88084-17-7Relevant academic research and scientific papers
2-Imidazole as a Substitute for the Electrophilic Group Gives Highly Potent Prolyl Oligopeptidase Inhibitors
Arja, Khaled,Auno, Samuli,Dillemuth, Pyry M. J.,Kilpel?inen, Tommi P.,Lahtela-Kakkonen, Maija K.,My?h?nen, Timo T.,P?tsi, Henri T.,Wallén, Erik A. A.
, p. 1578 - 1584 (2021/10/04)
Different five-membered nitrogen-containing heteroaromatics in the position of the typical electrophilic group in prolyl oligopeptidase (PREP) inhibitors were investigated and compared to tetrazole. The 2-imidazoles were highly potent inhibitors of the pr
4H-3,1-benzoxazin-4-one derivative
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, (2008/06/13)
4H-3,1-benzoxazin-4-one derivatives represented by formula (I) below: STR1 wherein R1 represents a lower alkyl group, R2 represents a lower alkyl group, a lower alkylthioalkyl group, or a lower alkanesulfinylalkyl group, R3/sup
Tri- and tetrapeptide analogues of kinins as potential renal vasodilators
Pfeiffer,Chambers,Hilbert,Woodward,Ackerman
, p. 325 - 341 (2007/10/02)
Tri- and tetrapeptide analogues were synthesized and evaluated as renal vasodilators. These peptides were prepared by standard coupling reactions which also provided good yields with hindered α-methyl amino acid derivatives. Preliminary evidence of renal vasodilator activity was determined in anesthetized dogs by measuring the effects on renal blood flow and calculating the accompanying changes in renal vascular resistance. The most potent compounds contained, in their structure, the L-prolyl-DL-α-methylphenylalanyl-L-arginine and L-prolyl-DL-α-methyl-phenyalanylglycyl-L-proline arrays. Substitution on the N-terminal proline with 4-phenylbutyryl and 4-(4-hydroxyphenyl)butyryl side chains produced enhanced renal vasodilator activity and, in certain cases, selectivity for the renal vasculature.
