Su, Shihu; Zhou, Xia; Zhou, Yan; Liao, Guoping; Shi, Li; Yang, Xia; Zhang, Xian; Jin, Linhong published the artcile< Synthesis and biological evaluation of novel sulfone derivatives containing 1,3,4-oxadiazole moiety>, Safety of Methyl 2-bromo-5-fluorobenzoate, the main research area is sulfonyl oxadiazole preparation fungicidal SAR antibacterial toxic regression.
Series of novel sulfone derivatives containing 1,3,4-oxadiazole moiety I [R1 = 4-F-2-Me, 2,5-Cl2, 2-Br-4-F, etc.; R2 = Me, Et, CH(CH3)2, n-propyl] and II [R2 = Me, Et, CH2Ph] were synthesized. All the target compounds were characterized by 1H and 13C NMR, IR spectroscopy and elemental anal. Their antifungal activities were tested in vitro with six important phytopathogenic fungi, namely, Gibberella zeae, Fusarium oxysporum, Cytospora mandshurica, Phytophthora infestans, Paralepetopsis sasakii and Sclerotinia sclerotiorum using the mycelium growth inhibition method. Their antibacterial activities were tested in vitro with two important phytopathogenic bacteria, namely, Xanthomonas oryzae and Ralstonia solanacearum from tobacco bacterial by the turbid meter test. Compounds I [R1 = 2-Cl-4-F, 4-CF3; R2 = Me] and II [R2 = Me, Et] exhibited the most potent inhibition against R. solanacearum and X. oryzae with 50% inhibition concentration (EC50) from 1.97 to 7.75 μg/mL and 0.45 to 0.52 μg/mL, resp. Their antifungal tests indicated that among target compounds exhibited good antifungal activities against six kinds of fungi, especially against S. sclerotiorum with EC50 from 3.71 to 17.44 μg/mL. In vivo antibacterial activities tests demonstrated that the controlling effect of compound II [R2 = Me] (81.9%) against rice bacterial leaf blight were better than that of bismerthiazol (50.8%) and thiodiazole-copper (44.7%). The results also demonstrated that compounds I [R1 = 2-Cl-4-F; R2 = Me] and II [R2 = Me, Et] had a better antifungal and antibacterial activity, with good characteristics of broad spectrum. The structure-activity relationships were also discussed.
World Journal of Organic Chemistry published new progress about Agrochemical antibacterial agents. 6942-39-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H6BrFO2, Safety of Methyl 2-bromo-5-fluorobenzoate.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary