130930-27-7Relevant articles and documents
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta
Anas, Andrea Roxanne J.,Kisugi, Takaya,Umezawa, Taiki,Matsuda, Fuyuhiko,Okino, Tatsufumi,Campitelli, Marc R.,Quinn, Ronald J.
, p. 1546 - 1552,7 (2012/12/12)
Bioassay-guided investigation of the cyanobacterium Anabaena compacta extracts afforded spumigin J (1) and the known thrombin inhibitor spumigin A (2). The absolute configuration of 1 was analyzed by advanced Marfey's methodology. Compounds 1 and 2 inhibi
Thrombin inhibitors from the freshwater cyanobacterium Anabaena compacta
Anas, Andrea Roxanne J.,Kisugi, Takaya,Umezawa, Taiki,Matsuda, Fuyuhiko,Campitelli, Marc R.,Quinn, Ronald J.,Okino, Tatsufumi
, p. 1546 - 1552 (2013/01/15)
Bioassay-guided investigation of the cyanobacterium Anabaena compacta extracts afforded spumigin J (1) and the known thrombin inhibitor spumigin A (2). The absolute configuration of 1 was analyzed by advanced Marfey's methodology. Compounds 1 and 2 inhibi
RNA-selective cross-pairing of backbone-extended pyrrolidine-amide oligonucleotide mimics (bePOMs)
Worthington, Roberta J.,Bell, Neil M.,Wong, Raymond,Micklefield, Jason
, p. 92 - 103 (2008/09/21)
Pyrrolidine-amide oligonucleotide mimics (POMs) can cross-pair strongly with complementary parallel and antiparallel DNA and RNA targets in a sequence-specific fashion. As a result POMs have significant potential for applications including in vivo gene silencing, diagnostics and bioanalysis. To further modulate the DNA- and RNA-recognition properties and fine-tune the physiochemical properties of POMs for nucleic acid targeting, backbone-extended pyrrolidine-amide oligonucleotide mimics (bePOM I and II) were introduced. The bePOMs differ from the original POMs through the insertion of an additional methylene group into the backbone units, which increases the flexibility of the oligomers. bePOM I and II oligomers were synthesised using solid-phase peptide chemistry. Interestingly, UV thermal denaturation and circular dichroism studies reveals bePOM I and II can hybridise with complementary RNA, but not DNA. The Royal Society of Chemistry 2008.
PYRROLIDINYL DI-CARBOXYLIC ACID DERIVATIVES AS METABOTROPIC GLUTAMATE RECEPTOR AGONISTS
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, (2008/06/13)
The present invention provides novel compounds that affect certain excitatory amino acid receptors, and are useful in the treatment of neurological disorders and psychiatric disorders.
Benzamide derivatives
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, (2008/06/13)
A benzamide derivative represented by the formula: STR1 having a promoting activity of gastrointestinal tract and pharmacentical composition containing the same.
Conformationally Defined Neurotransmitter Analogues. Selective Inhibition of Glutamate Uptake by One Pyrrolidine-2,4-dicarboxylate Diastereomer
Bridges, Richard J.,Stanley, Mark S.,Anderson, Michael W.,Cotman, Carl W.,Chamberlin, A. Richard
, p. 717 - 725 (2007/10/02)
In order to determine the conformational requirements for binding of L-glutamate to the proteins involved in the process of neurotransmission, rigid analogues containing an embedded glutamate moiety have been prepared.These "conformer mimics", the pyrrolidine-2,4-dicarboxylates 4, 7, 11, and 14, were synthesized from commercially available trans-4-hydroxy-L-proline and cis-4-hydroxy-D-proline, and then were tested for their ability to inhibit the high-affinity transport of -L-glutamate into synaptosomes and to block the binding of radioligands to the NMDA (N-methyl-D-aspartate), KA (kainate), and QA (quisqualate) glutamate neurotransmitter receptor sites.While none of the four analogues binds effectively to the excitatory receptors, the L-trans-isomer 7 is a potent and selective competitive inhibitor of L-glutamate transport.These results delineate a specific structural/conformational preference for binding to the uptake system that is distinct from that required for binding to the NMDA, KA, and QA receptors.
