In 2012,Tamura, Yuusuke; Omori, Naoki; Kouyama, Naoki; Nishiura, Yuji; Hayashi, Kyouhei; Watanabe, Kana; Tanaka, Yukari; Chiba, Takeshi; Yukioka, Hideo; Sato, Hiroki; Okuno, Takayuki published 《Design, synthesis and identification of novel benzimidazole derivatives as highly potent NPY Y5 receptor antagonists with attractive in vitro ADME profiles》.Bioorganic & Medicinal Chemistry Letters published the findings.Name: 3-Bromo-2-methylbenzoic acid The information in the text is summarized as follows:
Optimization of the HTS hit I, mainly focused on modification at the C-2 position of the benzimidazole core, is described. Elimination of the flexible and metabolically labile -S-CH2- part and utilization of less lipophilic pyridone substructure led to identification of novel NPY Y5 receptor antagonists II (R = n-Pr, t-Bu, CF3, F3CCH2), which have low to sub-nanomolar Y5 receptor binding affinity with improved CYP450 inhibition profiles, good solubilities and high metabolic stabilities. In the experiment, the researchers used many compounds, for example, 3-Bromo-2-methylbenzoic acid(cas: 76006-33-2Name: 3-Bromo-2-methylbenzoic acid)
3-Bromo-2-methylbenzoic acid(cas: 76006-33-2) 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. Name: 3-Bromo-2-methylbenzoic acid
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary