Computed Properties of C9H9BrO2In 2021 ,《Discovery of a First-In-Class Small Molecule Antagonist against the Adrenomedullin-2 Receptor: Structure-Activity Relationships and Optimization》 was published in Journal of Medicinal Chemistry. The article was written by Zirimwabagabo, Jean-Olivier; Jailani, Ameera B. A.; Avgoustou, Paris; Tozer, Matthew J.; Gibson, Karl R.; Glossop, Paul A.; Mills, James E. J.; Porter, Roderick A.; Blaney, Paul; Wang, Ning; Skerry, Timothy M.; Richards, Gareth O.; Harrity, Joseph P. A.. The article contains the following contents:
Class B G-protein-coupled receptors (GPCRs) remain an underexploited target for drug development. The calcitonin receptor (CTR) family is particularly challenging, as its receptors are heteromers comprising two distinct components: the calcitonin receptor-like receptor (CLR) or calcitonin receptor (CTR) together with one of three accessory proteins known as receptor activity-modifying proteins (RAMPs). CLR/RAMP1 forms a CGRP receptor, CLR/RAMP2 forms an adrenomedullin-1 (AM1) receptor, and CLR/RAMP3 forms an adrenomedullin-2 (AM2) receptor. The CTR/RAMP complexes form three distinct amylin receptors. While the selective blockade of AM2 receptors would be therapeutically valuable, inhibition of AM1 receptors would cause clin. unacceptable increased blood pressure. We report here a systematic study of structure-activity relationships that has led to the development of first-in-class AM2 receptor antagonists such as I. These compounds exhibit therapeutically valuable properties with 1000-fold selectivity over the AM1 receptor. These results highlight the therapeutic potential of AM2 antagonists. In the experiment, the researchers used many compounds, for example, Benzyl 2-bromoacetate(cas: 5437-45-6Computed Properties of C9H9BrO2)
Benzyl 2-bromoacetate(cas: 5437-45-6) has been used in the alkylation of (-)-2,3-O-isopropylidene-D-threitol that afforded lipopeptide, 2-[(4R,5R)-5-({[(9H-fluoren-9-yl)methoxy]carbonylaminomethyl}-2,2-dimethyl-1,3-dioxolan-4-yl)methoxy]acetic acid.Computed Properties of C9H9BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary