Application In Synthesis of 3,3,3-Trifluoropropan-1-olOn November 11, 2021 ,《DNDI-6148: A Novel Benzoxaborole Preclinical Candidate for the Treatment of Visceral Leishmaniasis》 appeared in Journal of Medicinal Chemistry. The author of the article were Mowbray, Charles E.; Braillard, Stephanie; Glossop, Paul A.; Whitlock, Gavin A.; Jacobs, Robert T.; Speake, Jason; Pandi, Bharathi; Nare, Bakela; Maes, Louis; Yardley, Vanessa; Freund, Yvonne; Wall, Richard J.; Carvalho, Sandra; Bello, Davide; Van den Kerkhof, Magali; Caljon, Guy; Gilbert, Ian H.; Corpas-Lopez, Victoriano; Lukac, Iva; Patterson, Stephen; Zuccotto, Fabio; Wyllie, Susan. The article conveys some information:
Visceral leishmaniasis (VL) is a parasitic disease endemic across multiple regions of the world and is fatal if untreated. Current therapies are unsuitable, and there is an urgent need for safe, short-course, and low-cost oral treatments to combat this neglected disease. The benzoxaborole chemotype has previously delivered clin. candidates for the treatment of other parasitic diseases. Here, we describe the development and optimization of this series, leading to the identification of compounds with potent in vitro and in vivo antileishmanial activity. The lead compound (DNDI-6148) combines impressive in vivo efficacy (>98% reduction in parasite burden) with pharmaceutical properties suitable for onward development and an acceptable safety profile. Detailed mode of action studies confirm that DNDI-6148 acts principally through the inhibition of Leishmania cleavage and polyadenylation specificity factor (CPSF3) endonuclease. As a result of these studies and its promising profile, DNDI-6148 has been declared a preclin. candidate for the treatment of VL. The experimental process involved the reaction of 3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2Application In Synthesis of 3,3,3-Trifluoropropan-1-ol)
3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2) is a important organic intermediate. It can be used in agrochemical, pharmaceutical and dyestuff field.Application In Synthesis of 3,3,3-Trifluoropropan-1-ol
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