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Antimicrobial Agents and Chemotherapy, March 2005, p. 1076-1080, Vol. 49, No. 3
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.3.1076-1080.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.

Synthesis and Antileishmanial Activities of Novel 3-Substituted Quinolines

André Gustavo Tempone,1,2* Ana Cláudia Melo Pompeu da Silva,3 Carlos Alberto Brandt,4 Fernanda Scalzaretto Martinez,1 Samanta Etel Treiger Borborema,1 Maria Amélia Barata da Silveira,3 and Heitor Franco de Andrade Jr.1

Laboratorio de Parasitologia, Divisao de Biologia Medica, Instituto Adolfo Lutz,2 Laboratorio de Protozoologia, Instituto de Medicina Tropical,1 Departamento de Farmácia, Faculdade de Ciências Farmacêuticas, Universidade de Sao Paulo,3 Instituto Butantan, Sao Paulo, Brazil4

Received 16 July 2004/ Returned for modification 25 August 2004/ Accepted 12 November 2004

The antileishmanial efficacy of four novel quinoline derivatives was determined in vitro against Leishmania chagasi, using extracellular and intracellular parasite models. When tested against L. chagasi-infected macrophages, compound 3b demonstrated 8.3-fold greater activity than did the standard pentavalent antimony. No significant activity was found for compounds 3a, 4a, and 4b. The antilesihmanial effect of compound 3b was independent of host cell activation, as demonstrated by nitric oxide production. Ultrastructural studies of promastigotes treated with compound 3b showed mainly enlarged mitochondria, with matrix swelling and reduction in the number of cristae. Synthetic analogues based on the quinoline ring structure, already an established template for antiparasitic drugs, could provide further useful compounds.

* Corresponding author. Mailing address: Lab. Parasitologia, Div. Biologia Medica Medical, Instituto Adolfo Lutz, Av. Dr. Arnaldo 355, 8° andar CEP, 01246-000 Sao Paulo, Brazil. Phone: 55 3066-7010. Fax: 55 3088-5237. E-mail: atempone{at}ial.sp.gov.br.

Antimicrobial Agents and Chemotherapy, March 2005, p. 1076-1080, Vol. 49, No. 3
0066-4804/05/$08.00+0     doi:10.1128/AAC.49.3.1076-1080.2005
Copyright © 2005, American Society for Microbiology. All Rights Reserved.





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