Journal Article PUBDB-2015-00006

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4-Amino-Substituted Benzenesulfonamides as Inhibitors of Human Carbonic Anhydrases

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2014
MDPI Basel

Molecules 19(11), 17356 - 17380 () [10.3390/molecules191117356]
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Abstract: Abstract: A series of N-aryl-β-alanine derivatives and diazobenzenesulfonamides containingaliphatic rings were designed, synthesized, and their binding to carbonic anhydrases (CA) I,II, VI, VII, XII, and XIII was studied by the fluorescent thermal shift assay and isothermaltitration calorimetry. The results showed that 4-substituted diazobenzenesulfonamides weremore potent CA binders than N-aryl-β-alanine derivatives. Most of the N-aryl-β-alaninederivatives showed better affinity for CA II while diazobenzenesulfonamides possessednanomolar affinities towards CA I isozyme. X-ray crystallographic structures showed themodes of binding of both compound groups.

Classification:

Note: OA

Contributing Institute(s):
  1. EMBL-User (EMBL-User)
Research Program(s):
  1. PETRA Beamline P13 (POF2-54G14) (POF2-54G14)
  2. MOBILI - Strengthening and Sustaining the European Perspectives of Molecular Biotechnology in Lithuania (245721) (245721)
Experiment(s):
  1. PETRA Beamline P13 (PETRA III)

Appears in the scientific report 2014
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Medline ; Creative Commons Attribution CC BY 4.0 ; DOAJ ; OpenAccess ; Current Contents - Physical, Chemical and Earth Sciences ; IF < 5 ; JCR ; NCBI Molecular Biology Database ; SCOPUS ; Science Citation Index Expanded ; Thomson Reuters Master Journal List ; Web of Science Core Collection
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 Record created 2015-01-02, last modified 2025-07-30


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