma triglyceride levels in vivo (in rodents and zebrafish) and also showed bodyweight gain reduction and glucose area under curve (AUC) lowering efficacy in diet-induced obesity (DIO) mice.
- Pagire, Suvarna H.,Pagire, Haushabhau S.,Lee, Gwi Bin,Han, Seo-Jung,Kwak, Hyun Jung,Kim, Ji Young,Kim, Ki Young,Rhee, Sang Dal,Ryu, Jeong Im,Song, Jin Sook,Bae, Myung Ae,Park, Mi-Jin,Kim, Dooseop,Lee, Duck Hyung,Ahn, Jin Hee
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p. 716 - 735
(2015/08/04)
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- BENZOIMIDAZOLE DERIVATIVES AND GLYCOGEN SYNTHASE KINASE-3 BETA INHIBITORS CONTAINING THE SAME
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Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.
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Page/Page column 81
(2010/04/03)
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- MTP INHIBITING TETRAHYDRO-NAPHTHALENE-1-CARBOXYLIC ACID DERIVATIVES
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The present invention is concerned with novel tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for preparing such compounds
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Page/Page column 25
(2008/12/05)
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- BENZAMIDE DERIVATIVES
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Benzamides of the formula I wherein R1 and R2 each independently is hydrogen, halogen, lower alkyl, lower alkoxy, cyano, trifluoromethyl, sulfamoyl, mono(lower alkyl)sulfamoyl or di(lower alkyl)sulfamoyl or R1 and R2 on adjacent carbon atoms together are
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