Optimization of the pharmacokinetic properties of potent anti-trypanosomal triazine derivatives was written by Salado, Irene G.;Baan, Adrienn;Verdeyen, Tomas;Matheeussen, An;Caljon, Guy;Van der Veken, Pieter;Kiekens, Filip;Maes, Louis;Augustyns, Koen. And the article was included in European Journal of Medicinal Chemistry in 2018.Recommanded Product: 4,6-Dichloro-N-phenyl-1,3,5-triazin-2-amine The following contents are mentioned in the article:
Human African trypanosomiasis is causing thousands of deaths every year in the rural areas of sub-saharan Africa. There is a high unmet medical need since the approved drugs are poorly efficacious, show considerable toxicity and are not easy to administer. This work describes the optimization of the pharmacokinetic properties of a previously published family of triazine lead compounds One compound (35 (UAMC-03011)) with potent anti-trypanosomal activity and no cytotoxicity was selected for further study because of its good microsomal stability and high selectivity for Trypanosoma brucei over a panel including Trypanosoma cruzi, Leishmania infantum, and Plasmodium falciparum. In vivo pharmacokinetic parameters were determined and the compound was studied in an acute in vivo mouse disease model. One of the important learnings of this study was that the rate of trypanocidal activity is an important parameter during the lead optimization process. This study involved multiple reactions and reactants, such as 4,6-Dichloro-N-phenyl-1,3,5-triazin-2-amine (cas: 2272-40-4Recommanded Product: 4,6-Dichloro-N-phenyl-1,3,5-triazin-2-amine).
4,6-Dichloro-N-phenyl-1,3,5-triazin-2-amine (cas: 2272-40-4) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Recommanded Product: 4,6-Dichloro-N-phenyl-1,3,5-triazin-2-amine
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics