Safety of 3-Nitrobenzaldehyde. Authors Kratky, M; Svrckova, K; Vu, QA; Stepankova, S; Vinsova, J in MDPI published article about in [Kratky, Martin; Vu, Quynh Anh; Vinsova, Jarmila] Charles Univ Prague, Dept Organ & Bioorgan Chem, Fac Pharm Hradec Kralove, Akad Heyrovskeho 1203, Hradec Kralove 50005, Czech Republic; [Svrckova, Katarina; Stepankova, Sarka] Univ Pardubice, Fac Chem Technol, Dept Biol & Biochem Sci, Studentska 573, Pardubice 53210, Czech Republic in 2021, Cited 31. The Name is 3-Nitrobenzaldehyde. Through research, I have a further understanding and discovery of 99-61-6
Based on the broad spectrum of biological activity of hydrazide-hydrazones, trifluoromethyl compounds, and clinical usage of cholinesterase inhibitors, we investigated hydrazones obtained from 4-(trifluoromethyl)benzohydrazide and various benzaldehydes or aliphatic ketones as potential inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). They were evaluated using Ellman’s spectrophotometric method. The hydrazide-hydrazones produced a dual inhibition of both cholinesterase enzymes with IC50 values of 46.8-137.7 mu M and 19.1-881.1 mu M for AChE and BuChE, respectively. The majority of the compounds were stronger inhibitors of AChE; four of them (2-bromobenzaldehyde, 3-(trifluoromethyl)benzaldehyde, cyclohexanone, and camphor-based 2o, 2p, 3c, and 3d, respectively) produced a balanced inhibition of the enzymes and only 2-chloro/trifluoromethyl benzylidene derivatives 2d and 2q were found to be more potent inhibitors of BuChE. 4-(Trifluoromethyl)-N’-[4-(trifluoromethyl)benzylidene]benzohydrazide 2l produced the strongest inhibition of AChE via mixed-type inhibition determined experimentally. Structure-activity relationships were identified. The compounds fit physicochemical space for targeting central nervous systems with no apparent cytotoxicity for eukaryotic cell line together. The study provides new insights into this CF3-hydrazide-hydrazone scaffold.
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