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Sulfonamide inhibition studies of the β carbonic anhydrase from Drosophila melanogaster.

Abstract：

:An inibition study of the β-carbonic anhydrase (CA, EC 4.2.1.1) DmBCA from the insect Drosophila melanogaster with sulfonamides and sulfamates is reported. Among the panel of 40 investigated compounds, the best DmBCA inhibitors were the sulfonylated benzenesulfonamides and ethoxzolamide, which showed inhibition constants in the range of 65.3-138 nM. Methazolamide and sulthiame were also effective inhibitors with KIs ranging between 237 and 249 nM, whereas most of the simple aromatic/heterocyclic sulfonamides showed inhibition constants in the range of 0.47-6.40 μM. Topiramate, zonisamide and saccharine did not inhibit DmBCA. As orthologs of this mitochondrial CA are found in many insect species involved in the spread of various diseases, inhibitors interfering with their activity may be of interest for developing insecticides with an alternative mechanism of action to the presently used agents, for which many insects developed extensive resistance.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Syrjänen L,Parkkila S,Scozzafava A,Supuran CT

doi

10.1016/j.bmcl.2014.04.117

subject

Has Abstract

pub_date

2014-07-01 00:00:00

pages

2797-801

issue

13

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(14)00484-3

journal_volume

24

pub_type

杂志文章

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