In 2022,Li, Yue; Ouyang, Yifan; Wu, Han; Wang, Peng; Huang, Yu; Li, Xue; Chen, Hongtong; Sun, Yu; Hu, Xinxin; Wang, Xiukun; Li, Guoqing; Lu, Yun; Li, Congran; Lu, Xi; Pang, Jing; Nie, Tongying; Sang, Xiaohong; Dong, Luyao; Dong, Wenting; Jiang, Jiandong; Paterson, Ian C.; Yang, Xinyi; Hong, Wei; Wang, Hao; You, Xuefu published an article in European Journal of Medicinal Chemistry. The title of the article was 《The discovery of 1, 3-diamino-7H-pyrrol[3, 2-f]quinazoline compounds as potent antimicrobial antifolates》.Application of 1129-28-8 The author mentioned the following in the article:
The shortage of new antibiotics makes infections caused by gram-neg. (G-) bacteria a significant clin. problem. The key enzymes involved in folate biosynthesis represent important targets for drug discovery, and new antifolates with novel mechanisms are urgently needed. By targeting to dihydrofolate reductase (DHFR), a series of 1,3-diamino-7H-pyrrol[3,2-f]quinazoline (PQZ) compounds were designed, and exhibited potent antibacterial activities in vitro, especially against multi-drug resistant G- strains. Multiple experiments indicated that PQZ compounds contain a different mol. mechanism against the typical DHFR inhibitor, trimethoprim (TMP), and the thymidylate synthase (TS) was identified as another potential but a relatively weak target. A significant synergism between the representative compound, OYYF-175, and sulfamethoxazole (SMZ) was observed with a strong cumulative and significantly bactericidal effect at extremely low concentrations (2 μg/mL for SMZ and 0.03 pg/mL for OYYF-175), which could be resulted from the simultaneous inhibition of dihydropteroate synthase (DHPS), DHFR and TS. PQZ compounds exhibited therapeutic effects in a mouse model of i.p. infections caused by Escherichia coli (E. coli). The co-crystal structure of OYYF-175-DHFR was solved and the detailed interactions were provided. The inhibitors reported represent innovative chem. structures with novel mol. mechanism of action, which will benefit the generation of new, efficacious bactericidal compounds In addition to this study using Methyl 3-(bromomethyl)benzoate, there are many other studies that have used Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8Application of 1129-28-8) was used in this study.
Methyl 3-(bromomethyl)benzoate(cas: 1129-28-8) belongs to organobromine compounds.Most of the natural organobromine compounds are produced by marine organisms , and several brominated metabolites with antibacterial , antitumor , antiviral , and antifungal activity have been isolated from seaweed, sponges, corals, molluscs, and others. Moreover, several studies demonstrate that the average proportion of bromine in drugs is significantly higher than that in natural products. Application of 1129-28-8
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary