Synthesis and screening of a combinatorial library of naphthalene substituted chalcones: inhibitors of leukotriene B4.
A combinatorial mini library of naphthalene substituted chalcones has been prepared by solution phase chemistry. Screening of these mixtures for leukotriene B4 inhibitory activity using human whole blood assay (HWBL) afforded a lead compound, 1-(6-butoxy-2-naphthyl)-3-(4-nitrophenyl)-prop-2-en-1-one (K4A3) with an IC50 value of 18.5 microM.
Deshpande
A M
AM
Division of Organic Chemistry (Synthesis), National Chemical Laboratory, Pune, India.
Argade
N P
NP
Natu
A A
AA
Eckman
J
J
D002599:Chalcone / Q000737:chemistry; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020024:Leukotriene Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D007975:Leukotriene B4 / Q000037:antagonists & inhibitors* / Q000378:metabolism; D009281:Naphthalenes / Q000737:chemistry
D020024:Leukotriene Antagonists; D009281:Naphthalenes; D007975:Leukotriene B4; C031721:naphthalene; D002599:Chalcone