104668-15-7Relevant academic research and scientific papers
TIPP: A Highly Potent and Stable Pseudopeptide δ Opioid Receptor Antagonist with Extraordinary δ Selectivity
Schiller, Peter W.,Weltrowska, Grazyna,Nguyen, Thi M.-D.,Wilkes, Brian C.,Chung, Nga N.,Lemieux, Carole
, p. 3182 - 3187 (1993)
Pseudopeptide analogues of the δ opioid antagonists H-Tyr-Tic-Phe-Phe-OH (TIPP) and H-Tyr-Tic-Phe-OH (TIP) containing a reduced peptide bond between the Tic2 and Phe3 residues were synthesized.The two compounds, H-Tyr-TicψPhe-
Facile generation of aziridines from the reaction of α-diazoamides with tethered oximino-ethers
McMills, Mark C.,Wright, Dennis L.,Zubkowski, Jeffrey D.,Valente, Edward J.
, p. 7205 - 7208 (1996)
In an attempt to prepare azomethine ylide intermediates for cycloaddition reactions with electron deficient olefins, oximino-ethers with tethered α-diazoamide moieties were reacted in the presence of metal catalyst. The reaction resulted in aziridine formation preferentially.
Structure-Based Drug Design of Bisubstrate Inhibitors of Phenylethanolamine N-Methyltransferase Possessing Low Nanomolar Affinity at Both Substrate Binding Domains1
Lu, Jian,Bart, Aaron G.,Wu, Qian,Criscione, Kevin R.,McLeish, Michael J.,Scott, Emily E.,Grunewald, Gary L.
, p. 13878 - 13898 (2020/12/02)
The enzyme phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28) catalyzes the final step in the biosynthesis of epinephrine and is a potential drug target, primarily for the control of hypertension. Unfortunately, many potent PNMT inhibitors also po
Investigations concerning the organolanthanide and group 3 metallocene-catalyzed cyclization-functionalization of nitrogen-containing dienes
Molander, Gary A.,Romero, Jan Antoinette C.
, p. 2631 - 2643 (2007/10/03)
Organolanthanide catalyzed cyclization-silylation of nitrogen-containing polyunsaturated systems allows access to core structures commonly found in naturally occurring alkaloids. Nitrogen-containing dienes with various substitution patterns were investigated. The method was most successful for substrates with terminal alkenes. Cyclization upon pendant 1,1-disubstituted olefins was not realized under various conditions. Interestingly, sterically hindered sulfonamides, which were previously believed to render the catalyst inactive, were actually compatible with the catalyst, thus affording the cyclized products after prolonged reaction times. Variations using fused ring systems were also investigated.
Piperazine- and piperidine-derivatives as melanocortin receptor agonists
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Page/Page column 58, (2010/02/06)
The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction.
Intramolecular aziridination: Decomposition of diazoamides with tethered imino bonds
Wright, Dennis L.,McMills, Mark C.
, p. 667 - 670 (2008/02/14)
(Matrix presented) Of three possible mechanistic pathways, tethered oximino ethers react intramolecularly with diazoamides to produce a diazabicyclo[5.1.0]-hexane aziridine containing skeleton. Several acyclic and cyclic templates were synthesized and reacted with rhodium catalysts to prepare their corresponding annulated aziridines. Anomalous behavior was discovered with the piperidine template, resulting in an aziridination occurring during the attempted diazo-transfer reaction, rather than the catalyzed carbenoid reaction.
