Barea C., Pabon A., Castillo D., Zimic M., Quiliano M., Galiano S., Perez-Silanes S., Monge A., Deharo Eric, Aldana I. (2011). New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities. Bioorganic and Medicinal Chemistry Letters, 21 (15), p. 4498-4502. ISSN 0960-894X.
Titre du document
New salicylamide and sulfonamide derivatives of quinoxaline 1,4-di-N-oxide with antileishmanial and antimalarial activities
Barea C., Pabon A., Castillo D., Zimic M., Quiliano M., Galiano S., Perez-Silanes S., Monge A., Deharo Eric, Aldana I.
Source
Bioorganic and Medicinal Chemistry Letters, 2011,
21 (15), p. 4498-4502 ISSN 0960-894X
Continuing with our efforts to identify new active compounds against malaria and leishmaniasis, 14 new 3-amino-1,4-di-N-oxide quinoxaline-2-carbonitrile derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum Colombian FCR-3 strain and Leishmania amazonensis strain MHOM/BR/76/LTB-012A. Further computational studies were carried out in order to analyze graphic SAR and ADME properties. The results obtained indicate that compounds with one halogenous group substituted in position 6 and 7 provide an efficient approach for further development of antimalarial and antileishmanial agents. In addition, interesting ADME properties were found.
Plan de classement
Sciences fondamentales / Techniques d'analyse et de recherche [020]
;
Entomologie médicale / Parasitologie / Virologie [052]
