Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1361750 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
Mono- and dihalogenated histamine derivatives incorporating fluorine, chlorine and bromine have been prepared together with the corresponding boc-protected compounds at the aminoethyl group. They have been investigated as activators of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1). The cytosolic human (h) isoforms hCA I and II were moderately activated by the boc-protected halogenated histamines and very effectively activated by the deprotected ones. Low nanomolar and subnanomolar hCA I and II activators have been detected for the first time, starting from histamine as lead which has an affinity of 2 μM against isoform I and of 125 μM against hCA II.
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Related Topics
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Organic Chemistry
Authors
Mohamed-Chiheb Saada, Daniela Vullo, Jean-Louis Montero, Andrea Scozzafava, Jean-Yves Winum, Claudiu T. Supuran,