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Molecules 2018, 23(10), 2607;

Aminobenzosuberone Scaffold as a Modular Chemical Tool for the Inhibition of Therapeutically Relevant M1 Aminopeptidases

Laboratoire d’Innovation Moléculaire et Applications, Université de Haute-Alsace, Université de Strasbourg, CNRS, 68093 Mulhouse, France
Centre for Chemical Biology, CSIR-Indian Institute of Chemical Technology, Hyderabad 500007, Telangana, India
Academy of Scientific and Innovative Research (AcSIR), Rafi Marg, New Dehli 110001, India
Protein Chemistry Laboratory, INRASTES, National Centre for Scientific Research Demokritos, Agia Paraskevi, 15310 Athens, Greece
Molécules de Communication et Adaptation des Micro-organismes, Muséum National d’Histoire Naturelle, CNRS, 75231 Paris, France
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Current address: Laboratoire Vigne, Biotechnologies et Environnement, Université de Haute-Alsace, Université de Strasbourg, 68008 Colmar, France.
Received: 19 September 2018 / Revised: 8 October 2018 / Accepted: 10 October 2018 / Published: 11 October 2018
(This article belongs to the Special Issue Medicinal Chemistry in Europe)
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The synthesis of racemic substituted 7-amino-5,7,8,9-tetrahydrobenzocyclohepten-6-one hydrochlorides was optimized to enhance reproducibility and increase the overall yield. In order to investigate their specificity, series of enzyme inhibition assays were carried out against a diversity of proteases, covering representative members of aspartic, cysteine, metallo and serine endopeptidases and including eight members of the monometallic M1 family of aminopeptidases as well as two members of the bimetallic M17 and M28 aminopeptidase families. This aminobenzosuberone scaffold indeed demonstrated selective inhibition of M1 aminopeptidases to the exclusion of other tested protease families; it was particularly potent against mammalian APN and its bacterial/parasitic orthologues EcPepN and PfAM1. View Full-Text
Keywords: M1 aminopeptidases; selective inhibitors; aminobenzosuberone scaffold M1 aminopeptidases; selective inhibitors; aminobenzosuberone scaffold

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Salomon, E.; Schmitt, M.; Marapaka, A.K.; Stamogiannos, A.; Revelant, G.; Schmitt, C.; Alavi, S.; Florent, I.; Addlagatta, A.; Stratikos, E.; Tarnus, C.; Albrecht, S. Aminobenzosuberone Scaffold as a Modular Chemical Tool for the Inhibition of Therapeutically Relevant M1 Aminopeptidases. Molecules 2018, 23, 2607.

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