《Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters in 2020. These research results belong to Tan, Xiangduan; Huang, Mohan; Nian, Siyun; Peng, Yanfen; Qin, Jianli; Kong, Bo; Duan, Xiaoqun. Category: bromides-buliding-blocks The article mentions the following:
Antibiotic resistance in bacteria has been an emerging public health problem, thus discovery of novel and effective antibiotics is urgent. A series of novel hybrids of N-aryl pyrrothine-base α-pyrone hybrids was designed, synthesized and evaluated as bacterial RNA polymerase (RNAP) inhibitors. Among them, compound I exhibited potent antibacterial activity against antibiotic-resistant S. aureus with the min. inhibitory concentration (MIC) in the range of 1-4μg/mL. Moreover, compound I exhibited strong inhibitory activity against E. coli RNAP with an IC50 value of 16.06μM, and cytotoxicity in HepG2 cells with IC50 value of 7.04μM. The mol. docking study further suggested that compound I binds to the switch region of bacterial RNAP. In summary, compound I is a novel bacterial RNAP inhibitor, and a promising lead compound for further optimization. In the part of experimental materials, we found many familiar compounds, such as Ethyl 5-bromovalerate(cas: 14660-52-7Category: bromides-buliding-blocks)
Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. Most organobromine compounds, like most organohalide compounds, are relatively nonpolar. Bromine is more electronegative than carbon (2.9 vs 2.5). Consequently, the carbon in a carbon–bromine bond is electrophilic, i.e. alkyl bromides are alkylating agents.Category: bromides-buliding-blocks
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary