Synthesis and antimicrobial studies of hydrazone derivatives of 4-[3-(2,4-difluorophenyl)-4-formyl-1H-pyrazol-1-yl]benzoic acid and 4-[3-(3,4-difluorophenyl)-4-formyl-1H-pyrazol-1-yl]benzoic acid

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:28

Article

Zakeyah, A. A.¹  Whitt, J.¹  Duke, C.¹  Gilmore, D. F.²  Meeker, D. G.³  Smeltzer, M. S.³  Alam, M. A.¹ 

[1] Arkansas State Univ, Dept Chem & Phys, Coll Sci & Math, Jonesboro, AR 72467 USA

[2] Arkansas State Univ, Dept Biol Sci, Coll Sci & Math, Jonesboro, AR 72467 USA

[3] Univ Arkansas Med Sci, Coll Med, Dept Microbiol & Immunol, 4301 W Markham St, Little Rock, AR 72205 USA

关键词: Antimicrobial;    Pyrazole;    Hydrazone;    Acinetobacter baumannii;    MRSA;   

DOI  :  10.1016/j.bmcl.2018.07.016

来源: Elsevier

【 摘 要 】

Microbial resistance to antibiotics is an unresolved global concern, which needs urgent and coordinated action. One of the guidelines of the Centers for Disease Control and Preventions (CDC) to combat antibiotic resistance is the development of new antibiotics to treat drug-resistant bacteria. In our effort to find new antibiotics, we report the synthesis and antimicrobial studies of 30 new pyrazole derivatives. These novel molecules have been synthesized by using readily available starting materials and benign reaction conditions. Some of these molecules have shown activity with MIC values as low as 0.78 mu g/mL against four bacterial strains; Staphylococcus aureus, methicillin-resistant S. aureus, Bacillus subtilis, and Acinetobacter baumannii. Furthermore, active molecules are non-toxic to mammalian cell line. [GRAPHICS] .

【 授权许可】

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