The title compound, C(11)H(22)NO(2) (+)·I(-), is a chiral mol-ecule with five stereogenic centres. The absolute configuration was assigned from the synthesis and confirmed by the structure determination. The central six-membered ring of the indolizine system adopts a chair conformation, with two atoms displaced by -0.690 (2) and 0.550 (2) Å from the plane of the other four atoms. The conformati...

We report a series of inhibitors of secreted phospholipases A2 (sPLA2s) based on substituted indoles, 6,7-benzoindoles, and indolizines derived from LY315920, a well-known indole-based sPLA2 inhibitor. Using the human group X sPLA2 crystal structure, we prepared a highly potent and selective indole-based inhibitor of this enzyme. Also, we report human and mouse group IIA and IIE specific inhibi...

The transition-metal-catalyzed denitrogenative transannulation of pyridotriazoles represents an efficient method for the synthesis of fused nitrogen-containing heterocycles. This method is based on the ability of pyridotriazole to exist in an equilibrium with diazo-form A, which can be trapped with Rh(II) to form the reactive pyridyl carbene intermediate B, capable of reacting with terminal alk...

There are two independent mol-ecules in the asymmetric unit of the title compound, C21H21N5O2. In each mol-ecule, the indolizine ring system is essentially planar, with r.m.s. deviations of 0.030 and 0.028 Å. The dihedral angles between the indolizine ring system and the pyrazole rings are 54.7 (3) and 8.6 (3)° in one mol-ecule and 54.4 (3) and 6.6 (3)° in the other. In the crystal, weak C-H⋯O ...

Short overview is given of the author’s group activities over the last decade in the research, educational and other projects related to combinatorial chemistry. The discovery of novel reactions and classes of heterocyclic scaffolds (oxazoles, indolizines, and imidazoles) led to new libraries, for which different types of biological activity (antimicrobial, adrenergic, anxiolytic, and anti-prot...

Design and synthesis of a new series of ethyl 7-methoxy-2-substituted-3-(substituted benzoyl) indolizine-1-carboxylates 2a-i was achieved and screened for their in vitro inhibitory activity against COX-2 enzyme. Compound 2a and 2c emerged as promising COX-2 enzyme inhibitor with IC50 of 6.56 and 6.94 μM respectively from the synthesized series when compared to Celecoxib and Indomethacin as sele...