Safety of 1-MethylpiperazineIn 2020 ,《Design and optimization of quinazoline derivatives: new non-nucleoside inhibitors of bovine viral diarrhea virus》 appeared in Frontiers in Chemistry (Lausanne, Switzerland). The author of the article were Fernandez, Gabriela A.; Castro, Eliana F.; Rosas, Rocio A.; Fidalgo, Daniela M.; Adler, Natalia S.; Battini, Leandro; Espana de Marco, Maria J.; Fabiani, Matias; Bruno, Ana M.; Bollini, Mariela; Cavallaro, Lucia V.. The article conveys some information:
In a previous work, potential mols. that dock into an allosteric binding pocket of BVDV RdRp via a structure-based virtual screening approach was identified. One of them, N-(2-morpholinoethyl)-2-phenylquinazolin-4-amine I [R2 = Ph; R4 = 2-morpholinoethylamino; R7 = H] [50% effective concentration (EC50) = 9.7 ± 0.5μM], was selected to perform different chem. modifications. Among synthesized derivatives I [R2 = H, Ph, 4-MeC6H4, etc.; R4 = 4-methylpiperazin-1-yl, HN(CH2)5CH3, 4-methoxyanilino, etc.; R7 = H, Cl], compound I [R2 = H, Ph, 4-(Me)2NC6H4; R4 = 4-methylpiperazin-1-yl, 3-(dimethylamino)propylamino, 4-(2-hydroxyethyl)piperazin-1-yl, (2-morpholinoethylamino), 2-(1-piperidyl)ethylamino, 2-(1-piperidyl)ethylamino, (2,2,6,6-tetramethyl-4-piperidyl)amino, ; R7 = H, Cl] of them showed considerable antiviral activity. Mol. modeling of the most active compounds I [R2 = H, Ph, 4-MeC6H4, 4-MeOC6H4, 4-O2NC6H4, 4-(Me)2NC6H4; R4 = 4-methylpiperazin-1-yl, 3-(dimethylamino)propylamino, 4-(2-hydroxyethyl)piperazin-1-yl, 2-morpholinoethylamino, 2-(1-piperidyl)ethylamino, (2,2,6,6-tetramethyl-4-piperidyl)amino; R7 = H, Cl] showed that they bind to a pocket located in the fingers and thumb domains in BVDV RdRp, which was different than that identified for other non-nucleoside inhibitors (NNIs) such as thiosemicarbazone (TSC). Compound 2-[4-(2-phenylquinazolin-4-yl)piperazin-1-yl]ethanol I [R2 = Ph; R4 = 4-(2-hydroxyethyl)piperazin-1-yl; R7 = H] ( EC50 = 1.7 ± 0.4μM) was selected for further anal. Compound I [R2 = Ph; R4 = 4-(2-hydroxyethyl)piperazin-1-yl; R7 = H] was found to inhibit the in vitro replication of TSC-resistant BVDV variants, which carry the N264D mutation in the RdRp. In addition, I [R2 = Ph; R4 = 4-(2-hydroxyethyl)piperazin-1-yl; R7 = H] presented adequate solubility in different media and a high-stability profile in murine and bovine plasma. In the experiment, the researchers used 1-Methylpiperazine(cas: 109-01-3Safety of 1-Methylpiperazine)
1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Safety of 1-Methylpiperazine
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics