Original scientific paper

https://doi.org/10.2478/acph-2014-0028

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

AWWAD A. RADWAN ; Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia; Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut-71527, Egypt
MOSTAFA M. GHORAB ; Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, P.O. 2457, Riyadh 11451, Saudi Arabia; Department of Drug Radiation Research, National Centre For Radiation Research and Technology, Atomic Energy Authority, P.O. Box 29, Nasr
MANSOUR S. ALSAID ; Department of Pharmacognosy, College of Pharmacy, King Saud University, Riyadh, P.O. 2457, Riyadh 11451, Saudi Arabia
FARES K. ALANAZI ; Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia

Abstract

A 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-dimethylthiophen-3-yl)-1-phenyl-1H-pyrazole-3-carboxylate (21) (MICE.coli =0.038 µmol mL–1, MICP. aerug = 0.067 µmol mL–1) is nearly as active as ampicillin (MIC = 0.033 and 0.067 µmol mL–1, respectively). Ethyl 5-(4-bromo-2-chlorophenyl)-1-phenyl-1H-pyrazole-3-carboxylate (16) (MIC = 0.015 µmol mL–1) is more active than fluconazole (0.020 µmol mL–1) as a reference drug against C. parapsilosis.

Keywords

pyrazole-3-carboxylates; antimicrobial screening

Hrčak ID:

121072

URI

https://hrcak.srce.hr/121072

Publication date:

30.9.2014.

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