Application In Synthesis of Diphenyl-2-pyridylphosphine. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: Diphenyl-2-pyridylphosphine, is researched, Molecular C17H14NP, CAS is 37943-90-1, about Discovery and Pharmacological Studies of 4-Hydroxyphenyl-Derived Phosphonium Salts Active in a Mouse Model of Visceral Leishmaniasis. Author is Manzano, Jose Ignacio; Cueto-Diaz, Eduardo J.; Olias-Molero, Ana Isabel; Perea, Ana; Herraiz, Tomas; Torrado, Juan J.; Alunda, Jose Maria; Gamarro, Francisco; Dardonville, Christophe.
We report the discovery of new 4-hydroxyphenyl phosphonium salt derivatives active in the submicromolar range (EC50 from 0.04 to 0.28μM, SI > 10) against the protozoan parasite Leishmania donovani. The pharmacokinetics and in vivo oral efficacy of compound 1 [(16-(2,4-dihydroxyphenyl)-16-oxohexadecyl)triphenylphosphonium bromide] in a mouse model of visceral leishmaniasis were established. Compound 1 reduced the parasite load in spleen (98.9%) and liver (95.3%) of infected mice after an oral dosage of four daily doses of 1.5 mg/kg. Mode of action studies showed that compound 1 diffuses across the plasma membrane, as designed, and targets the mitochondrion of Leishmania parasites. Disruption of the energetic metabolism, with a decrease of intracellular ATP levels as well as mitochondrial depolarization together with a significant reactive oxygen species production, contributes to the leishmanicidal effect of 1. Importantly, this compound was equally effective against antimonials and miltefosine-resistant clin. isolates of Leishmania infantum, indicating its potential as antileishmanial lead.
《Discovery and Pharmacological Studies of 4-Hydroxyphenyl-Derived Phosphonium Salts Active in a Mouse Model of Visceral Leishmaniasis》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(Diphenyl-2-pyridylphosphine)Application In Synthesis of Diphenyl-2-pyridylphosphine.
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