53202-58-7Relevant academic research and scientific papers
Solvent-induced selectivity of Williamson etherification in the pursuit of amides resistant against oxidative degradation
Clark, John A.,Derr, James B.,Espinoza, Eli M.,Morales, Maryann,Vadhin, Sandra,Vullev, Valentine I.
, p. 24419 - 24424 (2020/07/13)
This article reports two discoveries. (1) 2-Methoxyethanol induces unprecedented selectivity for etherification of 5-hydroxy-2-nitrobenzic acids without forming undesired esters. (2) Such compounds are precursors for amides showing unusual robustness agai
Discovery of a new class of ghrelin receptor antagonists
Mihalic, Jeffrey T.,Kim, Yong-Jae,Lizarzaburu, Mike,Deignan, Jeff,Wanska, Malgorzata,Yu, Ming,Fu, Jiasheng,Chen, Xi,Zhang, Alex,Connors, Richard,Liang, Lingming,Lindstrom, Michelle,Ma, Ji,Tang, Liang,Dai, Kang,Li, Leping,Chen, Xiaoqi
scheme or table, p. 2046 - 2051 (2012/04/17)
A series of benzodiazepine antagonists of the human ghrelin receptor GHSR1a were synthesized and their antagonism and metabolic stability were evaluated. The potency of these analogs was determined using a functional aequorin (Euroscreen) luminescent assay measuring the intracellular Ca2+ concentration, and their metabolic stability was measured using an in vitro rat and human S9 hepatocyte assay. These efforts led to the discovery of a potent ghrelin antagonist with good rat pharmacokinetic properties.
BENZODIAZEPINE AND BENZOPIPERAZINE ANALOG INHIBITORS OF HISTONE DEACETYLASE
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Page/Page column 94, (2010/11/26)
This invention relates to compounds for the inhibition of histone deacetylase More particularly, the invention provides for compounds of formula (I): wherein A, B, D, E, X1, X2, X3, X4 and n are as defined in the specification A method of inhibiting histone deacetylase in a cell, the method comprising contacting the cell with a compound of formula (I), in an amount sufficient to inhibit histone deacetylase, is also disclosed.
Anthranilic acid derivatives as inhibitors of 17beta-hydroxysteroid dehydrogenase 3
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Page/Page column 17-18, (2008/06/13)
Anthranilic acid drivatives, methods of using such compounds in the treatment of hormone sensitive diseases such as prostate cancer, and pharmaceutical compositions containing such compounds.
Synthesis and antinephritic activities of quinoline-3-carboxamides and related compounds
Tsuji, Kiyoshi,Spears, Glen W.,Nakamura, Katsuya,Tojo, Takashi,Seki, Nobuo,Sugiyama, Aiko,Matsuo, Masaaki
, p. 85 - 88 (2007/10/03)
A series of linomide-related quinoline-3-carboxamides and their analogues was prepared and evaluated for antinephritic activities. The 6-MeS derivative 7a was highly effective in two nephritis models, namely chronic graft-versus-host disease and autoimmune MRL/l mice.
