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A series of new substituted arylmethyl phenyl ethers has been prepared. These compounds were tested as inhibitors of 5-lipoxygenase (5-LO) in rat neutrophils, in vitro antagonists of leukotriene-induced contraction of guinea pig (GP) lung parenchymal strips, and inhibitors of slow reacting substance of anaphylaxis (SRS-A) mediated bronchospasm in the GP in vivo. Most representatives of this new class of potential antiallergic/antiinflammatory agents showed potent inhibition of 5-LO activity in rat PMNs. The most potent compound, 2-[[3-(1-hydroxyhexyl)phenoxy]-methyl]quinoline (33), had an I50 of 0.12 microM in the rat PMN 5-LO assay and an I50 of 3.6 microM in the leukotriene-induced contraction of GP lung parenchymal strips, and it also showed 91% inhibition of SRS-A-mediated bronchospasm in the GP in vivo at 10 mg/kg, administered intraduodenally. Some of the compounds in this series were also leukotriene antagonists in vitro, and several of them showed in vivo activity against SRS-A-mediated bronchospasm in the GP.
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
August 1986,
Journal of medicinal chemistry,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
January 1993,
The Annals of pharmacotherapy,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
June 1998,
American journal of respiratory and critical care medicine,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
June 1998,
American journal of respiratory and critical care medicine,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
April 2006,
Bioorganic & medicinal chemistry letters,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
August 2023,
ACS omega,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
January 1997,
Pharmacotherapy,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
May 1991,
Journal of medicinal chemistry,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
January 1997,
Pharmacotherapy,
J H Musser, and
U R Chakraborty, and
S Sciortino, and
R J Gordon, and
A Khandwala, and
E S Neiss, and
T P Pruss, and
R Van Inwegen, and
I Weinryb, and
S M Coutts
January 1989,
Advances in experimental medicine and biology,
