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In order to expand the structure-activity relationship(SAR) studies on arylazolylthioacetanilide NNRTIs [1-14],based on the structure-based bioisosterism principle,a series of novel 2-(5-(naphthalen-1-yl)-1,2,3-thiadiazol-4-ylthio)-N-acetamides derivatives were designed,synthesized and evaluated for their anti-HIV activities in MT-4 cells.