title: 3-Substituted indolizine-1-carbonitrile derivatives as phosphatase inhibitors.
abstract: In the course of studies directed toward the discovery of novel scaffolds for medicinal application, we synthesized a series of 3-substituted indolizine-1-carbonitrile derivatives. Some of them displayed activity against MPtpA/MPtpB phosphatases which are involved in infectious diseases. We report here the solid-phase synthesis and antiphosphatase activity of a series of indolizines.
authors.affiliation: Department Chemie, Lehrstuhl II für Organische Chemie, Technische Universität München, Lichtenbergstr. 4, D-85747 Garching, Germany.
authors.forename: Timo
authors.initials: T
authors.lastname: Weide
authors.forename: Lars
authors.initials: L
authors.lastname: Arve
authors.forename: Heino
authors.initials: H
authors.lastname: Prinz
authors.forename: Herbert
authors.initials: H
authors.lastname: Waldmann
authors.forename: Horst
authors.initials: H
authors.lastname: Kessler
mesh_terms: D019342:Acetic Acid / Q000737:chemistry; D000818:Animals; D002244:Carbon / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D004583:Electrons; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D006571:Heterocyclic Compounds; D007211:Indoles / Q000737:chemistry; D007212:Indolizines / Q000737:chemistry*; D020128:Inhibitory Concentration 50; D051379:Mice; D008956:Models, Chemical; D008968:Molecular Conformation; D015394:Molecular Structure; D009169:Mycobacterium tuberculosis / Q000378:metabolism; D009570:Nitriles / Q000737:chemistry*; D010744:Phosphoric Monoester Hydrolases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D017027:Protein Tyrosine Phosphatases / Q000737:chemistry; D011725:Pyridines; D012486:Salmonella typhimurium / Q000378:metabolism; D013329:Structure-Activity Relationship; D015010:Yersinia pestis / Q000378:metabolism
chemical_list: D004791:Enzyme Inhibitors; D006571:Heterocyclic Compounds; D007211:Indoles; D007212:Indolizines; D009570:Nitriles; D011725:Pyridines; C035094:indolizine; D002244:Carbon; D010744:Phosphoric Monoester Hydrolases; D017027:Protein Tyrosine Phosphatases; D019342:Acetic Acid