Robert M. Tynebor

Synthesis and biological activity of pyridopyridazin-6-one p38 MAP kinase inhibitors. Part 1.

This manuscript concludes the Structure Activity Relationship (SAR) on the pyridazinone scaffold and identifies a compound with subnanomolar p38α activity and 24h coverage in the rat arthritis efficacy model.

Synthesis and biological activity of 2H-quinolizin-2-one based p38alpha MAP kinase inhibitors.

The development and synthesis of potent p38alpha MAP kinase inhibitors containing a 2H-quinolizin-2-one platform is described. Evolution of the 2H-quinolizin-2-one series from an early lead to solving off target activity and pharmacokinetic issues is also discussed.

Novel Method of Synthesizing Various Five Membered Heterocycles from an Aryl Tribromomethyl Group

Abstract Synthesis of five membered heterocycles from an aryl tribromomethyl functional group is discussed. Exposing a tribromomethyl group to subsequent nucleophilic attacks by a 1,2-di-nucleophilic species promotes the cyclization of five membered heterocycles. Such heterocycles as oxadiazoles, thiadiazole, benzimidazole, benzothioazole, and benzoxazole were synthesized in moderate to good yields. Supplemental materials are available for this article. Go to the publishers online edition of Synthetic Communications® to view the free supplemental file. GRAPHICAL ABSTRACT

Synthesis and biological activity of 2H-quinolizin-2-one based p38α MAP kinase inhibitors

The development and synthesis of potent p38alpha MAP kinase inhibitors containing a 2H-quinolizin-2-one platform is described. Evolution of the 2H-quinolizin-2-one series from an early lead to solving off target activity and pharmacokinetic issues is also discussed.

Synthesis and biological activity of 2 H -quinolizin-2-one based p38α MAP kinase inhibitors

The development and synthesis of potent p38alpha MAP kinase inhibitors containing a 2H-quinolizin-2-one platform is described. Evolution of the 2H-quinolizin-2-one series from an early lead to solving off target activity and pharmacokinetic issues is also discussed.