Design, synthesis and structure of novel G-2 melamine-based dendrimers incorporating 4-(-octyloxy)aniline as a peripheral unit.

4-(-Octyloxy)aniline is a known component in the elaboration of organic materials with mesogenic properties such as -substituted Schiff bases, perylene bisimide assemblies with a number of 2-amino-4,6-bis[4-(-octyloxy)phenylamino]--triazines, amphiphilic azobenzene-containing linear-dendritic block copolymers and G-0 monomeric or dimeric dendritic liquid crystals with photochromic azobenzene mesogens. The present ab initio study explores a previously unknown use of 4-(-octyloxy)aniline in the synthesis, structure and supramolecular behaviour of new dendritic melamines. Starting from 4-(-octyloxy)aniline, seven G-2 melamine-based dendrimers were obtained in 29-79% overall yields.

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).