cheminform abstract: synthesis and pharmacological evaluation of novel conformationally constrained...

1
2008 Amino acids U 0400 Synthesis and Pharmacological Evaluation of Novel Conformationally Con- strained Homologues of Glutamic Acid. — A series of conformationally constrained homologues of glutamic acid [cf. (V), (IX)] issynthesized via 1,3-dipolar cycloaddition of nitrile oxides derived from (II) with suitable dipolarophiles. The products (12 exam- ples) do not exhibit any affinity for ionotropic glutamate receptors with the exception of racemic compounds (V), which show a moderate affinity for NMDA receptors. — (CONTI, P.; CALIGIURI, A.; PINTO, A.; RODA, G.; TAMBORINI, L.; NIELSEN, B.; MADSEN, U.; FRYDENVANG, K.; COLOMBO, A.; DE MICHELI*, C.; Eur. J. Med. Chem. 42 (2007) 8, 1059-1068; Ist. Chim. Farm. Tossicol., Univ. Milano, I-20131 Milano, Italy; Eng.) — D. Singer 01- 185

Upload: paola-conti

Post on 11-Jun-2016

214 views

Category:

Documents


1 download

TRANSCRIPT

Page 1: ChemInform Abstract: Synthesis and Pharmacological Evaluation of Novel Conformationally Constrained Homologues of Glutamic Acid

2008

Amino acidsU 0400 Synthesis and Pharmacological Evaluation of Novel Conformationally Con-

strained Homologues of Glutamic Acid. — A series of conformationally constrained homologues of glutamic acid [cf. (V), (IX)] issynthesized via 1,3-dipolar cycloaddition of nitrile oxides derived from (II) with suitable dipolarophiles. The products (12 exam-ples) do not exhibit any affinity for ionotropic glutamate receptors with the exception of racemic compounds (V), which show a moderate affinity for NMDA receptors. — (CONTI, P.; CALIGIURI, A.; PINTO, A.; RODA, G.; TAMBORINI, L.; NIELSEN, B.; MADSEN, U.; FRYDENVANG, K.; COLOMBO, A.; DE MICHELI*, C.; Eur. J. Med. Chem. 42 (2007) 8, 1059-1068; Ist. Chim. Farm. Tossicol., Univ. Milano, I-20131 Milano, Italy; Eng.) — D. Singer

01- 185