Twenty-three (3-nitrotriazole/2-nitroimidazole)-based amides and sulfonamides were 20 screened for antitubercular activity in aerobic Mycobacterium tuberculosis H37Rv (Mtb H37Rv), 21 by using the BacTiter-GloTM Microbial Cell Viability (BTG) assay. In general, 3-nitrotriazole22 based sulfonamides demonstrated anti-TB activity, whereas 3-nitrotriazole-based amides and 223 nitroimidazole-based am...

N,N-dialkoxyamides 1c, a virtually unstudied member of the new class of anomeric amides, amides bearing two electronegative atoms at nitrogen, have been synthesised in useful yields directly from hydroxamic esters using phenyliodine(III)bis(trifluoroacetate) (PIFA). Infrared carbonyl stretch frequencies and carbonyl (13)C NMR properties have been reported, which support strong inhibition of ami...

The S' subsite specificity of bovine trypsin has been studied by partitioning of o-nitrophenylsu1fenyl-Larginyl-trypsin (formed using o-nitrophenylsulfenyl-L-arginine alkyl esters as acyl donors) between various amino acid-derived nucleophiles and water. The data obtained from spectrophotometric measurements confirmed a preference of trypsin for arginine residues in the Pi-position, which is le...

The reaction of glycine-N-methyl amide with paraformaldehyde in the presence of ytterbium triflate (1 mol%) leads to a novel cage structure 6 which is chiral at nitrogen. Single crystal X-ray analysis and DFT calculations suggest this cage structure is rigid and adopts a single low energy conformation. Use of single enantiomer α-amino amides results in two diastereomeric tertiary amines that di...

Simple and efficient procedures for palladium-catalyzed cross-coupling reactions of N-substituted 4-bromo-7-azaindole (1H-pyrrole[2,3-b]pyridine), with amides, amines, amino acid esters and phenols through C-N and C-O bond formation have been developed. The C-N cross-coupling reaction of amides, amines and amino acid esters takes place rapidly by using the combination of Xantphos, Cs(2)CO(3), d...

A scalable CuI-catalyzed Goldberg C–N coupling between aryl iodides and amides is reported either in DESs or water.

microwave-assisted three component cyclocondensation reactions of aldehydes, amides and dienophiles in the presence of acetic anhydride and para-toluenesulfonic acid as a catalyst to afford the highly substituted cyclohexene derivatives, in relatively good yields after several minutes are reported.