title: Synthesis and antimicrobial activity of novel heterocyclic sulfamoyl-phenyl-carboximidamides derived from clinically applied sulfonamides.
abstract: A series of novel heterocyclic sulfamoyl-phenyl-carboximidamides were synthesized in satisfactory yields via condensation of clinically applied sulfonamides with heterocyclic methyl carbimidates. New structures were confirmed by IR and NMR spectra as well as elemental analyses. All the compounds were screened for their antibacterial, antifungal, and tuberculostatic activities. Preliminary results indicated that some target compounds exhibited promising antibacterial potency. Especially, N-[4-(thiazol-2-sulfamoyl)phenyl]pyrazine-2-carboximidamide (16) was found to be as potent as clinically applied sulfamethoxypyridazine.
authors.affiliation: Department of Organic Chemistry, Medical University of Gdańsk, Poland. kgobis@gumed.edu.pl
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Gobis
authors.forename: Henryk
authors.initials: H
authors.lastname: Foks
authors.forename: Katarzyna
authors.initials: K
authors.lastname: Wiśniewska
authors.forename: Maria
authors.initials: M
authors.lastname: Dąbrowska-Szponar
authors.forename: Ewa
authors.initials: E
authors.lastname: Augustynowicz-Kopeć
authors.forename: Agnieszka
authors.initials: A
authors.lastname: Napiórkowska
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000935:Antifungal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D009682:Magnetic Resonance Spectroscopy; D008826:Microbial Sensitivity Tests; D013055:Spectrophotometry, Infrared; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D000577:Amides; D000900:Anti-Bacterial Agents; D000935:Antifungal Agents; D000995:Antitubercular Agents; D013449:Sulfonamides