Development of a fluorogenic small substrate for dipeptidyl peptidase-4
A series of aniline and m-phenylenediamine derivatives with electron-withdrawing 3,3,3-trifluoropropenyl substituents were synthesized as small and chemically stable fluorescent organic compounds. Their fluorescence performances were evaluated by converting 2,4-disubstituted aniline 1 to the non-flu...
Main Authors: | , , , , , , , , |
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Format: | Article |
Language: | English |
Published: |
Beilstein-Institut
2017-12-01
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Series: | Beilstein Journal of Organic Chemistry |
Subjects: | |
Online Access: | https://doi.org/10.3762/bjoc.13.267 |
Summary: | A series of aniline and m-phenylenediamine derivatives with electron-withdrawing 3,3,3-trifluoropropenyl substituents were synthesized as small and chemically stable fluorescent organic compounds. Their fluorescence performances were evaluated by converting 2,4-disubstituted aniline 1 to the non-fluorescent dipeptide analogue H-Gly-Pro-1 for the use as a fluorogenic substrate for dipeptidyl peptidase-4 (DPP-4). The progress of the enzymatic hydrolysis of H-Gly-Pro-1 with DPP-4 was monitored by fluorometric determination of 1 released into the reaction medium. The results suggest that 1 could be used as fluorophore in OFF–ON-type fluorogenic probes. |
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ISSN: | 1860-5397 |