title: Synthesis, antibacterial activity and structure-activity relationships of N-substituted 4-diazo-pyrazole-5-carboxamides. 2.
abstract: A series of 4-diazopyrazole-5-carboxamides 1 d-n has been synthesized and their antibacterial activity against a number of Gram-negative and Gram-positive strains has been tested. Some of the compounds resulted quite active and the whole set allowed to further study the SAR of the class. Substituents in position 5 affect Gram-negative and Gram-positive activities via bulk and electronic properties respectively; position 3 mostly affects the Gram-negative activity, while the presence of the charged diazo group in position 4 is crucial for both antibacterial activities.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Universitá di Bologna.
authors.forename: P G
authors.initials: PG
authors.lastname: Baraldi
authors.forename: B
authors.initials: B
authors.lastname: Cacciari
authors.forename: A
authors.initials: A
authors.lastname: Leoni
authors.forename: M
authors.initials: M
authors.lastname: Recanatini
authors.forename: M
authors.initials: M
authors.lastname: Roberti
authors.forename: M
authors.initials: M
authors.lastname: Rossi
authors.forename: S
authors.initials: S
authors.lastname: Manfredini
authors.forename: V
authors.initials: V
authors.lastname: Periotto
authors.forename: D
authors.initials: D
authors.lastname: Simoni
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects; D003979:Diazonium Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000900:Anti-Bacterial Agents; D003979:Diazonium Compounds; D011720:Pyrazoles