title: Novel ethyl 1,5-disubstituted-1H-pyrazole-3-carboxylates as a new class of antimicrobial agents.
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) (MIC(E.coli) = 0.038 μmol mL⁻¹, MIC(P. 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.
authors.forename: Awwad A
authors.initials: AA
authors.lastname: Radwan
authors.forename: Mostafa M
authors.initials: MM
authors.lastname: Ghorab
authors.forename: Mansour S
authors.initials: MS
authors.lastname: Alsaid
authors.forename: Fares K
authors.initials: FK
authors.lastname: Alanazi
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D002175:Candida / Q000187:drug effects / Q000254:growth & development; D002264:Carboxylic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D015195:Drug Design; D015725:Fluconazole / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects / Q000254:growth & development; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D002264:Carboxylic Acids; D011720:Pyrazoles; D015725:Fluconazole