Design, Synthesis and Bioactivity of Novel 2-Aryl-4-alkylthiazole-5-carboxylic Acid Derivatives

To find new lead compounds with muti-bioactivities, a series of novel 1,3-thiazole-5-carboxylic acid derivatives containing aryloxyacetate were designed via the method of linking active sub-structures, in which the aryloxyacetate with multi-bioactivity was combined to the 1,3-thiazole moiety of ethaboxam, metsulfovax and thifluzamide. The target compounds were synthesized from beta-keto acid ester and 4-hydroxybenzothioamide in 6 steps. Their structures were confirmed by H-1 NMR, IR and HRMS techniques. The preliminary bioassay results indicated that some compounds showed obvious inhibition effects against Fusarium graminearum, and the fungicidal activity of 1j is 52% at 50 mu g/mL.