Isoxazolo[3,4-d]pyridazinones and analogues as Leishmania mexicana PDE inhibitors.
A series of isoxazolopyridazinones and analogues has been prepared and evaluated as Leishmania mexicana phosphodiesterase (PDE) inhibitors. Some of the synthesized compounds showed a moderate PDE inhibitory activity at 100 microM and preliminary structure-activity relationships were discussed.
Dal
Piaz Vittorio
PV
Dipartimento di Scienze Farmaceutiche, Florence, Italy. vittorio.dalpiaz@unifi.it
Rascón
A
A
Dubra
M E
ME
Giovannoni
M P
MP
Vergelli
C
C
Castellana
M C
MC
D000818:Animals; D006868:Hydrolysis; D007894:Leishmania mexicana / Q000187:drug effects* / Q000201:enzymology*; D009682:Magnetic Resonance Spectroscopy; D015394:Molecular Structure; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D010727:Phosphoric Diester Hydrolases / Q000378:metabolism*; D011724:Pyridazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013379:Substrate Specificity
D010726:Phosphodiesterase Inhibitors; D011724:Pyridazines; D010727:Phosphoric Diester Hydrolases