Synthesis And Structure-activity Relationships Of Antibacterial Activity Imidazole Amide Derivatives

Benzimidazole fungicide is the history of a suction-type fungicide containingbenzimidazole ring commercialization. The series fungicide selective, broad spectrumantimicrobial, vinca long, safe for mammals Benzimidazole ring is an importantpharmacophore, which derivative has excellent antibacterial activity, and anti-virus,anti-hypertensive, anti-parasitic, anti-cancer, anti-inflammatory, analgesic, enzyme inhibitors,and agonists other aspects also play a good role.Select this article4-methoxy-2–nitroaniline、4-nitro-o-phenylenediamine by a series ofchemical reactions for the synthesis of raw materials and241-isopropyl-3-acyl-5-methoxybenzothiazol imidazolidinone derivatives and20times1-isopropenyl-3-acyl-5(6)-nitro-benzimidazole derivative. All compounds using filter papermethod, inhibit mycelial growth inhibition of spore germination method and determination ofits biological activity, and analyze its structure-activity relationships.The results showed that all the tested compounds against Botrytis cinerea in varyingdegrees of inhibition:2-ethyl butyrate derivatives (A9) and2-methyl-benzoic acid derivative(A17) antibacterial activity particularly prominent, the rate of spore germination, respectively95.93%and93.35%;2-chloro-benzoic acid derivative (A20),4-chloro-benzoic acid derivative(A22) and4-fluoro-benzoic acid derivative (A23) spore germination rate on the performance ofBotrytis cinerea spore germination medium inhibited its inhibition rates were81.01%,84.30%and75.32%; among chloride5-nitrobenzoimidazole derivatives (B01) antibacterial activityespecially, its inhibition rate of mycelium and spore germination inhibition rates were85.7%and32.5%; acrylic acid derivatives (B03, B13), methacrylic acid derivatives (B04, B14) mycelialgrowth inhibition rate reached60%, respectively,65.7%,60.0%,65.7%,71.2%.All compounds for structure-activity relationships analysis, In inhibiting fungal activityareas: the type and location of the substituents A series of related antimicrobial activity ofaromatic acids and aromatic acid derivatives on the benzene ring, for electronic effect group(-CH3) in the ortho aromatic acids, or electron-withdrawing effect groups (-Cl,-F, and-NO2)in the ortho aromatic acids and antibacterial activity of bits of favorable; B series antibacterialactivity of C-chain substituents on the length of the shorter C-chain, the effect is more good.