7056-72-6Relevant articles and documents
Designer ligands. VIII. Thermal and microwave-assisted synthesis of silver(I)-selective ligands
Daubinet, Andre,Kaye, Perry T.
, p. 3207 - 3217 (2002)
Thermal and microwave-assisted methods have been used for preparing multidentate malonamide derivatives as silver(I)-selective ligands, the latter methodology providing convenient and rapid access to the target compounds in yields of up to 92%. Metal extr
Synthesis of symmetrically substituted 3,3-dibenzyl-4-hydroxy-3,4-dihydro- 1H-quinolin-2-ones, as novel quinoline derivatives with antibacterial activity
Ferretti, Matías D.,Neto, Alexandre T.,Morel, Ademir F.,Kaufman, Teodoro S.,Larghi, Enrique L.
, p. 253 - 266 (2014/06/09)
A novel series of symmetrically substituted 3,3-dibenzyl-4-hydroxy-3,4- dihydro-1H-quinolin-2-ones was synthesized and tested as antimicrobials. The minimum inhibitory concentration (MIC) values of the most active heterocycles were slightly higher than those exhibited by levofloxacin, employed as comparator. Structural factors affecting the activity were explored along three diversification points, including the substituents of the aromatic rings of the 3-benzyl moieties, as well as the functionalization of both, the homocyclic ring of the heterocycle and the quinolonic nitrogen atom. 6-Chloro and 3,3-bis(4′-chlorobenzyl) derivatives showed the lower MIC values. Optimally substituted heterocycles were synthesized, which exhibited enhanced activity.
Design and synthesis of bis-amide and hydrazide-containing derivatives of malonic acid as potential HIV-1 integrase inhibitors
Sechi, Mario,Azzena, Ugo,Delussu, Maria Paola,Dallocchio, Roberto,Dessi, Alessandro,Cosseddu, Alessia,Pala, Nicolino,Neamati, Nouri
experimental part, p. 2442 - 2461 (2009/04/05)
HIV-1 integrase (IN) is an attractive and validated target for the development of novel therapeutics against AIDS. In the search for new IN inhibitors, we designed and synthesized three series of bis-amide and hydrazide-containing derivatives of malonic acid. We performed a docking study to investigate the potential interactions of the title compounds with essential amino acids on the IN active site.