Literature DB >> 1479580

Synthesis and physicochemical properties of sulfamate derivatives as topical antiglaucoma agents.

Y S Lo1, J C Nolan, T H Maren, W J Welstead, D F Gripshover, D A Shamblee.   

Abstract

Several imidazolylphenyl sulfamate and (imidazolylphenoxy)alkyl sulfamate derivatives were synthesized and evaluated as topically active carbonic anhydrase inhibitors. Water solubility, pKa, carbonic anhydrase inhibition, and partition coefficient for the compounds were measured. Sulfamic acid 2-[4-(1H-imidazol-1-yl)phenoxy]ethyl ester monohydrochloride (16) has the best combination of properties and showed excellent topical activity in lowering the intraocular pressure in New Zealand white rabbits.

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Year:  1992        PMID： 1479580     DOI： 10.1021/jm00104a003

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  4 in total

Review 1.  Carbonic anhydrase as a model for biophysical and physical-organic studies of proteins and protein-ligand binding.

Authors:  Vijay M Krishnamurthy; George K Kaufman; Adam R Urbach; Irina Gitlin; Katherine L Gudiksen; Douglas B Weibel; George M Whitesides
Journal:  Chem Rev       Date:  2008-03       Impact factor: 60.622

2.  Discovery and Development of the Aryl O-Sulfamate Pharmacophore for Oncology and Women's Health.

Authors:  Mark P Thomas; Barry V L Potter
Journal:  J Med Chem       Date:  2015-06-12       Impact factor: 7.446

3.  A paradigm for drug discovery employing encoded combinatorial libraries.

Authors:  J J Burbaum; M H Ohlmeyer; J C Reader; I Henderson; L W Dillard; G Li; T L Randle; N H Sigal; D Chelsky; J J Baldwin
Journal:  Proc Natl Acad Sci U S A       Date:  1995-06-20       Impact factor: 11.205

Review 4.  Imidazoles as potential anticancer agents.

Authors:  Imran Ali; Mohammad Nadeem Lone; Haasan Y Aboul-Enein
Journal:  Medchemcomm       Date:  2017-04-13       Impact factor: 3.597
  4 in total

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