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Article ; Online: Novel 12-hydroxydehydroabietylamine derivatives act as potent and selective butyrylcholinesterase inhibitors.

Loesche, Anne / Wiemann, Jana / Rohmer, Matthias / Brandt, Wolfgang / Csuk, René

2019 Volume 90, Page(s) 103092

Abstract: The skeleton of the diterpene dehydroabietylamine was modified, and a set of 12-hydroxy-dehydroabietylamine derivatives was obtained. The compounds were screened in colorimetric Ellman's assays to determine their ability to act as inhibitors for the ... ...

Abstract	The skeleton of the diterpene dehydroabietylamine was modified, and a set of 12-hydroxy-dehydroabietylamine derivatives was obtained. The compounds were screened in colorimetric Ellman's assays to determine their ability to act as inhibitors for the enzymes acetylcholinesterase (AChE, from electric eel) and butyrylcholinesterase (BChE, from equine serum). Additional investigations concerning the enzyme kinetics were performed and showed 12-hydroxy-N-(4-nitro-benzoyl)dehydroabietylamine (13) and 12-hydroxy-N-(isonicotinoyl)dehydroabietylamine (17) as selective BChE inhibitors holding good inhibition constants K
MeSH term(s)	Acetylcholinesterase/chemistry ; Animals ; Butyrylcholinesterase/chemistry ; Cholinesterase Inhibitors/chemistry ; Cholinesterase Inhibitors/pharmacology ; Diterpenes/chemistry ; Diterpenes/pharmacology ; Electrophorus ; Ethylamines/chemistry ; Ethylamines/pharmacology ; Molecular Docking Simulation ; Structure-Activity Relationship
Chemical Substances	12-Hydroxy-N-(isonicotinoyl)dehydroabietylamine ; Cholinesterase Inhibitors ; Diterpenes ; Ethylamines ; Acetylcholinesterase (EC 3.1.1.7) ; Butyrylcholinesterase (EC 3.1.1.8)
Language	English
Publishing date	2019-07-02
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	120080-x
ISSN	1090-2120 ; 0045-2068
ISSN (online)	1090-2120
ISSN	0045-2068
DOI	10.1016/j.bioorg.2019.103092
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Zs.A 4207: Show issues

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Article ; Online: Unexpected AChE inhibitory activity of (2E)α,β-unsaturated fatty acids.

Loesche, Anne / Wiemann, Jana / Al Halabi, Zayan / Karasch, Julia / Sippl, Wolfgang / Csuk, René

Bioorganic & medicinal chemistry letters

2018 Volume 28, Issue 20, Page(s) 3315–3319

Abstract: A small library of (E) α,β-unsaturated fatty acids was prepared, and 20 different saturated and mono-unsaturated fatty acids differing in chain length were subjected to Ellman's assays to determine their ability to act as inhibitors for AChE or BChE. ... ...

Abstract	A small library of (E) α,β-unsaturated fatty acids was prepared, and 20 different saturated and mono-unsaturated fatty acids differing in chain length were subjected to Ellman's assays to determine their ability to act as inhibitors for AChE or BChE. While the compounds were only very weak inhibitors of BChE, seven molecules were inhibitors of AChE holding IC
MeSH term(s)	Acetylcholinesterase/chemistry ; Animals ; Butyrylcholinesterase/chemistry ; Catalytic Domain ; Cholinesterase Inhibitors/chemical synthesis ; Cholinesterase Inhibitors/chemistry ; Electrophorus ; Fatty Acids, Unsaturated/chemical synthesis ; Fatty Acids, Unsaturated/chemistry ; Horses ; Kinetics ; Models, Molecular ; Molecular Structure ; Small Molecule Libraries/chemical synthesis ; Small Molecule Libraries/chemistry
Chemical Substances	Cholinesterase Inhibitors ; Fatty Acids, Unsaturated ; Small Molecule Libraries ; Acetylcholinesterase (EC 3.1.1.7) ; Butyrylcholinesterase (EC 3.1.1.8)
Language	English
Publishing date	2018-09-11
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1063195-1
ISSN	1464-3405 ; 0960-894X
ISSN (online)	1464-3405
ISSN	0960-894X
DOI	10.1016/j.bmcl.2018.09.013
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Zs.A 3203: Show issues

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Article: Periodontal infection a risk factor for cardiovascular disease?

Loesche, W J

Postgraduate medicine

2000 Volume 107, Issue 5, Page(s) 17, 20

MeSH term(s)	Bacterial Infections/complications ; Coronary Disease/epidemiology ; Coronary Disease/microbiology ; Humans ; Periodontal Diseases/complications ; Periodontal Diseases/microbiology ; Risk Factors ; Stroke/epidemiology ; Stroke/microbiology
Language	English
Publishing date	2000-05-01
Publishing country	England
Document type	Journal Article
ZDB-ID	410138-8
ISSN	1941-9260 ; 0032-5481
ISSN (online)	1941-9260
ISSN	0032-5481
DOI	10.3810/pgm.2000.5.1.1076
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Ua VI Zs.407: Show issues

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Article: Periodontal disease: link to cardiovascular disease.

Loesche, W J

Compendium of continuing education in dentistry (Jamesburg, N.J. : 1995)

2000 Volume 21, Issue 6, Page(s) 463–6, 468, 470 passim; quiz 484

Abstract: Poor oral hygiene that leads to dental infections could contribute to adverse medical outcomes such as cardiovascular disease. Twelve studies of varying degrees of design rigor have associated dental conditions, such as periodontal disease, missing teeth, ...

Abstract	Poor oral hygiene that leads to dental infections could contribute to adverse medical outcomes such as cardiovascular disease. Twelve studies of varying degrees of design rigor have associated dental conditions, such as periodontal disease, missing teeth, and edentulousness, with either coronary heart disease or a cerebral vascular accident. Six of the studies were longitudinal so that the demonstration of the oral health parameters as significant predictors of the cardiovascular event would elevate the dental parameter to the status of a risk factor. Because dental diseases (especially periodontal disease) are treatable, the dental component is a modifiable risk factor; therefore, maintaining good oral health should receive the highest priority for a healthy life.
MeSH term(s)	Bacterial Infections ; Cardiovascular Diseases/complications ; Cerebrovascular Disorders/complications ; Coronary Disease/complications ; Forecasting ; Health Priorities ; Humans ; Longitudinal Studies ; Mouth, Edentulous/complications ; Oral Hygiene ; Periodontal Diseases/complications ; Periodontal Diseases/microbiology ; Periodontal Diseases/prevention & control ; Risk Factors ; Tooth Loss/complications
Language	English
Publishing date	2000-06
Publishing country	United States
Document type	Journal Article ; Research Support, U.S. Gov't, P.H.S. ; Review
ZDB-ID	632569-5
ISSN	1548-8578 ; 0734-0338
ISSN	1548-8578 ; 0734-0338
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Zs.B 2795: Show issues

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Article: The effects of antimicrobial mouthrinses on oral malodor and their status relative to US Food and Drug Administration regulations.

Loesche, W J

Quintessence international (Berlin, Germany : 1985)

1999 Volume 30, Issue 5, Page(s) 311–318

Abstract: This study was undertaken to review the rationale behind the usage of antibacterial mouthrinses to control oral malodor and to evaluate the claims made for antibacterial mouthrinses against the statements of US Food and Drug Administration regulations. ... ...

Abstract	This study was undertaken to review the rationale behind the usage of antibacterial mouthrinses to control oral malodor and to evaluate the claims made for antibacterial mouthrinses against the statements of US Food and Drug Administration regulations. The literature from 1960 to August 1997, found in a MEDLINE search on oral malodor, halitosis, and tongue microbiology, was examined. Clinical trials that were double blind and had selected subjects who exhibited a detectable level of oral malodor were evaluated. Individuals who experience oral malodor resulting from the overgrowth of proteolytic, anaerobic bacteria on their tongue surfaces can be successfully treated by a regimen that includes tongue brushing and toothbrushing, often in combination with use of a mouthrinse containing an antibacterial agent. Several candidate mouthrinses containing essential oils, zinc chloride, or an oil-water-cetylpyridinium chloride mouthrinse have reduced the organoleptic scores of individuals with moderate levels of oral malodor in the absence of tongue brushing. Very little long-term data beyond 6 weeks of usage are available. These mouthrinses should be marketed as oral deodorants that are analogous in purpose to the usage of deodorant soaps to control and/or eliminate body malodors.
MeSH term(s)	Anti-Infective Agents, Local/pharmacology ; Anti-Infective Agents, Local/therapeutic use ; Clinical Trials as Topic ; Deodorants ; Drug and Narcotic Control/legislation & jurisprudence ; Halitosis/drug therapy ; Humans ; Mouthwashes/pharmacology ; Mouthwashes/therapeutic use ; Sulfur-Reducing Bacteria/drug effects ; Tongue/microbiology ; United States ; United States Food and Drug Administration
Chemical Substances	Anti-Infective Agents, Local ; Deodorants ; Mouthwashes
Language	English
Publishing date	1999-05
Publishing country	Germany
Document type	Journal Article
ZDB-ID	7436-6
ISSN	1936-7163 ; 0033-6572
ISSN (online)	1936-7163
ISSN	0033-6572
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Zs.B 1210: Show issues

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Article: The antimicrobial treatment of periodontal disease: changing the treatment paradigm.

Loesche, W J

Critical reviews in oral biology and medicine : an official publication of the American Association of Oral Biologists

1999 Volume 10, Issue 3, Page(s) 245–275

Abstract: Over the last 100 years, methods of surgical periodontal treatment have enjoyed a history of success in improving oral health. The paradigm of care is based on the "non-specific plaque hypothesis"--that is, the overgrowth of bacterial plaques cause ... ...

Abstract	Over the last 100 years, methods of surgical periodontal treatment have enjoyed a history of success in improving oral health. The paradigm of care is based on the "non-specific plaque hypothesis"--that is, the overgrowth of bacterial plaques cause periodontal disease, and the suppression of this overgrowth reduces disease risk. The central feature of this approach to care is the removal of inflamed gingival tissue around the teeth to reduce periodontal pocket depth, thereby facilitating plaque removal by the dentist and by the patient at home. Over the last 30 years, with the recognition that periodontal disease(s) is caused by specific bacteria and that specific antimicrobial agents can reduce or eliminate the infection, a second paradigm has developed. This new paradigm, the "specific plaque hypothesis", focuses on reducing the specific bacteria that cause periodontal attachment loss. The contrast between the two paradigms can be succinctly stated as follows: The antimicrobial therapy reduces the cause, while the surgical therapy reduces the result of the periodontal infection. The specific plaque hypothesis has two important implications. First, with the increasing attention to evidence-based models for prevention, treatment, outcome assessment, and reimbursement of care, increasing attention and financial effort will be channeled into effective preventive and treatment methods. Second, the recent observations that periodontal infections increase the risk of specific systemic health problems, such as cardiovascular disease, argue for the prevention and elimination of these periodontal infections. This review highlights some of the evidence for the specific plaque hypothesis, and the questions that should be addressed if antimicrobial agents are to be used responsively and effectively.
MeSH term(s)	Anti-Bacterial Agents/therapeutic use ; Cardiovascular Diseases/etiology ; Cardiovascular Diseases/prevention & control ; Clinical Protocols ; Dental Plaque/microbiology ; Dental Plaque/therapy ; Evidence-Based Medicine ; Gingivitis/microbiology ; Gingivitis/therapy ; Humans ; Periodontal Attachment Loss/microbiology ; Periodontal Attachment Loss/therapy ; Periodontal Diseases/drug therapy ; Periodontal Diseases/microbiology ; Periodontal Diseases/prevention & control ; Periodontal Pocket/microbiology ; Periodontal Pocket/therapy ; Risk Factors ; Treatment Outcome
Chemical Substances	Anti-Bacterial Agents
Language	English
Publishing date	1999
Publishing country	United States
Document type	Journal Article ; Research Support, U.S. Gov't, P.H.S. ; Review
ZDB-ID	1130962-3
ISSN	1045-4411
ISSN	1045-4411
DOI	10.1177/10454411990100030101
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Zs.A 3504: Show issues

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Article ; Online: Longitudinal SARS-CoV-2 Nucleocapsid Antibody Kinetics, Seroreversion, and Implications for Seroepidemiologic Studies.

Emerging infectious diseases

2022 Volume 28, Issue 9, Page(s) 1859–1862

Abstract: Given widespread use of spike antibody in generating coronavirus disease vaccines, SARS-CoV-2 nucleocapsid antibodies are increasingly used to indicate previous infection in serologic surveys. However, longitudinal kinetics and seroreversion are poorly ... ...

Abstract	Given widespread use of spike antibody in generating coronavirus disease vaccines, SARS-CoV-2 nucleocapsid antibodies are increasingly used to indicate previous infection in serologic surveys. However, longitudinal kinetics and seroreversion are poorly defined. We found substantial seroreversion of nucleocapsid total immunoglobulin, underscoring the need to account for seroreversion in seroepidemiologic studies.
MeSH term(s)	Antibodies, Viral ; COVID-19/epidemiology ; Coronavirus Nucleocapsid Proteins/immunology ; Humans ; Kinetics ; Nucleocapsid ; Phosphoproteins/immunology ; SARS-CoV-2 ; Seroepidemiologic Studies
Chemical Substances	Antibodies, Viral ; Coronavirus Nucleocapsid Proteins ; Phosphoproteins ; nucleocapsid phosphoprotein, SARS-CoV-2
Language	English
Publishing date	2022-07-22
Publishing country	United States
Document type	Journal Article
ZDB-ID	1380686-5
ISSN	1080-6059 ; 1080-6040
ISSN (online)	1080-6059
ISSN	1080-6040
DOI	10.3201/eid2809.220729
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Zs.A 4778: Show issues

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Article ; Online: Piperlongumine B and analogs are promising and selective inhibitors for acetylcholinesterase.

Wiemann, Jana / Karasch, Julia / Loesche, Anne / Heller, Lucie / Brandt, Wolfgang / Csuk, René

European journal of medicinal chemistry

2017 Volume 139, Page(s) 222–231

Abstract: Piperlongumine B (19), an alkaloid previously isolated from long pepper (Piper longum) has been synthesized for the first time in a short sequence and in good yield together with 19 analogs. Screening of these compounds in Ellman's assays showed several ... ...

Abstract	Piperlongumine B (19), an alkaloid previously isolated from long pepper (Piper longum) has been synthesized for the first time in a short sequence and in good yield together with 19 analogs. Screening of these compounds in Ellman's assays showed several of them to be good inhibitors of acetylcholinesterase while being less active for butyrylcholinesterase. Activity of the compounds increased with the ring size of the heterocycle, and a maximum of activity was observed for an analog holding 12 methylene groups in the aliphatic side chain. These compounds may be regarded as promising candidates for the development of efficient inhibitors of acetylcholinesterase being useful for the treatment of Alzheimer's disease.
MeSH term(s)	Acetylcholinesterase/metabolism ; Animals ; Butyrylcholinesterase/metabolism ; Cholinesterase Inhibitors/chemical synthesis ; Cholinesterase Inhibitors/chemistry ; Cholinesterase Inhibitors/pharmacology ; Dioxolanes/chemical synthesis ; Dioxolanes/chemistry ; Dioxolanes/pharmacology ; Dose-Response Relationship, Drug ; Electrophorus/metabolism ; Molecular Structure ; Structure-Activity Relationship
Chemical Substances	Cholinesterase Inhibitors ; Dioxolanes ; Acetylcholinesterase (EC 3.1.1.7) ; Butyrylcholinesterase (EC 3.1.1.8) ; piperlongumine (SGD66V4SVJ)
Language	English
Publishing date	2017-08-02
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2017.07.081
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Zs.B 784: Show issues

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Article ; Online: Repurposing N,N'-bis-(arylamidino)-1,4-piperazinedicarboxamidines: An unexpected class of potent inhibitors of cholinesterases.

Loesche, Anne / Wiese, Jana / Sommerwerk, Sven / Simon, Vivienne / Brandt, Wolfgang / Csuk, René

European journal of medicinal chemistry

2017 Volume 125, Page(s) 430–434

Abstract: Drug repurposing (=drug repositioning) is an effective way to cut costs for the development of new therapeutics and to reduce the time-to-market time-span. Following this concept a small library of compounds was screened for their ability to act as ... ...

Abstract	Drug repurposing (=drug repositioning) is an effective way to cut costs for the development of new therapeutics and to reduce the time-to-market time-span. Following this concept a small library of compounds was screened for their ability to act as inhibitors of acetyl- and butyrylcholinesterase. Picloxydine, an established antiseptic, was shown to be an inhibitor for both enzymes. Systematic variation of the aryl substituents led to analogs possessing almost the same good properties as gold standard galantamine hydrobromide.
MeSH term(s)	Acetylcholinesterase/metabolism ; Anti-Infective Agents, Local/chemistry ; Anti-Infective Agents, Local/pharmacology ; Butyrylcholinesterase/metabolism ; Cholinesterase Inhibitors/chemistry ; Cholinesterase Inhibitors/pharmacology ; Drug Repositioning ; Humans ; Molecular Docking Simulation ; Piperazines/chemistry ; Piperazines/pharmacology
Chemical Substances	Anti-Infective Agents, Local ; Cholinesterase Inhibitors ; Piperazines ; picloxydine (4YC2PY3AEU) ; Acetylcholinesterase (EC 3.1.1.7) ; Butyrylcholinesterase (EC 3.1.1.8)
Language	English
Publishing date	2017-01-05
Publishing country	France
Document type	Journal Article
ZDB-ID	188597-2
ISSN	1768-3254 ; 0009-4374 ; 0223-5234
ISSN (online)	1768-3254
ISSN	0009-4374 ; 0223-5234
DOI	10.1016/j.ejmech.2016.09.051
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Zs.B 784: Show issues

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Article: Association of the oral flora with important medical diseases.

Loesche, W J

Current opinion in periodontology

1997 Volume 4, Page(s) 21–28

Abstract: Recently, there have been case-control and epidemiologic investigations that strongly associate poor dental health with cardiovascular disease, preterm low birth weight infants, and early death from any cause. In a 7-year prospective study, dental ... ...

Abstract	Recently, there have been case-control and epidemiologic investigations that strongly associate poor dental health with cardiovascular disease, preterm low birth weight infants, and early death from any cause. In a 7-year prospective study, dental disease was a significant predictor of coronary events leading to death after controlling for known coronary disease risk factors. Missing teeth displaces smoking as a risk factor for ischemic heart disease in another study. Periodontal disease was seven times more likely to be associated with a preterm delivery of a low birth weight infant than mother's age, race, number of live births, and use of tobacco or alcohol. This review examines the role of asymptomatic bacteremia as possibly explaining these associations, focusing on the bacterial load on the teeth as mediated via oral hygiene.
MeSH term(s)	Bacteremia/microbiology ; Bacteria, Anaerobic/pathogenicity ; Birth Weight/physiology ; Cardiovascular Diseases/etiology ; Cardiovascular Diseases/microbiology ; Dental Caries/complications ; Dental Health Surveys ; Dental Plaque/complications ; Dental Plaque/microbiology ; Focal Infection, Dental/complications ; Health Status ; Health Status Indicators ; Humans ; Infant, Low Birth Weight/immunology ; Infant, Newborn ; Mouth/microbiology ; Oral Hygiene ; Periodontal Diseases/complications ; Periodontal Diseases/microbiology ; Tooth Loss/complications
Language	English
Publishing date	1997
Publishing country	United States
Document type	Journal Article ; Research Support, U.S. Gov't, P.H.S. ; Review
ZDB-ID	1233570-8
ISSN	1065-626X
ISSN	1065-626X
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Se 1407: Show issues

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