28788-62-7Relevant articles and documents
O-Alkyl Hydroxamates Display Potent and Selective Antileishmanial Activity
Corpas-López, Victoriano,Tabraue-Chávez, Mavys,Sixto-López, Yudibeth,Panadero-Fajardo, Sonia,Alves De Lima Franco, Fernando,Domínguez-Seglar, José F.,Morillas-Márquez, Francisco,Franco-Montalbán, Francisco,Díaz-Gavilán, Mónica,Correa-Basurto, José,López-Viota, Julián,López-Viota, Margarita,Pérez Del Palacio, José,De La Cruz, Mercedes,De Pedro, Nuria,Martín-Sánchez, Joaquina,Gómez-Vidal, José A.
, p. 5734 - 5751 (2020)
Leishmania (L.) infantum causes visceral, cutaneous, and mucosal leishmaniasis in humans and canine leishmaniasis in dogs. Herein, we describe that O-alkyl hydroxamate derivatives displayed potent and selective in vitro activity against the amastigote stage of L. infantum while no activity was observed against promastigotes. Compound 5 showed potent in vivo activity against L. infantum. Moreover, the combination of compound 5 supported on gold nanoparticles and meglumine antimoniate was also effective in vivo and improved the activity of these compounds compared to that of the individual treatment. Docking studies showed that compound 5 did not reach highly conserved pocket C and established interactions with the semiconserved residues V44, A45, R242, and E243 in pocket A of LiSIR2rp1. The surface space determined by these four amino acids is not conserved in human sirtuins. Compound 5 represents a new class of selective ligands with antileishmanial activity.
Ni-Catalyzed Direct Carboxylation of Aryl C?H Bonds in Benzamides with CO2
Li, Bin,Pei, Chunzhe,Wang, Baiquan,Zong, Jiarui
supporting information, (2021/12/08)
The direct carboxylation of inert aryl C?H bond catalyzed by abundant and cheap nickel is still facing challenge. Herein, we report the Ni-catalyzed direct carboxylation of aryl C?H bonds in benzamides under 1 atm of CO2 to afford various methyl carboxylates or phthalimides, dealing with different post-processing. The reaction displays excellent functional group tolerance and affords moderate to high carboxylation yields under mild conditions. Detail mechanistic studies suggest that a Ni(0)?Ni(II)?Ni(I) catalytic cycle may be involved in this reaction. (Figure presented.).
Myobacterium Tuberculosis-Thioredoxin Reductase Inhibitor as an Antitubercular Agent
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Paragraph 0103; 0112, (2020/05/06)
The invention relates to Mycobacterium tuberculosis-thioredoxin reductase inhibitors, processes for the preparation thereof, drugs containing said compounds, and the use of said compounds for manufacturing drugs.