Running title: Antimalarial activity of peptido sulfonyl fluorides

Broad-spectrum antimalarial activity of peptido sulfonyl fluorides, a new class of proteasome inhibitors.

Despite declining numbers of cases and deaths, malaria remains a major public health problem in many parts of the world. Today, case management relies heavily on a single class of antimalarial compounds: artemisinins. Hence, development of resistance against artemisinins may destroy current malaria control strategies. Beyond malaria control are elimination and eradication programs that will req...

One-pot palladium-catalyzed synthesis of sulfonyl fluorides from aryl bromides.

A mild, efficient synthesis of sulfonyl fluorides from aryl and heteroaryl bromides utilizing palladium catalysis is described. The process involves the initial palladium-catalyzed sulfonylation of aryl bromides using DABSO as an SO2 source, followed by in situ treatment of the resultant sulfinate with the electrophilic fluorine source NFSI. This sequence represents the first general method for...

One-pot palladium-catalyzed synthesis of sulfonyl fluorides from aryl bromides† †Electronic supplementary information (ESI) available: Experimental details and supporting characterisation data. See DOI: 10.1039/c6sc03924c Click here for additional data file.

NOVEL AZOLYLALKYLTHIO, -SULFOXY, AND -SULFONYL COMPOUNDS WITH ANTIPICORNAVIRAL ACTIVITY

A novel series of azolylalkylthio, -sulfoxy, and-sulfonyl compounds was designed, synthesized, and evaluated for antipicornaviral activity. Two compounds (4i and 4 1) exhibited significant activity against various serotypes of human rhinovirus (HRV). It was found that incorporation of hydrophobic azoles such as 3-methylisoxazole or 4-methylthiazole led to increased activity. In addition, ac...

Sucrose and KF quenching system for solution phase parallel synthesis

The KF, sucrose (table sugar) exploited as quenching system in solution phase parallel synthesis. Excess of electrophiles were covalently trapped with hydroxyl functionality of sucrose and due to polar nature of sucrose derivative was solubilize in water. Potassium fluoride used to convert various excess electrophilic reagents such as acid chlorides, sulfonyl chlorides, isocyanates to correspon...