-transparent.png){kind=logo}
Several amino acid derived azolides (I) have been synthesized and investigated for their inhibitory activity toward human leukocyte elastase and porcine pancreatic elastase. The inhibitory activity was found to be dependent on the nature of the precursor amino acid ester. Thus, compounds derived from L-valine methyl ester 3, L-norvaline methyl ester 5, DL-norleucine methyl ester 9, and L-methionine methyl ester 10 were found to inhibit irreversibly both enzymes. Compound 10 was found to be a specific and selective inhibitor of human leukocyte elastase. In contrast to these, inhibitors derived from glycine methyl ester 1, D-valine methyl ester 4, and D-norvaline methyl ester 6 were found to be inactive. The results of the present study show that latent isocyanates derived from appropriate amino acids can serve as selective inhibitors of serine proteases and are of potential pharmacological value.
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
January 1977,
Advances in experimental medicine and biology,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
October 1976,
Biochemical and biophysical research communications,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
April 1973,
The Biochemical journal,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
May 1985,
Experientia,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
May 1982,
The Journal of biological chemistry,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
November 1977,
Biochimica et biophysica acta,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
July 1996,
Biochemistry,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
April 1984,
The Journal of biological chemistry,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
December 1985,
Journal of medicinal chemistry,
W C Groutas, and
W R Abrams, and
M C Theodorakis, and
A M Kasper, and
S A Rude, and
R C Badger, and
T D Ocain, and
K E Miller, and
M K Moi, and
M J Brubaker
April 1985,
Biochemistry,
