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Synthesis, antibacterial activity and structure-activity relationships of N-substituted 4-diazo-pyrazole-5-carboxamides. 2. 1991
P G Baraldi, and
B Cacciari, and
A Leoni, and
M Recanatini, and
M Roberti, and
M Rossi, and
S Manfredini, and
V Periotto, and
D Simoni
Dipartimento di Scienze Farmaceutiche, Universitá di Bologna.
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.
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