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 Trypanosomatid and plasmodium parasites are producing a great deal of chronic diseases and affecting hundreds of millions people mainly in developing countries. However, in the last years, such diseases are dramatically disseminating worldwide, due to some factors including vector and human migrations or co-infections in immunosuppressed patients. The current antiprotozoal therapies are unsatisfactory due to their low efficacy, high toxicity and appearance of resistant parasitic strains. Therefore, there is an speedy need to develop new antiprotozoal drugs.
Imidazole-based compounds show good antiprotozoal activity. Our company offers the chemical optimization service - synthesis of a unique 1-(aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazole derivatives for your biological projects, related to developing of antiprotozoal drugs. These novel compounds could be selected from a set of 5,000+ exclusive virtual 1-(aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazoles using our company’s proprietary molecular modeling platform ODDA™.
This set of novel 1-(aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazole derivatives will be synthesized exclusively upon your request.
A recent paper from the Journal of Medicinal Chemistry* showed that authors designed and synthesized a series of imidazole-based compounds structurally related to an antiprotozoal agent with nanomolar activity which they identified recently. Most of these analogs possess micromolar activities against T. b. rhodesiense and L. donovani, nanomolar – against P. falciparum and low nanomolar – against T. cruzi. Compounds 5i, 6a-c and 8b was the most potent:
Compounds 5i, 6a-c, 8b
Design and synthesis of novel 1-(aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazoles is a promising direction in protozoal diseases treatment.
* Francesco Saccoliti at al. Design, Synthesis, and Biological Evaluation of New 1-(Aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazole Derivatives as Antiprotozoal Agents. J. Med. Chem. 2019, Vol. 62(3), pp. 1330−1347, DOI: 10.1021/acs.jmedchem.8b01464.
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