17715-58-1Relevant articles and documents
Revised structure and synthesis of celastramycin A, A potent innate immune suppressor
Kikuchi, Haruhisa,Sekiya, Mizuki,Katou, Yasuhiro,Ueda, Kazunori,Kabeya, Takahiro,Kurata, Shoichiro,Oshima, Oshiteru
supporting information; experimental part, p. 1693 - 1695 (2009/10/02)
After searching for natural substances that regulate Innate Immunity using the ex vivo Drosophila culture system, a benzoyl pyrrole-type compound, celastramycin A, was Identified and Isolated as a potent suppressor. By synthesizing the previously reported
Leukotriene B4 Receptor Antagonists: The LY255283 Series of Hydroxyacetophenones
Herron, David K.,Goodson, Theodore,Bollinger, Nancy G.,Swanson-Bean, Dorothy,Wright, Ian G.,et al.
, p. 1818 - 1828 (2007/10/02)
A series of hydroxyacetophenones was prepared for evaluation as leukotriene B4 (LTB4) receptor antagonists, culminating in 1-oxy>phenyl>ethanone (compound 35, LY255283).Using an assay for inhibition of specific LTB4 binding to human PMN, we found that substitution of a nonpolar substituent in the 5-position was required for activity.Best activity was realized with hydrogen in the 3-position, hydroxyl in the 2-position, short chain alkyl ketone in the 1-position, and a six- or eight-carbon chain linking the oxygen in the 4-position with an unsaturated terminal function.Compound 35, having an IC50 of 87 nM in the binding assay, was chosen for further preclinical evaluation.
