Article

Indolin-2-one p38α inhibitors II: Lead optimisation.

Almirall Research Center, Almirall Laboratories, Ctra. Laureà Miró 408, E-08980 St. Feliu de Llobregat, Barcelona, Spain.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 09/2011; 21(18):5270-3. DOI:10.1016/j.bmcl.2011.07.033 pp.5270-3
Source: PubMed

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.

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Keywords

non-cytotoxic compounds
 
Optimisation
 
potential metabolic 'hot spot'