Microtubule-Stabilizing 1,2,4-Triazolo[1,5-<i>a</i>]pyrimidines as Candidate Therapeutics for Neurodegenerative Disease: Matched Molecular Pair Analyses and Computational Studies Reveal New Structure–Activity Insights-Reference-Cited by-同舟云学术

Microtubule-Stabilizing 1,2,4-Triazolo[1,5-a]pyrimidines as Candidate Therapeutics for Neurodegenerative Disease: Matched Molecular Pair Analyses and Computational Studies Reveal New Structure–Activity Insights

Published:2022-12-19 Issue:1 Volume:66 Page:435-459
ISSN:0022-2623
Container-title:Journal of Medicinal Chemistry
language:en
Short-container-title:J. Med. Chem.

Author:

Alle Thibault¹^ORCID,Varricchio Carmine²^ORCID,Yao Yuemang³,Lucero Bobby⁴,Nzou Goodwell³,Demuro Stefania¹,Muench Megan³,Vuong Khoa D.¹,Oukoloff Killian¹,Cornec Anne-Sophie⁵,Francisco Karol R.¹,Caffrey Conor R.¹^ORCID,Lee Virginia M.-Y.³,Smith Amos B.⁵^ORCID,Brancale Andrea²^ORCID,Brunden Kurt R.³,Ballatore Carlo¹^ORCID

Affiliation:

1. Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, 9500 Gilman Drive, La Jolla, California 92093, United States

2. Cardiff School of Pharmacy and Pharmaceutical Sciences, Cardiff University, King Edward VII Avenue, Cardiff CF103NB, U.K.

3. Center for Neurodegenerative Disease Research, Perelman School of Medicine, University of Pennsylvania, 3600 Spruce St., Philadelphia, Pennsylvania 19104, United States

4. Department of Chemistry & Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, California 92093, United States

5. Department of Chemistry, School of Arts and Sciences, University of Pennsylvania, 231 South 34th St., Philadelphia, Pennsylvania 19104-6323, United States

Funder

National Institute on Aging

Publisher

American Chemical Society (ACS)

Subject

Drug Discovery,Molecular Medicine

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.2c01411

Reference21 articles.

1. Tau-mediated neurodegeneration in Alzheimer's disease and related disorders

2. Microtubule-binding drugs offset tau sequestration by stabilizing microtubules and reversing fast axonal transport deficits in a tauopathy model

3. A brain-penetrant triazolopyrimidine enhances microtubule-stability, reduces axonal dysfunction and decreases tau pathology in a mouse tauopathy model