3-aminothiophene-2-acylhydrazones: non-toxic, analgesic and anti-inflammatory lead-candidates
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ID: 210322
2014
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Abstract
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.
| Reference Key |
silva2014molecules3-aminothiophene-2-acylhydrazones:
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|---|---|
| Authors | ;Yolanda Karla Cupertino da Silva;Christian Tadeo Moreno Reyes;Gildardo Rivera;Marina Amaral Alves;Eliezer J. Barreiro;Magna Suzana Alexandre Moreira;Lídia Moreira Lima |
| Journal | Journal of ethnopharmacology |
| Year | 2014 |
| DOI |
10.3390/molecules19068456
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| URL | |
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