Design, synthesis, and biological evaluation of a scaffold for iGluR ligands based on the structure of (-)-kaitocephalin.
The design and synthesis of four pyrrolidine scaffolds that are structurally related to the known ionotropic glutamate receptor antagonist, (-)-kaitocephalin, is described. Additionally, preliminary results of the biological evaluation of these compounds are disclosed.
Vaswani
Rishi G
RG
Department of Chemistry, University of California at Irvine, Irvine, CA 92697, USA.
Limon
Agenor
A
Reyes-Ruiz
Jorge Mauricio
JM
Miledi
Ricardo
R
Chamberlin
A Richard
AR
D015195:Drug Design; D018690:Excitatory Amino Acid Agonists / Q000737:chemistry; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry; D006801:Humans; D008024:Ligands; D011758:Pyrroles / Q000737:chemistry*; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D017470:Receptors, Glutamate / Q000187:drug effects*; D013329:Structure-Activity Relationship
D018690:Excitatory Amino Acid Agonists; D018691:Excitatory Amino Acid Antagonists; D008024:Ligands; D011758:Pyrroles; D011759:Pyrrolidines; D017470:Receptors, Glutamate; C442421:kaitocephalin