Synthesis of 4-aminoquinoline analogues and their platinum(II) complexes as new antileishmanial and antitubercular agents.

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.

Synthesis, characterization, and cytotoxic activity of novel platinum (II) complexes derived from n-benzyl-ethylenediamine and oxalate.

This work describes the synthesis and characterization of three novel complexes derived from N-benzyl-ethylenediamine and oxalate. Precursor compounds were synthesized by reacting N-benzyl-ethylenediamine with K(2)PtCl(4). Subsequent substitution of chlorides by oxalate led to the final products. Elemental analysis and the infrared, (1)H, (13)C, and (195)Pt NMR spectra of these complexes were provided. The cytotoxic activities were investigated against human non-small cell lung carcinoma (A(549)), mouse non-metastatic cell skin melanoma (B16-F1), mouse metastatic cell skin melanoma (B16-F10), human cell breast adenocarcinoma (MDA-MB-231) and normal cell lines such as baby hamster cell kidney (BHK-21), hamster cell ovary (CHO) and compared to cisplatin and carboplatin under the same experimental conditions. The presence of oxalate as a leaving group conferred an interesting cytotoxicity profile to the complexes in the tested cell lines.