title: Isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors: SAR and pharmacokinetic evaluation.
abstract: The synthesis and structure-activity relationship studies of isothiazole and isoxazole fused pyrimidones as PDE7 inhibitors are discussed. The pharmacokinetic profile of 10 and 21 with adequate CNS penetration, required for in vivo Parkinson's disease models, are disclosed.
authors.affiliation: Glenmark Pharmaceuticals Limited, Navi Mumbai, Maharashtra 400 709, India.
authors.forename: Abhisek
authors.initials: A
authors.lastname: Banerjee
authors.forename: Pravin S
authors.initials: PS
authors.lastname: Yadav
authors.forename: Malini
authors.initials: M
authors.lastname: Bajpai
authors.forename: Ramachandra Rao
authors.initials: RR
authors.lastname: Sangana
authors.forename: Srinivas
authors.initials: S
authors.lastname: Gullapalli
authors.forename: Girish S
authors.initials: GS
authors.lastname: Gudi
authors.forename: Laxmikant A
authors.initials: LA
authors.lastname: Gharat
mesh_terms: D002490:Central Nervous System; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7 / Q000037:antagonists & inhibitors*; D006801:Humans; D007555:Isoxazoles / Q000737:chemistry; D010300:Parkinson Disease / Q000188:drug therapy; D010599:Pharmacokinetics; D010726:Phosphodiesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D011744:Pyrimidinones / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry
chemical_list: D007555:Isoxazoles; D010726:Phosphodiesterase Inhibitors; D011744:Pyrimidinones; D013844:Thiazoles; D054708:Cyclic Nucleotide Phosphodiesterases, Type 7