title: Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent.
abstract: A series of novel pyrazole-5-carboxylate containing N-triazole derivatives 3,4; different heterocyclic amines 7a-b and 10a-b; pyrazolo[4,3-d]pyrimidine containing sulfa drugs 14a,b; and oxypyrazolo[4,3-d]pyrimidine derivatives 17, 19, 21 has been synthesized. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. All compounds have been screened for their in vitro antimicrobial activity against three gram-positive and gram-negative bacteria as well as three fungi. The results revealed that compounds 14b and 17 had more potent antibacterial activity against all bacterial strains than reference drug Cefotaxime. Moreover compounds 4, 7b, and 12b showed excellent antifungal activities against Aspergillus niger and Candida albicans in low inhibitory concentrations but slightly less than the reference drug miconazole against Aspergillus flavus.
authors: Department of Chemistry, College of Science, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), P.O. Box: 90950 Riyadh 11623, Saudi Arabia. dr.hendhafez@yahoo.com.|Photochemistry Department, Heterocyclic & Nucleosides Unit, National Research Centre, Dokki, Giza 12622, Egypt. dr.hendhafez@yahoo.com.
authors: Hend N
authors: HN
authors: Hafez
authors: Department of Chemistry, College of Science, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), P.O. Box: 90950 Riyadh 11623, Saudi Arabia. profelgazzar@yahoo.com.|Photochemistry Department, Heterocyclic & Nucleosides Unit, National Research Centre, Dokki, Giza 12622, Egypt. profelgazzar@yahoo.com.
authors: Abdel-Rhman B A
authors: AR
authors: El-Gazzar
mesh_terms: D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001230:Aspergillus / Q000254:growth & development*; D002176:Candida albicans / Q000254:growth & development*; D004353:Drug Evaluation, Preclinical; D006090:Gram-Negative Bacteria / Q000254:growth & development*; D006094:Gram-Positive Bacteria / Q000254:growth & development*; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000890:Anti-Infective Agents; D011720:Pyrazoles; D011725:Pyridines; C118531:pyrazolopyridine
keywords: N-substituted benzenesulfonamides; antimicrobial agent; pyrazole derivatives; pyrazolo[4,3-d]pyrimidine