| Topically active carbonic anhydrase inhibitors. 4. [(Hydroxyalkyl)sulfonyl]benzene and [(hydroxyalkyl)sulfonyl]thiophenesulfonamides. | |
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MedLine Citation:
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PMID: 1920359 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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For several decades a tantalizing goal for the treatment of primary open-angle glaucoma has been the development of a topically active carbonic anhydrase inhibitor. Recent results from several research groups indicate that considerable progress has been made toward this objective. In this report, we present the design and synthesis of (hydroxyalkyl)sulfonyl-substituted benzene- and thiophenesulfonamides. These compounds exhibit inhibition of carbonic anhydrase II in the nanomolar range and lower intraocular pressure in the alpha-chymotrypsinized rabbit model of ocular hypertension after topical instillation. |
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Authors:
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K L Shepard; S L Graham; R J Hudcosky; S R Michelson; T H Scholz; H Schwam; A M Smith; J M Sondey; K M Strohmaier; R L Smith |
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Publication Detail:
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Type: Comparative Study; Journal Article |
Journal Detail:
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Title: Journal of medicinal chemistry Volume: 34 ISSN: 0022-2623 ISO Abbreviation: J. Med. Chem. Publication Date: 1991 Oct |
Date Detail:
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Created Date: 1991-11-18 Completed Date: 1991-11-18 Revised Date: 2006-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9716531 Medline TA: J Med Chem Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 3098-105 Citation Subset: IM |
Affiliation:
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Department of Medicinal Chemistry, Merck Sharp & Dohme Research Laboratories, West Point, Pennsylvania 19486. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Administration, Topical Animals Carbonic Anhydrase Inhibitors / chemical synthesis*, pharmacology Chymotrypsin Glutathione / metabolism Intraocular Pressure / drug effects Ocular Hypertension / chemically induced, drug therapy Rabbits Structure-Activity Relationship Sulfonamides / chemical synthesis*, chemistry*, pharmacology, therapeutic use Thiophenes / chemical synthesis*, pharmacology, therapeutic use |
| Chemical | |
Reg. No./Substance:
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0/Carbonic Anhydrase Inhibitors; 0/Sulfonamides; 0/Thiophenes; 70-18-8/Glutathione; 98-10-2/benzenesulfonamide; EC 3.4.21.1/Chymotrypsin |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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