Receptor interacting protein 1 (RIP1) kinase plays an important role in necroptosis, and inhibitors of the RIP1 kinase are thought to have a potential therapeutic value in the treatment of diseases related to necrosis. Herein, we report the structural optimization of a RIP1 kinase inhibitor, 1-(2,4-dichlorobenzyl)-3-nitro-1H-pyrazole (1a). A number of 1-benzyl-1H-pyrazole derivatives were synth...

The synthesis of new binucleating pyrazole-derived ligands (HL2, HL3) with bulky 2,6-diisopropylphenylimine side arms and backbone phenyl groups at the pyrazole-C4 and/or at the imine-C, which are derivatives from the known ligand HL1, is reported. Crystallographic analyses of three cobalt(II) complexes coordinated by ligands [L1-3]- reveal distinct metal to ligand ratios and different structur...

The carbohydrazide 1 was used as the precursor for the synthesis of a number of new aromatic C-nucleosides containing 1,3,4-oxadiazole 7, [1,3,4]oxadiazolo[2,3-a]isoindole 10b and pyrazole units 18. On the other hand, the thiosemicarbazone 20 was used as the key intermediate for synthesis of 1,3,4-oxadiazole  and 1,2,4-triazole-3-thione derivatives 21 and 23. The antioxidant activities of the p...

Recently described biphenyl analogues of the antituberculosis drug PA-824 displayed improved potencies against M. tuberculosis but were poorly soluble. Heterobiaryl analogues of these, in which the first phenyl ring was replaced with various 5-membered ring heterocycles, were prepared with the aim of identifying potent new candidates with improved aqueous solubility. The compounds were construc...

This work examines theoretically the problem of migration borane groups between nitrogen atoms pyrazolyl rings. We have studied as a model BH2 derivatives pyrazol-1-yl to determine effects substituents on pyrazole ring; also 1-(9-borabicyclo[3.3.1]nonan-9-yl)-1H-pyrazoles compare calculated barriers with experimental ones well steric effects, i.e. how buttressing effect increases rate. The inte...

A novel series of pyrazole derivatives containing imidazo[1,2-a]pyridine D1-D8 moiety has been synthesized. The reaction 2-aminopyridine with 4-phenylphenacyl bromide and 4-bromophenacyl gave the products A1, respectively. These then reacted DMF POCl3 to obtain new aldehyde B B1. two aldehydes were condensed various acetophenone substitutes yield corresponding chalcone C1-C10. Following this, c...