title: Calmodulin inhibitory activity of the malbrancheamides and various analogs.
abstract: The preparation and biological activity of various structural analogs of the malbrancheamides are disclosed. The impact of indole chlorination, C-12a relative stereochemistry, and bicyclo[2.2.2]diazaoctane core oxidation state on the ability of these analogs to inhibit calmodulin dependent phosphodiesterase (PDE1) was studied, and a number of potent compounds were identified.
authors.affiliation: Department of Chemistry, Colorado State University, 1301 Center Avenue, Fort Collins, CO 80523-1872, USA.
authors.forename: Kenneth A
authors.initials: KA
authors.lastname: Miller
authors.forename: Mario
authors.initials: M
authors.lastname: Figueroa
authors.forename: Meriah W N
authors.initials: MW
authors.lastname: Valente
authors.forename: Thomas J
authors.initials: TJ
authors.lastname: Greshock
authors.forename: Rachel
authors.initials: R
authors.lastname: Mata
authors.forename: Robert M
authors.initials: RM
authors.lastname: Williams
mesh_terms: D000470:Alkaloids / Q000737:chemistry; D002147:Calmodulin / Q000037:antagonists & inhibitors* / Q000737:chemistry*; D002713:Chlorine / Q000737:chemistry; D002746:Chlorpromazine / Q000737:chemistry; D054677:Cyclic Nucleotide Phosphodiesterases, Type 1 / Q000737:chemistry; D015195:Drug Design; D006801:Humans; D026121:Indole Alkaloids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007211:Indoles / Q000737:chemistry; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D010100:Oxygen / Q000737:chemistry; D013237:Stereoisomerism
chemical_list: D000470:Alkaloids; D002147:Calmodulin; D026121:Indole Alkaloids; D007211:Indoles; C529354:malbrancheamide; D002713:Chlorine; D054677:Cyclic Nucleotide Phosphodiesterases, Type 1; D010100:Oxygen; D002746:Chlorpromazine