Parallel microwave-assisted library of imidazothiazol-3-ones and imidazothiazin-4-ones.

A methodology for the generation of a microwave-assisted parallel library and its conversion into a second library is described. A 24-membered library of substituted 4(5)-sulfanyl-1H-imidazoles was generated and subsequently converted into a second library of bicyclic imidazo[5,1-b]thiazol-3-ones and imidazo[5,1-b]thiazin-4-ones. The first library was generated using a three-component reaction and transformed into a daughter library with a polymer-supported coupling agent.

Synthesis and biological evaluation of halogenated naphthyridone carboxamides as potential ligands for in vivo imaging studies of substance P receptors.

With the aim of developing new radioligands for in vivo studies of substance P receptors using positron emission tomography or single photon emission computed tomography, 2- and 3-halo naphthyridone-6-carboxamide derivatives were synthesized. Their affinities toward the target receptors were evaluated on CHO cells and compared to the unsubstituted analogue EP 00652218 (IC(50) = 100 nM +/- 20). The IC(50) value was not altered in the case of 2-chloro compound 1 (IC(50) = 100 nM +/- 15) and only slightly reduced for the 2-fluoro and -iodo analogues 6 and 8 (IC(50) = 500 nM +/- 80).