Design, synthesis, and structure-activity relationship study of novel GLP-1/GIP/GCG triple receptor agonists.

In this study, to achieve more effective blood sugar lowering and weight-loss effects, eight glucagon-like peptide-1 (GLP-1)/glucose-dependent insulinotropic peptide (GIP)/glucagon (GCG) triple receptor agonists were designed and synthesized. Their sixteen related conjugates were obtained through Cys alkylation and Lys esterification modifications with two fatty acid side chains, respectively. After chemical structure confirmation using high-resolution mass spectrometry and peptide mapping, in vitro and in vivo biological effects of TRA01-24 were assessed.

DMR040, a potential antifungal compound.

Based on DMR022 [(AEEA-Gly)-AEEA-amphotericin B methyl ester, AEEA is the abbreviation of 8-amino-3,6-dioxaoctanoic acid] and DMR031 [(AEEA)-amphotericin B methyl ester], DMR040 [(AEEA)-amphotericin B methyl ester] was further designed and synthesised. Firstly, DMR040 was assessed for its antifungal activity and haemolytic toxicity with the broth dilution method and sterile defibrinated sheep blood, respectively. The minimal inhibitory concentration (MIC) of DMR040 (2 μg/mL) against Candida albicans ATCC 10231 and ATCC 90028 was reduced by 2 times compared to that of amphotericin B (1 μg/mL).