147021-86-1Relevant articles and documents
Novel cinnamic amides
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Page/Page column 10, (2008/06/13)
E-cinnamic amides of piperazine derivatives according to formula (I) wherein X is chloro or fluoro and R1 is an aromatic or heteroaromatic group, their pharmaceutically acceptable salts or solvates. The invention also relates to pharmaceutical
A novel series of highly potent benzimidazole-based microsomal triglyceride transfer protein inhibitors
Robl,Sulsky,Sun,Simpkins,Wang,Dickson Jr.,Chen,Magnin,Taunk,Slusarchyk,Biller,Lan,Connolly,Kunselman,Sabrah,Jamil,Gordon,Harrity,Wetterau
, p. 851 - 856 (2007/10/03)
A series of benzimidazole-based analogues of the potent MTP inhibitor BMS-201038 were discovered. Incorporation of an unsubstituted benzimidazole moiety in place of a piperidine group afforded potent inhibitors of MTP in vitro which were weakly active in vivo. Appropriate substitution on the benzimidazole ring, especially with small alkyl groups, led to dramatic increases in potency, both in a cellular assay of apoB secretion and especially in animal models of cholesterol lowering. The most potent in this series, 3g (BMS-212122), was significantly more potent than BMS-201038 in reducing plasma lipids (cholesterol, VLDL/LDL, TG) in both hamsters and cynomolgus monkeys.
Photoinduced Nitro-Nitrite Rearrangement of 5-Nitroquinoxalines
El'tsov,Selitrenikov,Rtishchev
, p. 285 - 294 (2007/10/03)
Unlike known o-nitro methyl derivatives of aromatic compounds, 6-methyl-5-nitro-, 2,3,6-trimethyl-5-nitro-, and 7-methyl-6-nitroquinoxaline and 1,6-dimethyl-5-nitroquinoxalinium perchlorate do not exhibit photochromism in aqueous-ethanolic solutions under conditions of flash photolysis with a time resolution of 50 μs. Under conditions of continuous photolysis, these 5-nitromethylquinoxaline derivatives and also 5-nitroquinoxaline undergo nitro-nitrite rearrangement to give 5-quinoxalinol derivatives with quantum yields ranging from 1 × 10-4 to 3 × 10-3; the efficiency of the photochemical reaction increases when irradiation is performed with a shorter-wave light. 6-Nitro derivatives do not form stable products of photochemical transformations under the same conditions.