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  • Title: Carbonic anhydrase I and II activation with mono- and dihalogenated histamine derivatives.
    Author: Saada MC, Vullo D, Montero JL, Scozzafava A, Winum JY, Supuran CT.
    Journal: Bioorg Med Chem Lett; 2011 Aug 15; 21(16):4884-7. PubMed ID: 21742491.
    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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