Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγnull Mouse Model of Malaria was written by Nchinda, Aloysius T.;Le Manach, Claire;Paquet, Tanya;Gonzalez Cabrera, Diego;Wicht, Kathryn J.;Brunschwig, Christel;Njoroge, Mathew;Abay, Efrem;Taylor, Dale;Lawrence, Nina;Wittlin, Sergio;Jimenez-Diaz, Maria-Belen;Santos Martinez, Maria;Ferrer, Santiago;Angulo-Barturen, Inigo;Lafuente-Monasterio, Maria Jose;Duffy, James;Burrows, Jeremy;Street, Leslie J.;Chibale, Kelly. And the article was included in Journal of Medicinal Chemistry in 2018.Reference of 5469-70-5 This article mentions the following:
Optimization of a chem. series originating from whole-cell phenotypic screening against the human malaria parasite, Plasmodium falciparum, led to the identification of two promising 2,6-disubstituted imidazopyridine compounds, 43 and 74. These compounds exhibited potent activity against asexual blood stage parasites that, together with their in vitro absorption, distribution, metabolism, and excretion (ADME) properties, translated to in vivo efficacy with clearance of parasites in the PfSCID mouse model for malaria within 48 h of treatment. In the experiment, the researchers used many compounds, for example, 3-Aminopyridazine (cas: 5469-70-5Reference of 5469-70-5).
3-Aminopyridazine (cas: 5469-70-5) belongs to pyridazine derivatives. The pyridazine derivatives are mostly present in biologically active compounds and are also present with different pharmacophores. Pyridazine can act as a hydrogen bond acceptor to improve the physicochemical properties of drug molecules by increasing their water solubility, and has a high affinity for complexing with targets due to its dipole moment.Reference of 5469-70-5
Referemce:
Pyridazine – Wikipedia,
Pyridazine | C4H4N2 – PubChem