title: Structure-activity relationship and docking studies of thiazolidinedione-type compounds with monoamine oxidase B.
abstract: The neuroprotective activity of pioglitazone and rosiglitazone in the MPTP parkinsonian mouse prompted us to evaluate a set of thiazolidinedione (TZD) type compounds for monoamine oxidase A and B inhibition activity. These compounds were able to inhibit MAO-B over several log units of magnitude (82 nM to 600 μM). Initial structure-activity relationship studies identified key areas to modify the aromatic substituted TZD compounds. Primarily, substitutions on the aromatic group and the TZD nitrogen were key areas where activity was enhanced within this group of compounds.
authors: Department of Pharmaceutical Sciences, Northeastern Ohio Universities Colleges of Medicine and Pharmacy, 4209 State Route 44, Rootstown, OH 44272, USA.
authors: Richard T
authors: RT
authors: Carroll
authors: Dean E
authors: DE
authors: Dluzen
authors: Hilary
authors: H
authors: Stinnett
authors: Prabha S
authors: PS
authors: Awale
authors: Max O
authors: MO
authors: Funk
authors: Werner J
authors: WJ
authors: Geldenhuys
mesh_terms: D000818:Animals; D006801:Humans; D008297:Male; D051379:Mice; D008810:Mice, Inbred C57BL; D008958:Models, Molecular; D015394:Molecular Structure; D008995:Monoamine Oxidase / Q000378:metabolism*; D008996:Monoamine Oxidase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D045162:Thiazolidinediones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D008996:Monoamine Oxidase Inhibitors; D045162:Thiazolidinediones; C089946:2,4-thiazolidinedione; D008995:Monoamine Oxidase