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1.
Mycoses ; 64(7): 727-733, 2021 Jul.
Article in English | MEDLINE | ID: mdl-33772895

ABSTRACT

Dermatophytosis is a superficial fungal infection that affects humans and is very common in small animals. The treatment using the most commonly used antifungals is failing, and new therapeutic alternatives are required to combat the resistance of these fungal infections. Previous studies by the group have shown that clioquinol is an important therapeutic alternative in the treatment of dermatophytosis. The object was to conduct studies of antidermatophytic activity and the irritant potential from the double and triple combinations of clioquinol, terbinafine and ciclopirox in ex vivo and in vivo alternative models. To evaluate the irritant potential of antifungal combinations, the alternative HET-CAM method (chicken egg test chorioallantoic membrane) was used. Ex vivo models were used to assess the effectiveness of antifungal combinations, using pig hooves and veterinary fur. Any possible tissue damage was to assess through in histopathology of swine ears. HET-CAM results showed that all combinations can be classified as non-irritating, corroborated by the results of the histopathological evaluation of the pig's ear skin. Only the double combinations managed to remove 100% of the colony-forming units (CFU) formed on the pig's hooves. The clioquinol + terbinafine combination and the triple combination were more effective than clioquinol + ciclopirox in eradicating the preformed biofilm in fur of veterinary origin. These results show the potential of formulations of clioquinol in combination with antifungals for use in humans and in the veterinary field to combat dermatophytosis, as an important alternative therapy, for use in the near future.


Subject(s)
Antifungal Agents , Dermatomycoses , Disease Models, Animal , Animals , Antifungal Agents/therapeutic use , Antifungal Agents/toxicity , Ciclopirox/therapeutic use , Ciclopirox/toxicity , Clioquinol/therapeutic use , Clioquinol/toxicity , Dermatomycoses/drug therapy , Dermatomycoses/veterinary , Drug Combinations , Humans , Microbial Sensitivity Tests , Swine , Terbinafine/therapeutic use , Terbinafine/toxicity
2.
J Med Chem ; 63(3): 1051-1067, 2020 02 13.
Article in English | MEDLINE | ID: mdl-31910018

ABSTRACT

Our previous study had identified ciclopirox (CPX) as a promising lead compound for treatment of ischemic stroke. To find better neuroprotective agents, a series of N-hydroxypyridone derivatives based on CPX were designed, synthesized, and evaluated in this study. Among these derivatives, compound 11 exhibits significant neuroprotection against oxygen glucose deprivation and oxidative stress-induced injuries in neuronal cells. Moreover, compound 11 possesses good blood-brain barrier permeability and superior antioxidant capability. In addition, a complex of compound 11 with olamine-11·Ola possesses good water solubility, negligible hERG inhibition, and superior metabolic stability. The in vivo experiment demonstrates that 11·Ola significantly reduces brain infarction and alleviates neurological deficits in middle cerebral artery occlusion rats. Hence, compound 11·Ola is identified in our research as a prospective prototype in the innovation of stroke treatment.


Subject(s)
Ciclopirox/analogs & derivatives , Ciclopirox/therapeutic use , Infarction, Middle Cerebral Artery/drug therapy , Neuroprotective Agents/therapeutic use , Animals , Antioxidants/chemical synthesis , Antioxidants/therapeutic use , Antioxidants/toxicity , Apoptosis/drug effects , Brain/pathology , Cell Line, Tumor , Ciclopirox/toxicity , Drug Design , Humans , Infarction, Middle Cerebral Artery/pathology , Male , Molecular Structure , Neuroprotective Agents/chemical synthesis , Neuroprotective Agents/toxicity , Rats, Sprague-Dawley , Structure-Activity Relationship
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