Hotra, Adam; Ragunathan, Priya; Ng, Pearly Shuyi; Seankongsuk, Pattarakiat; Harikishore, Amaravadhi; Sarathy, Jickky Palmae; Saw, Wuan-Geok; Lakshmanan, Umayal; Sae-Lao, Patcharaporn; Kalia, Nitin Pal; Shin, Joon; Kalyanasundaram, Revathy; Anbarasu, Sivaraj; Parthasarathy, Krupakar; Pradeep, Chaudhari Namrata; Makhija, Harshyaa; Droege, Peter; Poulsen, Anders; Tan, Jocelyn Hui Ling; Pethe, Kevin; Dick, Thomas; Bates, Roderick W.; Grueber, Gerhard published an article in Angewandte Chemie, International Edition. The title of the article was 《Discovery of a Novel Mycobacterial F-ATP Synthase Inhibitor and its Potency in Combination with Diarylquinolines》.Product Details of 86443-51-8 The author mentioned the following in the article:
The F1FO-ATP synthase is required for growth and viability of Mycobacterium tuberculosis and is a validated clin. target. A mycobacterium-specific loop of the enzyme’s rotary γ subunit plays a role in the coupling of ATP synthesis within the enzyme complex. We report the discovery of a novel antimycobacterial, termed GaMF1 (I), that targets this γ subunit loop. Biochem. and NMR studies show that GaMF1 inhibits ATP synthase activity by binding to the loop. GaMF1 is bactericidal and is active against multidrug- as well as bedaquiline-resistant strains. Chem. efforts on the scaffold revealed a dynamic structure activity relationship and delivered analogs with nanomolar potencies. Combining GaMF1 with bedaquiline or novel diarylquinoline analogs showed potentiation without inducing genotoxicity or phenotypic changes in a human embryonic stem cell reporter assay. These results suggest that GaMF1 presents an attractive lead for the discovery of a novel class of anti-tuberculosis F-ATP synthase inhibitors.2-Chloro-N-ethylpyrimidin-4-amine(cas: 86443-51-8Product Details of 86443-51-8) was used in this study.
2-Chloro-N-ethylpyrimidin-4-amine(cas: 86443-51-8) belongs to anime. In organic chemistry, amines are compounds and functional groups that contain a basic nitrogen atom with a lone pair. Amines are formally derivatives of ammonia (NH3), wherein one or more hydrogen atoms have been replaced by a substituent such as an alkyl or aryl group (these may respectively be called alkylamines and arylamines; amines in which both types of substituent are attached to one nitrogen atom may be called alkylarylamines).Product Details of 86443-51-8
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia