Author: Mizuhara, Tsukasa
Title: Structure–Activity Relationship Study of PD 404182 Derivatives for the Highly Potent Anti-HIV Agents Cord-id: 2f2yqsd2 Document date: 2013_10_8
ID: 2f2yqsd2
Snippet: Using facile synthetic approaches to pyrimido[1,2-c][1,3]benzothiazin-6-imines and related tricyclic derivatives, the parallel structural optimizations were investigated for the central 1,3-thiazin-2-imine core, the benzene part, and the cyclic amidine part of PD 404182. Replacement of the 6-6-6 pyrimido[1,2-c][1,3]benzothiazin-6-imine framework with 5-6-6 or 6-6-5 derivatives led to a significant loss of anti-HIV activity, and introduction of a hydrophobic group at the 9- or 10-positions improv
Document: Using facile synthetic approaches to pyrimido[1,2-c][1,3]benzothiazin-6-imines and related tricyclic derivatives, the parallel structural optimizations were investigated for the central 1,3-thiazin-2-imine core, the benzene part, and the cyclic amidine part of PD 404182. Replacement of the 6-6-6 pyrimido[1,2-c][1,3]benzothiazin-6-imine framework with 5-6-6 or 6-6-5 derivatives led to a significant loss of anti-HIV activity, and introduction of a hydrophobic group at the 9- or 10-positions improved the potency. The most potent PD 404182 derivative exerts anti-HIV effects at an early stage of viral infection including binding and fusion.
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