《Thiazolothiazepine Inhibitors of HIV-1 Integrase》 was written by Neamati, Nouri; Turpin, Jim A.; Winslow, Heather E.; Christensen, John L.; Williamson, Karen; Orr, Ann; Rice, William G.; Pommier, Yves; Garofalo, Antonio; Brizzi, Antonella; Campiani, Giuseppe; Fiorini, Isabella; Nacci, Vito. Recommanded Product: 1-Methylpiperazine dihydrochloride And the article was included in Journal of Medicinal Chemistry on August 26 ,1999. The article conveys some information:
A series of thiazolothiazepines were prepared and tested against purified human immunodeficiency virus type-1 integrase (HIV-1 IN) and viral replication. Structure-activity studies reveal that the compounds possessing the pentat. moiety SC(O)CNC(O) with two carbonyl groups are in general more potent against purified IN than those containing only one carbonyl group. Substitution with electron-donating or -withdrawing groups did not enhance nor abolish potency against purified IN. By contrast, compounds with a naphthalene ring system showed enhanced potency, suggesting that a hydrophobic pocket in the IN active site might accommodate an aromatic system rather than a halogen. The position of sulfur in the thiazole ring appears important for potency against IN, as its replacement with an oxygen or carbon abolished activity. Further extension of the thiazole ring diminished potency. I [R, R1 = H, X = S, Y = CH2; RR1 = CH:CHCH:CH; X = S, Y = CH2; X = CH2, Y = S] showed antiviral activity and inhibited IN within similar concentrations These compounds inhibited IN when Mn2+ or Mg2+ was used as cofactor. None of these compounds showed detectable activities against HIV-1 reverse transcriptase, protease, virus attachment, or nucleocapsid protein zinc fingers. Therefore, thiazolothiazepines are potentially important lead compounds for development as inhibitors of IN and HIV replication. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Recommanded Product: 1-Methylpiperazine dihydrochloride)
1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Recommanded Product: 1-Methylpiperazine dihydrochloride
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics