4329-75-3Relevant articles and documents
Synthesis, computational studies, antimycobacterial and antibacterial properties of pyrazinoic acid-isoniazid hybrid conjugates
Panda, Siva S.,Girgis, Adel S.,Mishra, Bibhuti B.,Elagawany, Mohamed,Devarapalli, Venkatasai,Littlefield, William F.,Samir, Ahmed,Fayad, Walid,Fawzy, Nehmedo G.,Srour, Aladdin M.,Bokhtia, Riham M.
, p. 20450 - 20462 (2019/07/09)
Benzotriazole and microwave mediated syntheses led to a new set of hybrid conjugates of pyrazinoic acid with isoniazid via amino acid linkers in excellent yields with retention of chirality. Microbiological screening of the synthesized conjugates revealed an exceptionally high activity against some of the pathogenic bacterial strains at low concentrations. Promising antimycobacterial properties were observed against tuberculous and non-tuberculous mycobacteria. Robust molecular models (2D-QSAR and 3D-pharmacophore) support the observed biological properties. Safety profile of the synthesized conjugates against human normal cell (RPE1) was evaluated by MTT technique.
Synthesis of novel 5-amino-1-aroylpyrazoles
Quiroga, Jairo,Portilla, Jaime,Abonía, Rodrigo,Insuasty, Braulio,Nogueras, Manuel,Cobo, Justo
experimental part, p. 5943 - 5945 (2009/04/11)
A series of 5-amino-1-aroylpyrazoles 3 are synthesized directly by the reaction of β-aminocrotononitrile 1 with some structures containing the hydrazine moiety (X-NHNH2) 2 by refluxing ethanol in presence of sodium acetate. When semicarbazide 3i was used (X = CONH2), the reaction afforded the unexpected 7-aminopyrazolo[1,5-a]pyrimidine 4.
Migration of an acyl group in the pyrazole system: Synthesis of 1-acyl-3-hydroxy-1H-pyrazoles and related derivatives. A new preparation of N,N′-diacylhydrazines
Kepe, Vladimir,Pozgan, Franc,Golobic, Amalija,Polanc, Slovenko,Kocevar, Marijan
, p. 2813 - 2816 (2007/10/03)
A new general method for the synthesis of 1-acyl-3-hydroxy-1H-pyrazoles 5a-f and related derivatives 5g-i starting from 4-ethoxymethylene-2-phenyloxazol-5(4H)-one (1) and hydrazides, 4-phenylsemicarbazide, 4-phenylthiosemicarbazide and benzyl carbazate in boiling dioxane is described. The method includes a migration of an acyl or related unit. The X-ray study and NMR spectroscopic examination confirmed the structure of the products. A one-pot synthesis of N,N′-diacylhydrazines from hydrazides by the assistance of oxazolone 1 is also presented.