55486-27-6Relevant articles and documents
In quest of small-molecules as potent non-competitive inhibitors against influenza
Malbari, Khushboo,Saha, Priyanka,Chawla-Sarkar, Mamta,Dutta, Shanta,Rai, Swita,Joshi, Mamata,Kanyalkar, Meena
, (2021/07/19)
A series of scaffolds namely aurones, 3-indolinones, 4-quinolones and cinnamic acid-piperazine hybrids, was designed, synthesized and investigated in vitro against influenza A/H1N1pdm09 virus. Designed molecules adopted different binding mode i.e., in 430-cavity of neuraminidase, unlike sialic acid and oseltamivir in molecular docking studies. All molecules reduced the viral titer and exhibited non-cytotoxicity along with cryo-protective property towards MDCK cells. Molecules (Z)-2-(3′-Chloro-benzylidene)-1,2-dihydro-indol-3-one (2f), (Z)-2-(4′-Chloro-benzylidene)-1,2-dihydro-indol-3-one (2g) and 2-(2′-Methoxy-phenyl)-1H-quinolin-4-one (3a) were the most interesting molecules identified in this research, endowed with robust potencies showing low-nanomolar EC50 values of 4.0 nM, 6.7 nM and 4.9 nM, respectively, compared to reference competitive and non-competitive inhibitors: oseltamivir (EC50 = 12.7 nM) and quercetin (EC50 = 0.56 μM), respectively. Besides, 2f, 2g and 3a exhibited good neuraminidase inhibitory activity in sub-micromolar range (IC50 = 0.52 μM, 3.5 μM, 1.3 μM respectively). Moreover, these molecules were determined as non-competitive inhibitors similar to reference non-competitive inhibitor quercetin unlike reference competitive inhibitor oseltamivir in kinetics studies.
1 - (cinnamoyl) - 4-piperidyl amide piperazine compound and its preparation method
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Paragraph 0021-0023, (2016/10/08)
The invention discloses a 1-(cinnamoyl)-4-piperidyl amide piperazidine compound and a preparation method thereof. The 1-(cinnamoyl)-4-piperidyl amide piperazidine compound is a compound shown as the formula (I) and pharmaceutically acceptable salt. The co
Preparing method of N-monosubstituted piperazine compound
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Paragraph 0028; 0029, (2017/06/02)
The invention discloses a preparing method of an N-monosubstituted piperazine compound shown in the formula (6). Piperazine monohydrochloride (1) and RX or RCl react in solvent to prepare monosubstituted piperazine dihydrochloride (4) or (5), alkali is added for neutralizing, and the product (6) is obtained through rectification steaming.