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Future Med Chem ; 11(24): 3109-3124, 2019 12.
Article in English | MEDLINE | ID: mdl-31838897

ABSTRACT

Aim: To find alternative compounds against methicillin-resistant Staphylococcus aureus (MRSA) and methicillin-susceptible S. aureus (MSSA), novel derivatives from dehydroabietic acid were synthesized. Methods & results: Compound 12 was the most effective against 15 MRSA and 11 MSSA with minimum inhibitory concentration values ranging from 3.9 to 15.6 µg/ml. Although less active than 12, compound 11, followed by 25 and 13, also exhibited anti-staphylococcal activity. Additional studies showed that compound 12 is devoid of toxic effect on non-target cells. A structure-activity relationship study revealed that an oxime at C-13 together with a hydroxyl at C-12 could play a key role in the activity. Conclusion: These structures, in particular compound 12, could arise as templates for the development of agents against MRSA and MSSA.


Subject(s)
Abietanes/chemical synthesis , Anti-Bacterial Agents/chemical synthesis , Methicillin-Resistant Staphylococcus aureus/drug effects , Abietanes/chemistry , Abietanes/pharmacology , Abietanes/toxicity , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/pharmacology , Anti-Bacterial Agents/toxicity , Cell Survival/drug effects , Cells, Cultured , Chromosome Aberrations/chemically induced , Erythrocytes/drug effects , Hemolysis/drug effects , Humans , Leukocytes, Mononuclear/drug effects , Microbial Sensitivity Tests , Molecular Structure , Onions/drug effects , Onions/genetics , Structure-Activity Relationship
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