Journal Article 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, Masao  ,  Fujii, Nobutaka

23 ( 7 )  , pp.1447 - 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.

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