Tetrahydroimidazo[4,5-<i>c</i>]pyridine-Based Inhibitors of <i>Porphyromonas gingivalis</i> Glutaminyl Cyclase
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...
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| Format: | Book |
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MDPI AG,
2021-11-01T00:00:00Z.
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| LEADER | 00000 am a22000003u 4500 | ||
|---|---|---|---|
| 001 | doaj_c83c92b5888541eb8c2136912ad25b5a | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Daniel Ramsbeck |e author |
| 700 | 1 | 0 | |a Nadine Taudte |e author |
| 700 | 1 | 0 | |a Nadine Jänckel |e author |
| 700 | 1 | 0 | |a Stefanie Strich |e author |
| 700 | 1 | 0 | |a Jens-Ulrich Rahfeld |e author |
| 700 | 1 | 0 | |a Mirko Buchholz |e author |
| 245 | 0 | 0 | |a Tetrahydroimidazo[4,5-<i>c</i>]pyridine-Based Inhibitors of <i>Porphyromonas gingivalis</i> Glutaminyl Cyclase |
| 260 | |b MDPI AG, |c 2021-11-01T00:00:00Z. | ||
| 500 | |a 10.3390/ph14121206 | ||
| 500 | |a 1424-8247 | ||
| 520 | |a 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 <i>Porphyromonas gingivalis</i>. Hence, targeting <i>P. gingivalis</i> 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 <i>P. gingivalis</i> QC inhibitors according to a tetrahydroimidazo[4,5-<i>c</i>]pyridine scaffold. Some compounds exhibited activity in the lower nanomolar range and thus were further characterized with regard to their selectivity and toxicity. | ||
| 546 | |a EN | ||
| 690 | |a PgQC | ||
| 690 | |a <i>Porphyromonas gingivalis</i> | ||
| 690 | |a periodontitis | ||
| 690 | |a glutaminyl cyclase | ||
| 690 | |a Medicine | ||
| 690 | |a R | ||
| 690 | |a Pharmacy and materia medica | ||
| 690 | |a RS1-441 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Pharmaceuticals, Vol 14, Iss 12, p 1206 (2021) | |
| 787 | 0 | |n https://www.mdpi.com/1424-8247/14/12/1206 | |
| 787 | 0 | |n https://doaj.org/toc/1424-8247 | |
| 856 | 4 | 1 | |u https://doaj.org/article/c83c92b5888541eb8c2136912ad25b5a |z Connect to this object online. |