A Practical Green Synthesis and Biological Evaluation of Benzimidazoles Against Two Neglected Tropical Diseases: Chagas and Leishmaniasis
| Autor: | Gildardo Rivera, Luvia Enid Sánchez-Torres, Bimal K. Banik, Benjamín Nogueda-Torres, Selina Samano, Debashis Bandyopadhyay, Juan Carlos Villalobos-Rocha |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
0301 basic medicine
Chagas disease Trypanosoma cruzi Leishmania mexicana Antiprotozoal Agents Disease 01 natural sciences Biochemistry Heating 03 medical and health sciences Antibiotic resistance Amphotericin B Drug Discovery medicine Chagas Disease 0101 mathematics Nifurtimox Microwaves Leishmaniasis Biological evaluation Pharmacology biology Organic Chemistry Green Chemistry Technology biology.organism_classification medicine.disease Virology 010101 applied mathematics 030104 developmental biology Nitroimidazoles Neglected tropical diseases Molecular Medicine Benzimidazoles medicine.drug |
| Zdroj: | Current medicinal chemistry. 24(41) |
| ISSN: | 1875-533X |
| Popis: | Antimicrobial resistance is an ever-increasing problem throughout the world and has already reached severe proportions. Two very common neglected tropical diseases are Chagas' disease and leishmaniasis. Chagas' disease is a severe health problem, mainly in Latin America, causing approximately 50000 deaths a year and millions of people are infected. About 25-30% of the patients infected with Trypanosoma cruzi develop the chronic form of the disease. On the other hand, Leishmaniasis represents complex diseases with an important clinical and epidemiological diversity. It is endemic in 88 countries 72 of which are developing countries and it has been estimated that are 12 million people infected and 350 million are in areas with infection risk. On this basis, research on organic compounds that can be used against these two diseases is an important target. A very simple, green, and efficient protocol is developed in which bismuth nitrate pentahydrate is employed as a Lewis acid catalyst in aqueous media under microwave irradiation for the synthesis of various 2-aryl substituted benzimidazoles from aldehydes and o-phenylenediamine. Other salient features of this protocol include milder conditions, atom-economy, easy extraction, and no wastes. Nine 1H-benzimidazole derivatives (1-9) with substituents at positions 2 and 5 were synthesized and the structure of the compounds was elucidated by spectroscopic methods. The compounds were screened to identify whether they posses pharmacological activity against Chagas' disease and leishmaniasis. Compound 8 showed better activity than the control Nifurtimox against INC-5 Trypanosoma cruzi strain whereas compounds 3 and 9 have demonstrated potent leshmanicidal activity. A systematic green synthetic procedure and in vitro biological evaluation of nine 1H-benzimidazoles are described. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|