Solid Supported Synthesis of Polyamines with Antimycobacterial Activity

GUILLERMO R. LABADIE AND MITCHELL A. AVERY

Sao Pedro - Brasil

Simposio; The 3rd Brazilian Symposium on Medicinal Chemistry - BrazMedChem2006; 2006

Divisão de Química Medicinal (MD) da Sociedade Brasileira de Química (SBQ).

Tuberculosis incidence has been increasing substantially over the past decade, but no specific drugs have been discovered in 40 years. Almost 2 billion people, one third of world population, harbours the bacillus that causes tuberculosis with the latent risk of developing an active disease and spreading to others. The necessity of long term treatment of common medications and the development of resistance make imperative to find of new medications. Also, other mycobacterium has an increasing impact as AIDS related opportunistic infection. As a part of program to develop new chemotherapies against parasitic diseases, we have selected polyamins synthesis and uptake as a target. Libraries of diamines and polyamines have been prepared by parallel solid support synthesis, being screened against different parasites. When those compounds were tested towards Mycobacterium intracellulare, they have shown activity at low micromolar concentration. The synthesis of the libraries and the structural-activity relationship will be discussed.