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Communication

Tetrahydroimidazo[4,5-c]pyridine-Based Inhibitors of Porphyromonas gingivalis Glutaminyl Cyclase

1
Fraunhofer Institute for Cell Therapy and Immunology IZI, Department of Drug Design and Target Validation MWT, Weinbergweg 22, 06120 Halle (Saale), Germany
2
PerioTrap Pharmaceuticals GmbH, Weinbergweg 22, 06120 Halle (Saale), Germany
*
Authors to whom correspondence should be addressed.
Academic Editor: Pascal Sonnet
Pharmaceuticals 2021, 14(12), 1206; https://doi.org/10.3390/ph14121206
Received: 15 October 2021 / Revised: 12 November 2021 / Accepted: 17 November 2021 / Published: 23 November 2021
(This article belongs to the Section Medicinal Chemistry)
Periodontitis is a severe yet underestimated oral disease. Since it is linked to several systemic diseases, such as diabetes, artheriosclerosis, and even Alzheimer’s disease, growing interest in treating periodontitis has emerged recently. The major cause of periodontitis is a shift in the oral microbiome. A keystone pathogen that is associated with this shift is Porphyromonas gingivalis. Hence, targeting P. gingivalis came into focus of drug discovery for the development of novel antiinfective compounds. Among others, glutaminyl cyclases (QCs) of oral pathogens might be promising drug targets. Here, we report the discovery and structure–activity relationship of a novel class of P. gingivalis QC inhibitors according to a tetrahydroimidazo[4,5-c]pyridine scaffold. Some compounds exhibited activity in the lower nanomolar range and thus were further characterized with regard to their selectivity and toxicity. View Full-Text
Keywords: PgQC; Porphyromonas gingivalis; periodontitis; glutaminyl cyclase PgQC; Porphyromonas gingivalis; periodontitis; glutaminyl cyclase
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MDPI and ACS Style

Ramsbeck, D.; Taudte, N.; Jänckel, N.; Strich, S.; Rahfeld, J.-U.; Buchholz, M. Tetrahydroimidazo[4,5-c]pyridine-Based Inhibitors of Porphyromonas gingivalis Glutaminyl Cyclase. Pharmaceuticals 2021, 14, 1206. https://doi.org/10.3390/ph14121206

AMA Style

Ramsbeck D, Taudte N, Jänckel N, Strich S, Rahfeld J-U, Buchholz M. Tetrahydroimidazo[4,5-c]pyridine-Based Inhibitors of Porphyromonas gingivalis Glutaminyl Cyclase. Pharmaceuticals. 2021; 14(12):1206. https://doi.org/10.3390/ph14121206

Chicago/Turabian Style

Ramsbeck, Daniel, Nadine Taudte, Nadine Jänckel, Stefanie Strich, Jens-Ulrich Rahfeld, and Mirko Buchholz. 2021. "Tetrahydroimidazo[4,5-c]pyridine-Based Inhibitors of Porphyromonas gingivalis Glutaminyl Cyclase" Pharmaceuticals 14, no. 12: 1206. https://doi.org/10.3390/ph14121206

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