Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents
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 aerugino...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Sciendo
2014-09-01
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| Series: | Acta Pharmaceutica |
| Subjects: | |
| Online Access: | https://doi.org/10.2478/acph-2014-0028 |
| _version_ | 1826844604618506240 |
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| author | Radwan Awwad A. Ghorab Mostafa M. Alsaid Mansour S. Alanazi Fares K. |
| author_facet | Radwan Awwad A. Ghorab Mostafa M. Alsaid Mansour S. Alanazi Fares K. |
| author_sort | Radwan Awwad A. |
| collection | DOAJ |
| description | 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. |
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| format | Article |
| id | doaj.art-c84f57f0e1384666888568f12a1f3d87 |
| institution | Directory Open Access Journal |
| issn | 1846-9558 |
| language | English |
| last_indexed | 2025-02-16T14:10:50Z |
| publishDate | 2014-09-01 |
| publisher | Sciendo |
| record_format | Article |
| series | Acta Pharmaceutica |
| spelling | doaj.art-c84f57f0e1384666888568f12a1f3d872025-02-02T03:11:11ZengSciendoActa Pharmaceutica1846-95582014-09-0164333534410.2478/acph-2014-0028acph-2014-0028Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial AgentsRadwan Awwad A.0Ghorab Mostafa M.1Alsaid Mansour S.2Alanazi Fares K.3Department 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, EgyptDepartment 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, EgyptDepartment of Pharmacognosy College of Pharmacy King Saud University, Riyadh P.O. 2457, Riyadh 11451, Saudi ArabiaDepartment of Pharmaceutics College of Pharmacy King Saud University, P.O. Box 2457 Riyadh 11451, Saudi ArabiaA 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.https://doi.org/10.2478/acph-2014-0028pyrazole-3-carboxylatesantimicrobial activity |
| spellingShingle | Radwan Awwad A. Ghorab Mostafa M. Alsaid Mansour S. Alanazi Fares K. Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents Acta Pharmaceutica pyrazole-3-carboxylates antimicrobial activity |
| title | Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents |
| title_full | Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents |
| title_fullStr | Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents |
| title_full_unstemmed | Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents |
| title_short | Novel Ethyl 1,5-Disubstituted-1H-Pyrazole-3-Carboxylates as a New Class of Antimicrobial Agents |
| title_sort | novel ethyl 1 5 disubstituted 1h pyrazole 3 carboxylates as a new class of antimicrobial agents |
| topic | pyrazole-3-carboxylates antimicrobial activity |
| url | https://doi.org/10.2478/acph-2014-0028 |
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