Novel ethyl 1,5-disubstituted-1H-pyrazole-3-carboxylates as a new class of antimicrobial agents

作者：Radwan Awwad A^*; Ghorab Mostafa M; Alsaid Mansour S; Alanazi Fares K

来源：Acta Pharmaceutica, 2014, 64(3): 335-344.

DOI：10.2478/acph-2014-0028

• pyrazole-3-carboxylates
• antimicrobial activity

series of pyrazole derivatives 9-22 were designed and synthesized. All the newly synthesized compounds were assayed for their antimicrobial activity against the Gram-positive bacteria Staphyllococcus aureus and Bacillius subtilis and the Gram-negative bacteria Escherichia coli, Pseudomonas aeruginosa, in addition to the fungi organisms, Candida albicans, C. parapsilosis and C. tropicalis. Ethyl 5-(2,5-dimethyl-thiophen-3-yl)-1-pheny1-1H-pyrazole-3-carboxylate (21) (MICE.coli = 0.038 mu mol mL(-1), MICP.aerug. = 0.067 mu mol mL(-1)) is nearly as active as ampicillin (MIC = 0.033 and 0.067 mu mol mL(-1)), respectively. Ethyl5-(4-bromo-2-chlorophenyl)1-phenyl-1H-pyrazole-3-carboxylate (16) (MIC = 0.015 mu mol mL(-1)) is more active than fluconazole (0.020 mu mol mL(-1) as a reference drug against C. parapsilosis.

• 出版日期2014-9