Synthesis and biological evaluation of novel phthalazinone derivatives as topically active phosphodiesterase 4 inhibitors

Design, Synthesis, and Pharmacological Screening of Pyridazinone Hybrids as Anticonvulsant Agents

“…The synthetic route of synthesized derivatives is outlined in Scheme . Subsequently, these 6‐substitued‐4,5‐dihydropyridazine‐3(2 H )‐ones on treatment with ethyl bromoacetate in the presence of potassium carbonate in dry acetone produce ethyl 2‐(6‐oxo‐3‐aryl‐5,6‐dihyropyidazin‐1(4 H )‐yl acetate ( SS1C – SS19C ) . Finally, the synthesized ( SS1C – SS19C ) compounds were cyclized on treatment with ortho phenylene diamine in acidic condition to yield the final product ( SS‐1F to SS‐19F ).…”

Phthalazin-1(2H)-one as a remarkable scaffold in drug discovery

“…More recently, with the aim to develop topically active PDE4Is and in order to minimize gastrointestinal side effects associated with oral administration of classical PDE4Is, novel cis-tetrahydro and hexahydrophthalazinone related compounds showing substitutents with increased lipophilicity at N2 were synthesized and biologically evaluated as both PDE4 and TNF-α inhibitors [91]. SAR studies confirmed that there is a strong dependence between the substituent at N2 of the phthalazinone system and these inhibitory activities.…”

Ninhydrin in synthesis of heterocyclic compounds

“…Phthalazinones are an important class of heterocycles with diverse biological activities like vasorelaxant activity, 437 phosphodiesterase inhibitors, 438 inhibitor of Poly(ADP-ribose), 439 or protein kinase inhibitors. 440 The synthesis of biologically important phthalazinones was reported by Pramanik and co-workers.…”