title: Synthesis of 4-aminoquinoline analogues and their platinum(II) complexes as new antileishmanial and antitubercular agents.
abstract: A series of 4-amino-7-chloroquinoline derivatives were synthesized by the reaction of 4,7-dichloro-quinoline with the corresponding diamine and then with propargyl bromide. In addition, platinum(II) complexes were obtained by reacting some of the organic derivatives with K(2)PtCl(4). Several of the synthesized compounds displayed antituberculosis activities. Compound 3 was 47.5 times more active than amphotericin B against Leishmania chagasi (IC(50)=0.04 μg/mL). Compounds 5, 6, 7, 9, 10, 11 and 13 presented promising results against Mycobacterium tuberculosis, with MIC values ranging from 12.5 to 15.6 μg/mL, comparable to the "first and second line" drugs used to treat tuberculosis.
authors: Departamento de Química, ICE, Universidade Federal de Juiz de Fora, Campus Universitário, Juiz de Fora, MG 36036-900, Brazil.
authors: Arturene M L
authors: AM
authors: Carmo
authors: Flávia M C
authors: FM
authors: Silva
authors: Patrícia A
authors: PA
authors: Machado
authors: Ana P S
authors: AP
authors: Fontes
authors: Fernando R
authors: FR
authors: Pavan
authors: Clarice Q F
authors: CQ
authors: Leite
authors: Sergio R de A
authors: SR
authors: Leite
authors: Elaine S
authors: ES
authors: Coimbra
authors: Adilson D
authors: AD
authors: Da Silva