Synthesis and immunomodulating activity of condensed N-aryl-2-cyano-3-oxo-3-pyrazolyl-propanamides.
A series of condensed N-aryl-2-cyano-3-oxo-3-pyrazolyl-propanamides were synthesized and evaluated for immunomodulating activity following intraperitoneal administration. These new molecules were found to enhance macrophage cytotoxicity and stimulate host mediated antibacterial defences in mice. The compound 3-cyano-3-(1,4-dihydro-1-phenyl-[1]-benzothiopyrano[4,3-c]pyrazol- 3-yl]-3-oxo-N-phenyl-propanamide, chosen for wider pharmacological investigation, proved effective in preventing adjuvant-induced arthritis development in rats.
Doria
G
G
Immunology Line, Farmitalia Carlo Erba (Erbamont Group), Milano, Italy.
Isetta
A M
AM
Ferreccio
R
R
Ferrari
M
M
Fornasiero
M C
MC
Tibolla
M
M
Rossi
M
M
Carlini
O
O
Motta
P
P
Magistrelli
M
M
D000276:Adjuvants, Immunologic / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001169:Arthritis, Experimental / Q000517:prevention & control; D003601:Cytotoxicity Tests, Immunologic; D005260:Female; D008264:Macrophages / Q000187:drug effects; D051379:Mice; D008810:Mice, Inbred C57BL; D009570:Nitriles / Q000138:chemical synthesis* / Q000494:pharmacology; D011552:Pseudomonas Infections / Q000276:immunology / Q000517:prevention & control; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D000276:Adjuvants, Immunologic; D009570:Nitriles; D011720:Pyrazoles; C073243:2-cyano-3-(1,4-dihydro-1-phenyl-(1)-benzothiopyrano(4,3-c)pyrazol-3-yl)-3-oxo-N-phenylpropanamide