《Discovery and Optimization of α-Mangostin Derivatives as Novel PDE4 Inhibitors for the Treatment of Vascular Dementia》 was written by Liang, Jinhao; Huang, Yi-You; Zhou, Qian; Gao, Yuqi; Li, Zhe; Wu, Deyan; Yu, Si; Guo, Lei; Chen, Zhen; Huang, Ling; Liang, Steven H.; He, Xixin; Wu, Ruibo; Luo, Hai-Bin. Category: bromides-buliding-blocks And the article was included in Journal of Medicinal Chemistry in 2020. The article conveys some information:
To validate PDE4 inhibitors as novel therapeutic agents against vascular dementia (VaD), 25 derivatives were discovered from the natural inhibitor α-mangostin (IC50 = 1.31μM). Hit-to-lead optimization identified a novel and selective PDE4 inhibitor 4e (IC50 = 17 nM), which adopted a different binding pattern from PDE4 inhibitors roflumilast and rolipram. Oral administration of 4e at a dose of 10 mg/kg exhibited remarkable therapeutic effects in a VaD model and did not cause emesis to beagle dogs, indicating its potential as a novel anti-VaD agent. In the experiment, the researchers used many compounds, for example, Ethyl 5-bromovalerate(cas: 14660-52-7Category: bromides-buliding-blocks)
Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Category: bromides-buliding-blocks
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary