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KOSK-Katalyse og organisk syntetisk kjemi

Synthesis of agelasines and evaluation of their antimycobacterial activity

Awarded: NOK 3.1 mill.

Tuberculosis (TB) is the major cause of death from a single infectious agent among adults in developing countries and there has been a revival of TB in the industrialized world. Multidrug-resistant tuberculosis defined as resistance to the two most import ant drugs, isoniazid and rifampicin, is a growing. Ca I 3 of the world population is infected with Mycobacterium Tuberculosis even though most of them only carry a dormant infection. There are ca. 8 mill new cases of TB each year, and it has been e stimated that ca. 30 million people will die from tuberculosis in about 10 years. There is an urgent need for new antimycobacterial agents, but no new chemotherapeutic agent directed specifically against TB have been introduced for the last 25-30 years. Agelasines belong to a group of 7,9-dialkylpurinium salts isolated from the marine sponges. The purine 7-substituent carries a diterpenoide substituent. Agelasine F exhibits antimycobacterial activity. In this project we will synthesize a number of other Agelasines and evaluate their ability to inhibit Mycobacterium Tuberculosis and hence have a potential as drugs against TB. Stereo and regioselective allylic rearrangements and oxidations are important reactions in the planned side chain syntheses.

Funding scheme:

KOSK-Katalyse og organisk syntetisk kjemi

Thematic Areas and Topics

No thematic area or topic related to the project