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.
Copyright © 2012 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
MeSH terms
-
Amides / chemical synthesis
-
Amides / chemistry
-
Amides / pharmacology*
-
Anti-Bacterial Agents / chemical synthesis
-
Anti-Bacterial Agents / chemistry
-
Anti-Bacterial Agents / pharmacology*
-
Antifungal Agents / chemical synthesis
-
Antifungal Agents / chemistry
-
Antifungal Agents / pharmacology
-
Antitubercular Agents / chemical synthesis
-
Antitubercular Agents / chemistry
-
Antitubercular Agents / pharmacology
-
Drug Design
-
Magnetic Resonance Spectroscopy
-
Microbial Sensitivity Tests
-
Spectrophotometry, Infrared
-
Structure-Activity Relationship
-
Sulfonamides / chemical synthesis
-
Sulfonamides / chemistry
-
Sulfonamides / pharmacology*
Substances
-
Amides
-
Anti-Bacterial Agents
-
Antifungal Agents
-
Antitubercular Agents
-
Sulfonamides