Structure-Activity Relationships of 9-Substituted-9-Dihydroerythromycin-Based Motilin Agonists: Optimizing for Potency and Safety was written by Shaw, Simon J.;Chen, Yue;Zheng, Hao;Fu, Hong;Burlingame, Mark A.;Marquez, Saul;Li, Yong;Claypool, Mark;Carreras, Christopher W.;Crumb, William;Hardy, Dwight J.;Myles, David C.;Liu, Yaoquan. And the article was included in Journal of Medicinal Chemistry in 2009.Formula: C8H7BrO2 This article mentions the following:
A series of 9-dihydro-9-acetamido-N-desmethyl-N-iso-Pr erythromycin A analogs and related derivatives was generated as motilin agonists. The compounds were optimized for potency while showing both minimal antibacterial activity and hERG inhibition. As the substituent on the amide was increased in lipophilicity the potency and hERG inhibition increased, while polar groups lowered potency, without significantly impacting hERG inhibition. The N-Me acetamide (7a) showed the optimal in vitro profile and was probed further by varying the chain length to the macrocycle as well as changing the macrocycle scaffold. Compound 7a remained the compound with the best in vitro properties. In the experiment, the researchers used many compounds, for example, 3-(Bromomethyl)benzoic acid (cas: 6515-58-8Formula: C8H7BrO2).
3-(Bromomethyl)benzoic acid (cas: 6515-58-8) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. In the pharmaceutical industry organo bromine derivatives are used as sedatives, vasodilators, antiseptic agents, and anticancer agents.Formula: C8H7BrO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary