The New Pyrazolyltetrazole Derivative MSN20 Is Effective via Oral Delivery against Cutaneous Leishmaniasis
| Autor: | Eduardo Caio Torres-Santos, Maurício S. dos Santos, Viviane dos Santos Faiões, Edézio Ferreira Cunha-Júnior, Marilene Marcuzzo do Canto Cavalheiro, Alice M. R. Bernardino |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Oral treatment
Antiprotozoal Agents Administration Oral Leishmaniasis Cutaneous Tetrazoles Allopurinol Pharmacology Parasite load Inhibitory Concentration 50 Mice Structure-Activity Relationship Cutaneous leishmaniasis medicine Animals Experimental Therapeutics Pharmacology (medical) Amastigote IC50 Leishmania amazonensis biology business.industry Leishmaniasis medicine.disease biology.organism_classification Infectious Diseases Immunology Pyrazoles business medicine.drug |
| Zdroj: | Antimicrobial Agents and Chemotherapy. 58:6290-6293 |
| ISSN: | 1098-6596 0066-4804 |
| Popis: | An orally delivered, safe and effective treatment for leishmaniasis is an unmet medical need. Azoles and the pyrazolylpyrimidine allopurinol present leishmanicidal activity, but their clinical efficacies are variable. Here, we describe the activity of the new pyrazolyltetrazole hybrid, 5-[5-amino-1-(4′-methoxyphenyl)1H-pyrazole-4-yl]1H-tetrazole (MSN20). MSN20 showed a 50% inhibitory concentration (IC 50 ) of 22.3 μM against amastigotes of Leishmania amazonensis and reduced significantly the parasite load in infected mice, suggesting its utility as a lead compound for the development of an oral treatment for leishmaniasis. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|