Bai, Xiaohui published the artcileA new GLP-1 analogue with prolonged glucose-lowering activity in vivo via backbone-based modification at the N-terminus, Recommanded Product: (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, the publication is Bioorganic & Medicinal Chemistry (2016), 24(6), 1163-1170, database is CAplus and MEDLINE.
Glucagon-like peptide-1 (GLP-1) is an endogenous insulinotropic hormone with wonderful glucose-lowering activity. However, its clin. use in type II diabetes is limited due to its rapid degradation at the N-terminus by dipeptidyl peptidase IV (DPP-IV). Among the N-terminal modifications of GLP-1, backbone-based modification was rarely reported. Herein, the authors employed two backbone-based strategies to modify the N-terminus of tGLP-1. Firstly, the amide N-methylated analogs were designed and synthesized to make a full screening of the N-terminal amide bonds, and the loss of GLP-1 receptor (GLP-1R) activation indicated the importance of amide H-bonds. Secondly, with retaining the N-terminal amide H-bonds, the β-peptide replacement strategy was used and analogs were synthesized. By two rounds of screening, analog (I) was identified. Analog (I) greatly improved the DPP-IV resistance with maintaining good GLP-1R activation in vitro, and showed approx. a 4-fold prolonged blood glucose-lowering activity in vivo in comparison with tGLP-1. This modification strategy will benefit the development of GLP-1-based anti-diabetic drugs.
Bioorganic & Medicinal Chemistry published new progress about 77128-73-5. 77128-73-5 belongs to ethers-buliding-blocks, auxiliary class Inhibitor, name is (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid, and the molecular formula is C25H23NO4, Recommanded Product: (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)(methyl)amino)-3-phenylpropanoic acid.
Referemce:
https://en.wikipedia.org/wiki/Ether,
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