Application of 1129-28-8In 2016 ,《Discovery of Novel Indoline Cholesterol Ester Transfer Protein Inhibitors (CETP) through a Structure-Guided Approach》 appeared in ACS Medicinal Chemistry Letters. The author of the article were Wilson, Jonathan E.; Kurukulasuriya, Ravi; Reibarkh, Mikhail; Reiter, Maud; Zwicker, Aaron; Zhao, Kake; Zhang, Fengqi; Anand, Rajan; Colandrea, Vincent J.; Cumiskey, Anne-Marie; Crespo, Alejandro; Duffy, Ruth A.; Murphy, Beth Ann; Mitra, Kaushik; Johns, Douglas G.; Duffy, Joseph L.; Vachal, Petr. The article conveys some information:
Using the collective body of known (CETP) inhibitors as inspiration for design, a structurally novel series of tetrahydroquinoxaline CETP inhibitors were discovered. An exemplar from this series, compound I, displayed potent in vitro CETP inhibition and was efficacious in a transgenic cynomologus-CETP mouse HDL PD (pharmacodynamic) assay. However, an undesirable metabolic profile and chem. instability hampered further development of the series. A three-dimensional structure of tetrahydroquinoxaline inhibitor was proposed from 1H NMR structural studies, and this model was then used in silico for the design of a new class of compounds based upon an indoline scaffold. This work resulted in the discovery of compound II, which displayed potent in vitro CETP inhibition, a favorable PK-PD profile relative to tetrahydroquinoxaline I, and dose-dependent efficacy in the transgenic cynomologus-CETP mouse HDL PD assay. After reading the article, we found that the author used Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Application of 1129-28-8)
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products. Application of 1129-28-8
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary