Name: N,N-Dimethylformamide Dimethyl AcetalIn 2020 ,《Novel bis(pyrazole-benzofuran) hybrids possessing piperazine linker: Synthesis of potent bacterial biofilm and MurB inhibitors》 appeared in Bioorganic Chemistry. The author of the article were Mekky, Ahmed E. M.; Sanad, Sherif M. H.. The article conveys some information:
Novel 1,4-bis[(2-(3-(dimethylamino)-1-oxoprop-2-en-1-yl)benzofuran-5-yl)methyl]piperazine I [X = Me2NCH:CHC(O)] was prepared and used as a key synthon for the this protocol. 1,3-Dipolar cycloaddition of this synthon with the appropriate hydrazonyl chlorides R1C(O)CCl:NNHR2 (R1 = Me, EtO; R2 = Ph, 4-ClC6H4, 4-MeC6H4, 4-MeOC6H4, 4-O2NC6H4) afforded a new series of bis-pyrazoles I (X = 1-R2-3-(R1CO)-pyrazol-4-ylcarbonyl). Furthermore, the latter reacted with hydrazine hydrate to afford bis(pyrazolo[3,4-d]pyridazine)s I (X = 7-methyl-2-R2-2H-pyrazolo[3,4-d]pyridazin-4-yl, 7-oxo-2-R2-6,7-dihydro-2H-pyrazolo[3,4-d]pyridazin-4-yl). Reaction of the synthon I [X = Me2NCH:CHC(O)] with hydrazine hydrate or phenylhydrazine afforded the corresponding bis(pyrazole)s I (X = 1H-pyrazol-3-yl, 1-phenyl-1H-pyrazol-5-yl), resp. The reaction of I (X = MeCO) with Ph hydrazine followed by treatment with DMF-DMA resulted in I (X = 1-phenyl-1H-pyrazol-4-yl). Various bacterial strains and cell lines were selected to study the in-vitro antibacterial and cytotoxic activities for the synthesized compounds The compound I [X = 1-(4-nitrophenyl)-3-acetyl-1H-pyrazol-4-ylcarbonyl; (II)] showed the best antibacterial efficacies with MIC/MBC values of 1.2/1.2, 1.2/2.4 and 1.2/2.4μM against each of E. coli, S. aureus and S. mutans strains, resp. In addition, the inhibitory activity of some compounds as MRSA and VRE inhibitors were studied. The compound II gave the best inhibitory activity with MIC/MBC values of 18.1/36.2, 9.0/18.1 and 18.1/18.1μM, resp., against MRSA (ATCC:33591 and ATCC:43300) and VRE (ATCC:51575) bacterial strains, resp. This compound also showed more effective biofilm inhibition activities than the reference Ciprofloxacin. The compound II showed IC50 values of 3.0 ±0.05, 3.2 ±0.08 and 3.3 ± 0.07μM against S. aureus, S. mutans and E. coli strains, resp. Furthermore, exptl. study showed excellent inhibitory activities of compounds I [X = 1-R2-3-(R1CO)-pyrazol-4-ylcarbonyl; R2 = 4-ClC6H4, 4-O2NC6H4] against MurB enzyme. The compound II gave the best MurB inhibitory activity with IC50 value of 3.1μM. The in-silico study was performed to predict the capability of compounds I [X = 1-R2-3-(R1CO)-pyrazol-4-ylcarbonyl; R2 = 4-ClC6H4, 4-O2NC6H4] as potential inhibitors of MurB enzyme. In the experiment, the researchers used N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5Name: N,N-Dimethylformamide Dimethyl Acetal)
N,N-Dimethylformamide Dimethyl Acetal(cas: 4637-24-5) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Name: N,N-Dimethylformamide Dimethyl Acetal
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