α-substituted quisqualic acid analogs: New metabotropic glutamate receptor group II selective antagonists

…, D Steensma, M Varasi, S Pshenichkin, E Surina…

Index: Kozikowski, Alan P.; Steensma, Darryl; Varasi, Mario; Pshenichkin, Sergey; Surina, Elena; Wroblewski, Jarda T. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 5 p. 447 - 452

Full Text: HTML

Citation Number: 11

Abstract

Syntheses of both the α-methyl and benzyl analogs of quisqualic acid are described. Testing of these compounds for their activity at excitatory amino acid receptors revealed a striking change in activity in comparison to quisqualic acid. This structural modification results in the loss of quisqualate's potent agonist action at both non-NMDA ionotropic glutamate receptors as well as at group I mGluRs, while allowing these analogs to acquire antagonist ...

Related Articles:

Synthesis of an immunomodulator (+)-conagenin and its analogs

[Yakura, Takayuki; Yoshimoto, Yuya; Ishida, Chisaki; Mabuchi, Shunsuke Tetrahedron, 2007 , vol. 63, # 21 p. 4429 - 4438]

Synthesis, radiolabeling, and biological evaluation of (R)-and (S)-2-amino-3-[18F] fluoro-2-methylpropanoic acid (FAMP) and (R)-and (S)-3-[18F] fluoro-2-methyl-2-N-( …

[Yu, Weiping; McConathy, Jonathan; Olson, Jeffrey; Camp, Vernon M.; Goodman, Mark M. Journal of Medicinal Chemistry, 2007 , vol. 50, # 26 p. 6718 - 6721]

Synthesis of an immunomodulator (+)-conagenin and its analogs

[Yakura, Takayuki; Yoshimoto, Yuya; Ishida, Chisaki; Mabuchi, Shunsuke Tetrahedron, 2007 , vol. 63, # 21 p. 4429 - 4438]

Enantioselective synthesis of (S)-and (R)-α-methylserines: application to the synthesis of (S)-and (R)-N-Boc-N, O-isopropylidene-α-methylserinals

[Avenoza, Alberto; Cativiela, Carlos; Corzana, Francisco; Peregrina, Jesus M.; Sucunza, David; Zurbano, Maria M. Tetrahedron Asymmetry, 2001 , vol. 12, # 6 p. 949 - 957]

Enantioselective synthesis of (S)-and (R)-α-methylserines: application to the synthesis of (S)-and (R)-N-Boc-N, O-isopropylidene-α-methylserinals

[Avenoza, Alberto; Cativiela, Carlos; Corzana, Francisco; Peregrina, Jesus M.; Sucunza, David; Zurbano, Maria M. Tetrahedron Asymmetry, 2001 , vol. 12, # 6 p. 949 - 957]

More Articles...