New Broad-Spectrum Antibiotics Containing a Pyrrolobenzodiazepine Ring with Activity against Multidrug-Resistant Gram-Negative Bacteria was written by Picconi, Pietro;Hind, Charlotte K.;Nahar, Kazi S.;Jamshidi, Shirin;Di Maggio, Lucia;Saeed, Naima;Evans, Bonnie;Solomons, Jessica;Wand, Matthew E.;Sutton, J. Mark;Rahman, Khondaker Miraz. And the article was included in Journal of Medicinal Chemistry in 2020.Name: Methyl 4-bromo-1-methyl-1H-pyrrole-2-carboxylate This article mentions the following:
It is urgent to find new antibiotic classes with activity against multidrug-resistant (MDR) Gram-neg. pathogens as the pipeline of antibiotics is essentially empty. Modified pyrrolobenzodiazepines with a C8-linked aliphatic heterocycle provide a new class of broad-spectrum antibacterial agents with activity against MDR Gram-neg. bacteria, including WHO priority pathogens. The structure-activity relationship established that the third ring was particularly important for Gram-neg. activity. Min. inhibitory concentrations for the lead compounds ranged from 0.125 to 2 mg/L for MDR Gram-neg., excluding Pseudomonas aeruginosa, and between 0.03 and 1 mg/L for MDR Gram-pos. species. The lead compounds were rapidly bactericidal with >5 log reduction in viable count within 4 h for Acinetobacter baumannii and Klebsiella pneumoniae. The lead compound inhibited DNA gyrase in gel-based assays, with an IC50 of 3.16 ± 1.36 mg/L. This study provides a new chem. scaffold for developing novel broad-spectrum antibiotics which can help replenish the pipeline of antibiotics. In the experiment, the researchers used many compounds, for example, Methyl 4-bromo-1-methyl-1H-pyrrole-2-carboxylate (cas: 1196-90-3Name: Methyl 4-bromo-1-methyl-1H-pyrrole-2-carboxylate).
Methyl 4-bromo-1-methyl-1H-pyrrole-2-carboxylate (cas: 1196-90-3) belongs to organobromine compounds. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Name: Methyl 4-bromo-1-methyl-1H-pyrrole-2-carboxylate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary