Pyrimethamine Derivatives: Insight into Binding Mechanism and Improved Enhancement of Mutant β-N-acetylhexosaminidase Activity.

doi:10.1021/jm5017895

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Article

Pyrimethamine Derivatives: Insight into Binding Mechanism and Improved Enhancement of Mutant β-N-acetylhexosaminidase Activity.

Journal of medicinal chemistry - 11 Jun 2015

Tropak Michael B, Zhang Jianmin, Yonekawa Sayuri, Rigat Brigitte A, Aulakh Virender S, Smith Matthew R, Hwang Hee-Jong, Ciufolini Marco A, Mahuran Don J

Abstract excerpt

In order to identify structural features of pyrimethamine (5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine) that contribute to its inhibitory activity (IC50 value) and chaperoning efficacy toward β-N-acetylhexosaminidase, derivatives of the compound were synthesized that differ at the positions bearing the amino, ethyl, and chloro groups. Whereas the amino groups proved to be critical to its inhibitory activity,...

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PMID: 25984755
DOI: 10.1021/jm5017895

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.