title: Indolin-2-one p38α inhibitors II: Lead optimisation.
abstract: Optimisation of a series of indolin-2-one p38α inhibitors was achieved via both blocking of a potential metabolic 'hot spot' and by increasing overall polarity of the lead series leading to non-cytotoxic compounds which showed improved oral bioavailabilities in the rat.
authors.affiliation: Almirall Research Center, Almirall Laboratories, Ctra. Laureà Miró 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain. paul.eastwood@almirall.com
authors.forename: Paul
authors.initials: P
authors.lastname: Eastwood
authors.forename: Jacob
authors.initials: J
authors.lastname: González
authors.forename: Elena
authors.initials: E
authors.lastname: Gómez
authors.forename: Francisco
authors.initials: F
authors.lastname: Caturla
authors.forename: Cristina
authors.initials: C
authors.lastname: Balagué
authors.forename: Adelina
authors.initials: A
authors.lastname: Orellana
authors.forename: María
authors.initials: M
authors.lastname: Domínguez
mesh_terms: D000818:Animals; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D048308:Mitogen-Activated Protein Kinase 14 / Q000032:analysis* / Q000378:metabolism; D015394:Molecular Structure; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; C456900:indolin-2-one; D048308:Mitogen-Activated Protein Kinase 14