Wang, Lei; Zhou, Xia; Lu, Hui; Mu, Xianfu; Jin, Linhong published the artcile< Synthesis and antibacterial evaluation of novel 1,3,4-oxadiazole derivatives containing sulfonate/carboxylate moiety>, Category: esters-buliding-blocks, the main research area is sulfonate carboxylate oxadiazole preparation agrochem antibacterial activity; 1,3,4-oxadiazole derivatives; antibacterial activity; scanning electron microscopy; xanthomonas axonopodis pv. Citri; xanthomonas oryzae pv. oryzae.
Novel sulfonate/carboxylate functionalized 1,3,4-oxadiazole derivatives I (R1 = Me, Et, 2-fluoroethyl; R2 = Ph, 2-fluorophenyl, 4-chlorophenyl, etc.) and II [R1 = Me; R3 = Ph, 4-bromophenyl, N(CH3)2, etc.] were synthesized and evaluated for their antibacterial activities. Antibacterial activity against two phytopathogens, Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas axonopodis pv. citri (Xac), was assayed in vitro. The preliminary results indicated that ten compounds including I [R1 = Ph, R2 = Me (A); R1 = 4-fluorophenyl, R2 = Me (B); R1 = 4-chlorophenyl, R2 = Me (C); R1 = 4-bromophenyl, R2 = Me (D); R1 = 4-fluorophenyl, R2 = Et; R1 = 4-chlorophenyl, R2 = Et; R1 = 4-bromophenyl, R2 = Et; R1 = 4-fluorophenyl, R2 = 2-fluoroethyl; R1 = 4-chlorophenyl, R2 = 2-fluoroethyl; R1 = 4-bromophenyl, R2 = 2-fluoroethyl] had good antibacterial activity against Xoo, with EC50 values ranging from 50.1-112.5μM, which was better than those of Bismerthiazol (253.5μM) and thiadiazole copper (467.4μM). Meanwhile, compounds(A), (B), (C), (D) demonstrated good inhibitory effect against Xanthomonas axonopodis pv. citri with EC50 values around 95.8-155.2μM which were better than those of bismerthiazol (274.3μM) and thiadiazole copper (406.3μM). In addition, in vivo protection activity of compounds (B), (C) against rice bacterial leaf blight was 68.6% and 62.3%, resp., which were better than bismerthiazol (49.6%) and thiadiazole copper (42.2%). Curative activity of compounds (B), (C) against rice bacterial leaf blight was 62.3% and 56.0%, which were better than bismerthiazol (42.9%) and thiadiazole copper (36.1%). Through SEM (SEM) anal., it was observed that compound (B) caused the cell membrane of Xanthomonas oryzae pv. oryzae ruptured or deformed. The present results indicated novel derivatives of 4-Ph sulfonate Me 1,3,4-oxadiazole I might be potential antibacterial agents.
Molecules published new progress about Acid chlorides Role: RCT (Reactant), RACT (Reactant or Reagent). 623-50-7 belongs to class esters-buliding-blocks, and the molecular formula is C4H8O3, Category: esters-buliding-blocks.
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