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A series of desamino-2-nor-leukotriene analogs has been prepared by the reaction of various thiols with several methyl trans-4,5-epoxy-6Z-alkenoates, followed by deprotection. The products were assessed for their ability to antagonize the LTD4-induced contraction of the isolated guinea pig trachea. Several compounds displayed potent leukotriene antagonist activity, i.e., KB values in the sub-micromolar range, while only minimally affecting basal airway tone. The most potent analog, 4-hydroxy-5-(2-carboxyethylthio)-6Z-nonadecenoic acid, antagonized both LTD4- and LTE4-induced contractions of the trachea in an apparently competitive fashion. These agents possess increased potency relative to SK&F 101132, the first leukotriene analog identified as having LT-antagonist activity. Thus, these results demonstrate that deletion of the peptide amino group can produce leukotriene analogs which have minimal intrinsic contractile activity on the isolated guinea pig trachea, yet possess potent leukotriene-antagonistic effects.
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
December 1985,
Journal of medicinal chemistry,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
January 1989,
Advances in prostaglandin, thromboxane, and leukotriene research,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
January 1988,
International archives of allergy and applied immunology,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
January 1991,
Journal of medicinal chemistry,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
July 1984,
Archiv der Pharmazie,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
June 1997,
Thorax,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
December 1983,
Biochemical and biophysical research communications,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
March 1995,
Biochemical and biophysical research communications,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
January 1990,
Eicosanoids,
C D Perchonock, and
I Uzinskas, and
T W Ku, and
M E McCarthy, and
W E Bondinell, and
B W Volpe, and
J G Gleason, and
B M Weichman, and
R M Muccitelli, and
J F DeVan
December 1986,
Kokyu to junkan. Respiration & circulation,
