||Identification of anti-HIV agents with a novel benzo[4,5]isothiazolo[2,3-a]pyrimidine scaffold.
Okazaki, Shiho ,
Mizuhara, Tsukasa ,
Shimura, Kazuya ,
Murayama, Hiroto ,
Ohno, Hiroaki ,
Oishi, Shinya ,
Matsuoka, MasaoFujii, Nobutaka
Bioorganic & medicinal chemistry
1452 , 2015-04-01 , Elsevier Ltd.
3, 4-Dihydro-2H-benzo[4, 5]isothiazolo[2, 3-a]pyrimidine is a newly identified antiviral agent against human immunodeficiency virus type 1 (HIV-1) infection, derived from 3, 4-dihydro-2H, 6H-pyrimido[1, 2-c][1, 3]benzothiazin-6-imine (PD 404182). The introduction of the hydrophobic 8-aryl substituent on the benzene substructure improved its anti-HIV activity, resulting in the identification of 6-fold more potent analogs. In addition, it was demonstrated that these isothiazolopyrimidine derivatives exert anti-HIV effects at an early stage of viral infection.