Macrocycles as potential therapeutic agents in neglected diseases

Author:

Peña Stella1,Scarone Laura1,Serra Gloria1

Affiliation:

1. Cátedra de Química Farmacéutica, (DQO), Facultad de Química, Universidad de la República, Gral. Flores 2124, Montevideo, CP 11800, Uruguay

Abstract

Macrocycles possess desirable properties that make them promising candidates for the discovery of novel drugs. They present structural features to favor bioactive conformations, selectivity to the receptors, cell permeability and metabolic stability. More effective and nontoxic drugs to cure human African trypanosomiasis, Leishmaniasis and Chagas disease are needed, especially because resistance has been detected. Therefore, major efforts should be made for investigation in new bioactive compounds exhibiting different mechanisms of action. Macrocycles might fulfill the expectations for the development of new drugs to treat those diseases. In the current review, we focus on macrocycles exhibiting biological activities as antitrypanosomal and/or antileishmanial. The isolation, synthetic and biological studies of this class of compounds published from 2005 to 2014 are summarized.

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

Reference105 articles.

1. Macrocyclic Drugs and Clinical Candidates: What Can Medicinal Chemists Learn from Their Properties?

2. The exploration of macrocycles for drug discovery — an underexploited structural class

3. Macrocycles in new drug discovery

4. World Health Organization. Human African trypanosomiasis (HAT) control. www.afro.who.int/en/clusters-a-programmes/dpc/neglected-tropical-diseases/programme-components/human-african-trypanosomiasis-control.html.

5. World Health Organization. Trypanosomiasis, human African (sleeping sickness). www.who.int/mediacentre/factsheets/fs259/en/.

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