<abstract xmlns="http://www.w3.org/1999/xhtml"> A series of pyrazole derivatives 9-22 were designed and synthesized. All the newly synthesized compounds were assayed for their antimicrobial activity against the Grampositive 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.</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 Grampositive 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.

Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents

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

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 City, Cairo, Egypt

Department of Pharmacognosy College of Pharmacy King Saud University, Riyadh P.O. 2457, Riyadh 11451, Saudi Arabia

Department of Pharmaceutics College of Pharmacy King Saud University, P.O. Box 2457 Riyadh 11451, Saudi Arabia

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

A series of pyrazole derivatives 9-22 were designed and synthesized. All the newly synthesized compounds were assayed for their antimicrobial activity against...

Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents

Publicado en línea: 08 oct 2014

Páginas: 335 - 344

Aceptado: 15 may 2014

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

Palabras clave
pyrazole-3-carboxylates, antimicrobial activity

© by Awwad A. Radwan

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents

Publicado en línea: 08 oct 2014

Páginas: 335 - 344

Aceptado: 15 may 2014

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

Palabras clavepyrazole-3-carboxylates, antimicrobial activity

© by Awwad A. Radwan

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Palabras clave
pyrazole-3-carboxylates, antimicrobial activity