Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0595921 (intraocular pressure)
 11,750 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

A series of N-hydroxy sulfonamides has been prepared by reaction of alkyl-, arylalkyl- and arylsulfonyl halides or sulfonic acid anhydrides with hydroxylamine. Structurally related inhibitors were also obtained from acyl chlorides and hydroxylamine, as well as by reaction of tosyl isocyanate with hydroxylamine, sulfamic acid and sulfamide. Inhibition of three carbonic anhydrase (CA) isozymes, hCA I, hCA II and bCA IV (h = human; b = bovine) with the prepared compounds has been investigated. Good inhibitors, as well as compounds with moderate activity against these isozymes were detected, depending on the R group to which the SO2NHOH or CONHOH moieties were attached. Susceptibility to inhibition was generally: hCA II > bCA IV >> hCA I. Some of the new inhibitors showed very good antiglaucoma action when administered directly into the eye in experimental animals, acting as more efficient intraocular pressure lowering agents as compared to the clinical drug dorzolamide. This constitutes an encouraging result for obtaining novel antiglaucoma drugs from this class of CA inhibitors.
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PMID:Carbonic anhydrase inhibitors: inhibition of isozymes I, II and IV with N-hydroxysulfonamides--a novel class of intraocular pressure lowering agents. 979 65

Selective inhibition of ciliary process enzyme i.e. Carbonic Anhydrase-II is an excellent approach in reducing elevated intraocular pressure, thus treating glaucoma. Due to characteristic physicochemical properties of sulphonamide (Inhibition of Carbonic Anhydrase), they are clinically effective against glaucoma. But the non-specificity of sulphonamide derivatives to isozyme, leads to a range of side effects. Presently, the absence of comparative studies related to the binding of the sulphonamides as inhibitors to CA isozymes limits their use. In this paper we have represented "Three Dimensional Quantitative Structure Activity Relationship" study to characterize structural features of Sulfamide derivative [RR'NSO(2)NH(2)] as inhibitors, that are required for selective binding of carbonic anhydrase isozymes (CAI and CAII). In the analysis, stepwise multiple linear regression was performed using physiochemical parameters as independent variable and CA-I and CA-II inhibitory activity as dependent variable, respectively. The best multiparametric QSAR model obtained for CA-I inhibitory activity shows good statistical significance (r= 0.9714) and predictability (Q(2)=0.8921), involving the Electronic descriptors viz. Highest Occupied Molecular Orbital, Lowest Unoccupied Molecular Orbital and Steric descriptors viz. Principal moment of Inertia at X axis. Similarly, CA-II inhibitory activity also shows good statistical significance (r=0.9644) and predictability (Q(2)=0.8699) involving aforementioned descriptors. The predictive power of the model was successfully tested externally using a set of six compounds as test set for CA-I inhibitory activity and a set of seven compounds in case of CA-II inhibitory activity with good predictive squared correlation coefficient, r(2)(pred)=0.6016 and 0.7662, respectively. Overview of analysis favours substituents with high electronegativity and less bulk at R and R' positions of the parent nucleus, provides a basis to design new Sulfamide derivatives possessing potent and selective carbonic anhydrase-II inhibitory activity.
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PMID:Quantitative structure activity relationship studies of sulfamide derivatives as carbonic anhydrase inhibitor: as antiglaucoma agents. 1762 76

We report the case of a 75-year-old woman who developed an acute bilateral angle-closure associated with choroidal effusion a day after an uneventful cataract surgery. The same patient had undergone a similarly uneventful cataract surgery two weeks before, under the same protocol, with no postoperative complication in the other eye. Medical treatment, including the use of oral sulfamide-related drugs (acetazolamide), topical beta-blockers and steroids led to a gradual decrease in intraocular pressure (IOP) and choroidal effusion. Despite initial reports suggesting a link between sulfamide-exposure and these rare forms of angle-closure, our report would suggest a more complex pathophysiology behind this intriguing phenomenon. How to cite this article: Hoskens K, Pinto LA, Vandewalle E, Verdonk N, Stalmans I. Bilateral Acute Angle-closure after Intraocular Surgery. J Curr Glaucoma Pract 2014;8(3):113-114.
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PMID:Bilateral Acute Angle-closure after Intraocular Surgery. 2699 22