5. Mitt.: Über den Einfluß von Ethambutol auf den endogenen Stoffwechsel von M. smegmatis / The Endogenous Metabolism of Mycobacteria V: The Influence of Ethambutol on the Endogenous Metabolism of M. smegmatis

Reutgen, H; Iwainsky, H

doi:10.1515/znb-1972-1125

Cited by 4 publications

References 2 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Antimycobacterial Agents

Sensi¹,

Grassi²

2003

Burger's Medicinal Chemistry and Drug Discovery

View full text Add to dashboard Cite

A few decades ago, the idea that a treatise on chemotherapy, to be published in this millennium, could include a chapter on antimycobacterial agents was probably considered acceptable mainly to illustrate the history of a strong successful fight against some human diseases present in the world since antiquity, such as tuberculosis and leprosy. In fact, starting from the middle of the last century, the introduction of chemotherapy for mycobacterial infections, together with improvements in the hygienic and nutritional conditions, brought about a dramatic decrease in the mortality and morbidity of these illnesses, with a trend toward their elimination. Unfortunately, these successes notwithstanding, mycobacterial infections still require particular attention as a worldwide, challenging health problem. In particular, in the last few years, an unexpected resurgence of tuberculosis has occurred in industrialized countries, probably because of the spread of HIV infection and the increasing and uncontrolled waves of immigration. Moreover, the emergence of multidrug resistant strains of Mycobacterium tuberculosis has made the older therapies largely ineffective. This chapter has been written for the medicinal chemist who wants to be updated on the situation in this area. The present knowledge of the biology of the pathogens, the mycobacteria, has been reviewed, taking into account the recent information on the genome sequence of M. tuberculosis and M. leprae. It also will review the information on the pathogenesis and epidemiology of the mycobacterial diseases. The antimycobacterial drugs used in therapy have been described in detail, mentioning some aspects of their discovery, but particularly their in vitro and in vivo activity, their mechanism of action, their side effects, and the general structure‐activity relationships in the frame of the chemical class to which they belong. Their use in therapy has been considered and evaluated when combined with other antimycobacterial drugs, when the combination is important for an improvement of efficacy and a decrease of probability of resistant strains selection. Some products in the early stage of development, as a starting point for new drugs that are needed, possibly acting on novel targets of the pathogens are also discussed.

show abstract