Synthesis and preliminary pharmacological evaluation of coumestans with different patterns of oxygenation.
Five coumestans with different patterns of oxygenation in rings A and D were synthesized from resorcinol and aromatic aldehydes, and screened for their antimyotoxic activity. The most potent compound (2b, IC50 = 1 microM) was selected for study of its pharmacological profile.
da Silva AJM
Laboratório de Química Bioorgânica (LQB), Núcleo de Pesquisas de Produtos Naturais, Universidade Federal do Rio de Janeiro, Brazil.
Melo
P A
PA
Silva
N M
NM
Brito
F V
FV
Buarque
C D
CD
de Souza
D V
DV
Rodrigues
V P
VP
Poças
E S
ES
Noël
F
F
Albuquerque
E X
EX
Costa
P R
PR
D000818:Animals; D014151:Anti-Anxiety Agents / Q000378:metabolism; D017837:Bothrops; D020650:Combinatorial Chemistry Techniques; D003374:Coumarins / Q000138:chemical synthesis* / Q000494:pharmacology*; D003402:Creatine Kinase / Q000037:antagonists & inhibitors; D003435:Crotalid Venoms / Q000037:antagonists & inhibitors; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D005445:Flunitrazepam / Q000378:metabolism; D018757:GABA Modulators / Q000378:metabolism; D020128:Inhibitory Concentration 50; D010100:Oxygen / Q000737:chemistry; D010936:Plant Extracts / Q000138:chemical synthesis / Q000494:pharmacology; D051381:Rats; D000254:Sodium-Potassium-Exchanging ATPase / Q000187:drug effects; D013329:Structure-Activity Relationship; D013574:Synaptosomes / Q000378:metabolism
D014151:Anti-Anxiety Agents; D003374:Coumarins; D003435:Crotalid Venoms; D004791:Enzyme Inhibitors; D018757:GABA Modulators; D010936:Plant Extracts; C051122:wedelolactone; D005445:Flunitrazepam; D003402:Creatine Kinase; D000254:Sodium-Potassium-Exchanging ATPase; D010100:Oxygen