Safety of 3,5-Dimethyl-1H-pyrazole. Liu, J; Ren, ZH; Fan, L; Wei, JY; Tang, XM; Xu, XR; Yang, DC in [Liu, Jie; Ren, Zhenghong; Fan, Li; Wei, Jianyong; Yang, Dacheng] Southwest Univ, Sch Chem & Chem Engn, Inst Bioorgan & Med Chem, Key Lab Appl Chem Chongqing Municipal, Chongqing 400715, Peoples R China; [Tang, Xuemei] Southwest Univ, Sch Life Sci, Chongqing 400715, Peoples R China; [Xu, Xingran] Southwest Univ, Coll Pharmaceut Sci, Chongqing 400715, Peoples R China published Design, synthesis, biological evaluation, structure-activity relationship, and toxicity of clinafloxacin-azole conjugates as novel antitubercular agents in 2019.0, Cited 44.0. The Name is 3,5-Dimethyl-1H-pyrazole. Through research, I have a further understanding and discovery of 67-51-6.
Based on the advantages of azole molecules and fluoroquinolone drugs, we designed and synthesized 34 clinafloxacin- azole conjugates using fragment-based drug design and drug combination principles. The in vitro activities of the synthesized conjugates against Mycobacterium tuberculosis (H37Rv), Hela cell as well as Gram-positive and Gram-negative bacteria were assayed. The bioassay results revealed that most of the target molecules had anti-tuberculosis (anti-TB) activity, of which 14 compounds had very strong anti-TB activity [minimum inhibitory concentration (MIC) < 2 mu M]. In addition, the compounds with strong activity towards H37Rv had weak activity towards Gram-negative and Gram-positive bacteria, showing obvious selectivity towards H37Rv. Predicted toxicity data indicated that 27 molecules were less toxic or equivalent to that of the original drug (clinafloxacin). Especially, it is demonstrated that compound TM2l exhibited the strongest anti-TB activity (MIC = 0.29 mu M), low antibacterial activity, negligible toxicity, and good drug-likeness values, which can be considered as an ideal lead molecule for future optimization. Welcome to talk about 67-51-6, If you have any questions, you can contact Liu, J; Ren, ZH; Fan, L; Wei, JY; Tang, XM; Xu, XR; Yang, DC or send Email.. Safety of 3,5-Dimethyl-1H-pyrazole
Reference:
Pyrazole – Wikipedia,
,Pyrazoles – an overview | ScienceDirect Topics