3-Aminothiophene-2-Acylhydrazones: Non-Toxic, Analgesic and Anti-Inflammatory Lead-Candidates
| Autor: | Lídia Moreira Lima, Christian Tadeo Moreno Reyes, Gildardo Rivera, Marina Amaral Alves, Yolanda Karla Cupertino da Silva, Magna Suzana Alexandre Moreira, Eliezer J. Barreiro |
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| Jazyk: | angličtina |
| Rok vydání: | 2014 |
| Předmět: |
Male
medicine.drug_class Analgesic Anti-Inflammatory Agents Pharmaceutical Science Arthritis Pharmacology Anti-inflammatory Article Analytical Chemistry lcsh:QD241-441 privileged structure Mice lcsh:Organic chemistry Oral administration Drug Discovery medicine Potency Animals Physical and Theoretical Chemistry anti-inflammatory Analgesics Chemistry Organic Chemistry Hydrazones toxicity analgesic medicine.disease arthritis Chemistry (miscellaneous) Toxicity Molecular Medicine acylhydrazone |
| Zdroj: | Molecules Volume 19 Issue 6 Pages 8456-8471 Molecules, Vol 19, Iss 6, Pp 8456-8471 (2014) |
| ISSN: | 1420-3049 |
| DOI: | 10.3390/molecules19068456 |
| Popis: | Different chemotypes are described as anti-inflammatory. Among them the N-acylhydrazones (NAH) are highlighted by their privileged structure nature, being present in several anti-inflammatory drug-candidates. In this paper a series of functionalized 3-aminothiophene-2-acylhydrazone derivatives 5a–i were designed, synthesized and bioassayed. These new derivatives showed great anti-inflammatory and analgesic potency and efficacy. Compounds 5a and 5d stand out in this respect, and were also active in CFA-induced arthritis in rats. After daily treatment for seven days with 5a and 5d (50 µmol/Kg), by oral administration, these compounds were not renal or hepatotoxic nor immunosuppressive. Compounds 5a and 5d also displayed good drug-scores and low risk toxicity calculated in silico using the program OSIRIS Property Explorer. |
| Databáze: | OpenAIRE |
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