Grob, Nathalie M.; Schibli, Roger; Behe, Martin; Valverde, Ibai E.; Mindt, Thomas L. published an article in 2021. The article was titled 《1,5-Disubstituted 1,2,3-Triazoles as Amide Bond Isosteres Yield Novel Tumor-Targeting Minigastrin Analogs》, and you may find the article in ACS Medicinal Chemistry Letters.Application In Synthesis of Benzyl 2-bromoacetate The information in the text is summarized as follows:
1,5-Disubstituted 1,2,3-triazoles (1,5-Tz) are considered bioisosteres of cis-amide bonds. However, their use for enhancing the pharmacol. properties of peptides or proteins is not yet well established. Aiming to illustrate their utility, we chose the peptide conjugate [Nle15]MG11 (DOTA-DGlu-Ala-Tyr-Gly-Trp-Nle-Asp-Phe-NH2) as a model compound since it is known that the cholecystokinin-2 receptor (CCK2R) is able to accommodate turn conformations. Analogs of [Nle15]MG11 incorporating 1,5-Tz in the backbone were synthesized and radiolabeled with lutetium-177, and their pharmacol. properties (cell internalization, receptor binding affinity and specificity, plasma stability, and biodistribution) were evaluated and compared with [Nle15]MG11 as well as their previously reported analogs bearing 1,4-disubstituted 1,2,3-triazoles. Our investigations led to the discovery of novel triazole-modified analogs of [Nle15]MG11 with nanomolar CCK2R-binding affinity and 2-fold increased tumor uptake. This study illustrates that substitution of amides by 1,5-disubstituted 1,2,3-triazoles is an effective strategy to enhance the pharmacol. properties of biol. active peptides. In the part of experimental materials, we found many familiar compounds, such as Benzyl 2-bromoacetate(cas: 5437-45-6Application In Synthesis of Benzyl 2-bromoacetate)
Benzyl 2-bromoacetate(cas: 5437-45-6) belongs to benzyl acetate. Benzyl acetate is an aromatic chemical, usually appearing as a clear liquid with a moderate sweet-jasmine fragrance. This compound appears as a component of some of our fragrance blends.Application In Synthesis of Benzyl 2-bromoacetate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary