Muraglia, Ester; Kinzel, Olaf; Gardelli, Cristina; Crescenzi, Benedetta; Donghi, Monica; Ferrara, Marco; Nizi, Emanuela; Orvieto, Federica; Pescatore, Giovanna; Laufer, Ralph; Gonzalez-Paz, Odalys; Di Marco, Annalise; Fiore, Fabrizio; Monteagudo, Edith; Fonsi, Massimiliano; Felock, Peter J.; Rowley, Michael; Summa, Vincenzo published an article on February 28 ,2008. The article was titled 《Design and Synthesis of Bicyclic Pyrimidinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors》, and you may find the article in Journal of Medicinal Chemistry.SDS of cas: 1688-95-5 The information in the text is summarized as follows:
HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral replication, but integrase inhibitors as marketed drugs have just very recently started to emerge. In this study, the evolution from the N-methylpyrimidinone structure to bicyclic pyrimidinones, e.g., I and II, is shown. Introduction of a suitably substituted amino moiety modulated the phys.-chem. properties of the mols. and conferred nanomolar activity in the inhibition of spread of HIV-1 infection in cell culture. An extensive SAR study led to sulfamide I, which inhibited the strand transfer with an IC50 of 7 nM and HIV infection in MT4 cells with a CIC95 of 44 nM, and ketoamide II that inhibited strand transfer with an IC50 of 12 nM and the HIV infection in MT4 cells with a CIC95 of 13 nM and exhibited a good pharmacokinetic profile when dosed orally to preclin. species. The experimental process involved the reaction of 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5SDS of cas: 1688-95-5)
4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.SDS of cas: 1688-95-5
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics