73736-50-2
Chemical Structure
Desmethylastemizole
Synonym(s): O-Demethylastemizole
- CAS No.: 73736-50-2
- Formula:C27H29FN4O
- Molecular Weight:444.54
IUPAC Name: 4-(2-(4-((1-(4-fluorobenzyl)-1H-benzo[d]imidazol-2-yl)amino)piperidin-1-yl)ethyl)phenol
InChIKey: LAGYWHSFHIMTPE-UHFFFAOYSA-N
SMILES: FC(C=C1)=CC=C1CN2C3=CC=CC=C3N=C2NC4CCN(CCC5=CC=C(O)C=C5)CC4
Biological Activity: Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC50 of 0.12, 0.11 and 0.06 μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K+ channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research[1][2][3].
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Desmethylastemizole | Desmethylastemizole (O-Demethylastemizole) , a metabolite of Astemizole (HY-12532), is a β-hematin (βH) inhibitor. Desmethylastemizole has an antiplasmodium activity against P. falciparum with IC50 of 0.12, 0.11 and 0.06 μM for Pf3D7, PfDd2, and PfItG strains, respectively. Desmethylastemizole is also a Histamine H1 receptor antagonist. Desmethylastemizole significantly blocks hERG K+ channels and also inhibits histone-lysine N-methyltransferase EZH2 activity. Desmethylastemizole can be used for long QT syndrome and malaria research. | |||||||||||||||||||||
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- [1]. Kamei C, Mio M, Izushi K, et al. Antiallergic effects of major metabolites of astemizole in rats and guinea pigs. Arzneimittelforschung. 1991;41(9):932-936. [Content Brief]
- [2]. Kumar M, Okombo J, Mambwe D, et al. Multistage Antiplasmodium Activity of Astemizole Analogues and Inhibition of Hemozoin Formation as a Contributor to Their Mode of Action. ACS Infect Dis. 2019;5(2):303-315. [Content Brief]
- [3]. Zhou Z, et al. Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. J Cardiovasc Electrophysiol. 1999 Jun;10(6):836-43. [Content Brief]
Keywords
