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    • 58. 发明授权
    • Antimicrobial/antifungal compositions
    • 抗微生物/抗真菌组合物
    • US4876277A
    • 1989-10-24
    • US55737
    • 1987-05-29
    • Basil A. BurkeMuraleedharan G. Nair
    • Basil A. BurkeMuraleedharan G. Nair
    • A01N43/30C07D317/64
    • A01N43/30C07D317/64
    • Substituted olefinic (allyl) benzene compounds which exhibit important antimicrobial (antibacterial and antifungal) activity, compositions and methods of delivery against pathovars and pathogens, and methods of synthesis from commonly available reactants. The antifungal composition active ingredient is one or more 4,5-substituted 2,3-alkylidenedioxy-1-olefinic benzenes of the formula: ##STR1## where R.sub.1 and R.sub.2 may be the same or different, and are selected from OH, and C.sub.1 -C.sub.5 alkoxy (--OR) or thioalkyl (--SR) groups. R.sub.3 and R.sub.4 are selected from H and C.sub.1 -C.sub.5 alkyl, alkenyl and alkynyl groups, and R.sub.5 is selected from C.sub.3 -C.sub.7 alkyl, alkenyl and alkynyl groups. The preferred compounds are 4,5-substituted-2,3-methylenedioxy-1-allyl benzenes. Where R.sub.1 =OCH.sub.3, R.sub.2 =OH, R.sub.3 and R.sub.4 =H and R.sub.5 =allyl (2',3' propenyl) the compound may be called nor methyl-pseudo-dillapiole. Where R.sub.1 =R.sub.2 =OCH.sub.3, R.sub.3 and R.sub.4 are again H, and R.sub.5 =allyl, the compound may be called pseudo-dillapiole. Compositions including these compounds exhibit antimicrobial activity against a variety of pathogens and pathovars, e.g., Xanthomonas campestris spp. bacteria, antifungal activity against a variety of fungi and bacteria, and are highly specific, e.g., antifungal activity against wheat powdery mildew, but do not affect seed germination or have herbicidal or insecticial activity. Methods and compositions for delivery of these agents against such pathogens, and methods of chemical synthesis of the compounds are disclosed.
    • 显示出重要的抗微生物(抗菌和抗真菌)活性,组合物和递送针对病原体和病原体的方法的取代的烯丙基(烯丙基)苯化合物,以及通常可得的反应物的合成方法。 抗真菌组合物活性成分是一种或多种下式的4,5-取代的2,3-亚烷基二氧基-1-烯烃苯:其中R 1和R 2可以相同或不同,并且选自OH, 和C 1 -C 5烷氧基(-OR)或硫代烷基(-SR)基团。 R3和R4选自H和C1-C5烷基,烯基和炔基,R5选自C3-C7烷基,烯基和炔基。 优选的化合物是4,5-取代-2,3-亚甲二氧基-1-烯丙基苯。 其中R1 = OCH3,R2 = OH,R3和R4 = H,R5 =烯丙基(2',3'丙烯基),化合物可称为甲基假鞭毛虫。 当R 1 = R 2 = OCH 3时,R 3和R 4再次为H,R 5为烯丙基,该化合物可称为伪鞭毛虫。 包括这些化合物的组合物对各种病原体和病原体表现出抗菌活性,例如野油菜黄单胞菌(Xanthomonas campestris spp。) 细菌,针对各种真菌和细菌的抗真菌活性,并且是高度特异性的,例如抗小麦白粉病的抗真菌活性,但不影响种子发芽或具有除草或昆虫活性。 公开了用于递送这些试剂以抵抗这种病原体的方法和组合物,以及化合物的化学合成方法。