1.
Bioorg Med Chem Lett
; 17(15): 4154-7, 2007 Aug 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-17555960
RESUMO
Several analogues of the potent anthelmintic praziquantel were prepared with variation in the aromatic ring. The biological activity of these analogues was evaluated and compared against known analogues. Amination of the ring was tolerated while other variations were not. These results have important implications for drug development for schistosomiasis.
Assuntos
Anti-Helmínticos/química , Praziquantel/análogos & derivados , Animais , Anti-Helmínticos/farmacologia , Avaliação Pré-Clínica de Medicamentos , Espectroscopia de Ressonância Magnética , Praziquantel/farmacologia , Schistosoma mansoni/efeitos dos fármacos
2.
Bioorg Med Chem Lett
; 15(10): 2621-3, 2005 May 16.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15863329
RESUMO
Synthesis of pyrrolo[2,1-c][1,4]benzodiazepines via azido reductive cyclization process employing FeCl3-NaI reagent system. This methodology has been extended for the preparation of new nicotinamido-pyrrolobenzodiazepine hybrids linked through piperazino-alkane-oxy spacers that exhibit good DNA binding affinity.