《Discovery of triazole-based uracil derivatives bearing amide moieties as novel dipeptidyl peptidase-IV inhibitors》 was written by Deng, Xiaoyan; Han, Li; Zhou, Jinpei; Zhang, Huibin; Li, Qing. SDS of cas: 3395-91-3This research focused ontriazole amide uracil preparation dipeptidyl peptidase IV inhibitor antidiabetic; Amide; DPP-4 inhibitor; T2DM; Triazole; Uracil derivatives. The article conveys some information:
Dipeptidyl peptidase-IV (DPP-4) is a validated target for T2DM treatment. The authors previously reported a novel series of triazole-based uracil derivatives bearing aliphatic carboxylic acids with potent DPP-4 inhibitory activities in vitro, but these compounds showed poor hypoglycemic effects in vivo. Herein the authors further optimized the triazole moiety by amidation of the carboxylic acid to improve in vivo activities. Two series of compounds 3a-f and 4a-g were designed and synthesized. By screening in DPP-4, compound 4c ((R)-2-(4-((4-(3-aminopiperidin-1-yl)-3-(but-2-yn-1-yl)-2,6-dioxo-3,6-dihydropyrimidin-1(2H)-yl)methyl)-1H-1,2,3-triazol-1-yl)-N,N-dimethylacetamide hydrochloride) was identified as a potent DPP-4 inhibitor with the IC50 value of 28.62 nM. Docking study revealed compound 4c has a favorable binding mode and interpreted the SAR of these analogs. DPP-8 and DPP-9 tests indicated compound 4c had excellent selectivity over DPP-8 and DPP-9. Further in vivo evaluations revealed that compound 4c showed more potent hypoglycemic activity than its corresponding carboxylic acid in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice. The overall results have shown that compound 4c could be a promising lead for further development of novel DPP-4 agents treating T2DM. The experimental part of the paper was very detailed, including the reaction process of Methyl 3-bromopropanoate(cas: 3395-91-3SDS of cas: 3395-91-3)
Methyl 3-bromopropanoate(cas: 3395-91-3) belongs to bromides. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.SDS of cas: 3395-91-3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary