2,4-Dicarboxy-pyrroles as selective non-competitive mGluR1 antagonists: an exploration of the role of the pyrrolic scaffold.
Following the disclosure of 3-(1,2,2-trimethylpropyl) 4-[3,5-dimethyl-2-propyloxycarbonyl]pyrrolecarboxylate as a potent and selective mGluR1 non-competitive antagonist, the role and the importance of the pyrrole template were investigated. Different aromatic moieties were investigated as possible bio-isosteric replacement of the original scaffold and some of them were shown to be partially able to mimic the properties of the original pyrrole ring.
D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001555:Benzene Derivatives / Q000737:chemistry / Q000494:pharmacology; D001667:Binding, Competitive / Q000187:drug effects; D016466:CHO Cells; D006224:Cricetinae; D004952:Esters / Q000138:chemical synthesis / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D051379:Mice; D009619:Nociceptors / Q000187:drug effects; D010147:Pain Measurement; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D018094:Receptors, Metabotropic Glutamate / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000235:genetics; D013116:Spinal Cord / Q000187:drug effects / Q000378:metabolism; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry / Q000494:pharmacology
D018712:Analgesics, Non-Narcotic; D001555:Benzene Derivatives; D004952:Esters; D011758:Pyrroles; D018094:Receptors, Metabotropic Glutamate; D013876:Thiophenes; C104077:metabotropic glutamate receptor type 1