title: Pyrazoline based MAO inhibitors: synthesis, biological evaluation and SAR studies.
abstract: Twenty-two pyrazoline derivatives were synthesized and tested for their human MAO (hMAO) inhibitory activity. Twelve molecules with unsubstituted ring A and substituted ring C (5-16) were found to be potent inhibitors of hMAO-A isoform with SI(MAO-A) in the order 10(3) and 10(4). Ten molecules with unsubstituted ring A and without ring C (21-30), in which eight molecules (21, 23-26, and 28-30) were selective for hMAO-A, one for hMAO-B (22) and the other one non-selective (27). Presence of ring C increases potency as well as SI towards hMAO-A; however its absence decreases both potency and SI towards hMAO-A and hMAO-B.
authors.affiliation: Department of Pharmaceutical Sciences, Birla Institute of Technology, Mesra, Ranchi 835215, Jharkhand, India.
authors.forename: Monika
authors.initials: M
authors.lastname: Jagrat
authors.forename: Jagannath
authors.initials: J
authors.lastname: Behera
authors.forename: Samiye
authors.initials: S
authors.lastname: Yabanoglu
authors.forename: Ayse
authors.initials: A
authors.lastname: Ercan
authors.forename: Gulberk
authors.initials: G
authors.lastname: Ucar
authors.forename: Barij Nayan
authors.initials: BN
authors.lastname: Sinha
authors.forename: Vadivelan
authors.initials: V
authors.lastname: Sankaran
authors.forename: Arijit
authors.initials: A
authors.lastname: Basu
authors.forename: Venkatesan
authors.initials: V
authors.lastname: Jayaprakash
mesh_terms: D001665:Binding Sites; D003198:Computer Simulation; D006801:Humans; D008995:Monoamine Oxidase / Q000737:chemistry / Q000378:metabolism; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000378:metabolism; D017434:Protein Structure, Tertiary; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D008996:Monoamine Oxidase Inhibitors; D020033:Protein Isoforms; D011720:Pyrazoles; D008995:Monoamine Oxidase