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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

The design and synthesis of second generation leukotriene B4 (LTB4) receptor antagonists related to SC-41930.

SC-41930, 7-[3-(4-acetyl-3-methoxy-2-propylphenoxy)propoxy]-3,4- dihydro-8-propyl-2H-1-benzopyran-2-carboxylic acid, is a selective, orally active, LTB4 receptor antagonist currently in clinical trials for psoriasis and ulcerative colitis. Exhaustive SAR studies found a potential backup compound, SC-50605, which was 7-16 times more potent than SC-41930 in LTB4 receptor binding, chemotaxis and degranulation assays. SC-50605 also inhibited LTB4-induced intradermal chemotaxis in cavine skin at an oral dose of 0.10 mg/kg and displayed good activity in animal models of colitis and epidermal inflammation both orally and topically.[1]

References

  1. The design and synthesis of second generation leukotriene B4 (LTB4) receptor antagonists related to SC-41930. Penning, T.D., Djuric, S.W., Docter, S.H., Yu, S.S., Spangler, D., Anglin, C.P., Fretland, D.J., Kachur, J.F., Keith, R.H., Tsai, B.S. Agents Actions (1993) [Pubmed]
 
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