In 2016,Li, Qing; Han, Li; Zhang, Bin; Zhou, Jinpei; Zhang, Huibin published 《Synthesis and biological evaluation of triazole based uracil derivatives as novel DPP-4 inhibitors》.Organic & Biomolecular Chemistry published the findings.COA of Formula: C4H7BrO2 The information in the text is summarized as follows:
A series of triazole based uracil derivatives I (R1 = H, 2-F, 2-Me-5-Cl, 4-OMe, etc.) and II [R2 = 2-EtO2CC6H4, 3-HO2CC6H4, CH2CO2H, CH2CO2Et, CH(CH3)CO2H, etc.] were designed and synthesized as novel DPP-4 inhibitors. Compound I (R1 = H) was identified as a lead compound for SAR studies focused on the structural modification at the S2′ subsite of DPP-4. The novel analogs I (R1 = 2-F, 3-F, 4-F, 2,4-F2) were obtained by modifying the substituents at the Ph group and compounds II by introducing the carbonyl group. On screening in DPP-4, compounds II [R2 = (CH2)2CO2H, (CH2)2CO2Me, CH2CH:CHCO2H] showed a significant improvement in DPP-4 inhibitory activities compared to compound I (R1 = H) and showed comparable activities to the marketed DPP-4 inhibitor, alogliptin. Docking studies revealed new favorable binding modes of designed compounds in the S2′ subsite and proved that structural modifications in the S2′ subsite were an effective option to increase the inhibition of DPP-4. In vitro DPP-8 and DPP-9 tests indicated that all compounds showed excellent selectivity against DPP-8 and DPP-9. Further in vivo evaluation showed that compound II [R2 = (CH2)2CO2Me] could significantly improve oral glucose tolerance in ICR mice and dose-dependently reduced glucose levels in type 2 diabetic C57BL/6 mice. These data suggest that compound II (R2 = (CH2)2CO2Me) could be a promising DPP-4 inhibitor for future treatment of T2DM. The experimental part of the paper was very detailed, including the reaction process of Methyl 3-bromopropanoate(cas: 3395-91-3COA of Formula: C4H7BrO2)
Methyl 3-bromopropanoate(cas: 3395-91-3) 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.COA of Formula: C4H7BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary