On July 22, 2021, Nardella, Flore; Halby, Ludovic; Dobrescu, Irina; Viluma, Johanna; Bon, Corentin; Claes, Aurelie; Cadet-Daniel, Veronique; Tafit, Ambre; Roesch, Camille; Hammam, Elie; Erdmann, Diane; Mairet-Khedim, Melissa; Peronet, Roger; Mecheri, Salah; Witkowski, Benoit; Scherf, Artur; Arimondo, Paola B. published an article.Related Products of 35444-44-1 The title of the article was Procainamide-SAHA Fused Inhibitors of hHDAC6 Tackle Multidrug-Resistant Malaria Parasites. And the article contained the following:
Epigenetic post-translational modifications are essential for human malaria parasite survival and progression through its life cycle. Here, we present new functionalized suberoylanilide hydroxamic acid (SAHA) derivatives that chem. combine the pan-histone deacetylase inhibitor SAHA with the DNA methyltransferase inhibitor procainamide. A three- or four-step chem. synthesis was designed starting from cheap raw materials. Compared to the single drugs, the combined mols. showed a superior activity in Plasmodium and a potent inhibition against human HDAC6, exerting no cytotoxicity in human cell lines. These new compounds are fully active in multidrug-resistant Plasmodium falciparum Cambodian isolates. They target transmission of the parasite by inducing irreversible morphol. changes in gametocytes and inhibiting exflagellation. The compounds are slow-acting and have an additive antimalarial effect in combination with fast-acting epidrugs and dihydroartemisinin. The lead compound decreases parasitemia in mice in a severe malaria model. Taken together, this novel fused mol. offers an affordable alternative to current failing antimalarial therapy. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).Related Products of 35444-44-1
The Article related to procainamide saha fused inhibitor hhdac6 dnmt multidrug resistant plasmodium, Pharmacology: Effects Of Antimicrobials and Parasiticides and other aspects.Related Products of 35444-44-1
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