Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine.
The synthesis and in vitro evaluation of the acetamidine derivatives of hetero-substituted lysine and homolysine analogues have identified potent inhibitors of human nitric oxide synthase enzymes, including examples with marked selectivity for the inducible isoform.
Young
R J
RJ
Glaxo Wellcome Research and Development, Stevenage, Hertfordshire, UK. rjy40958@glaxowellcome.co.uk
Beams
R M
RM
Carter
K
K
Clark
H A
HA
Coe
D M
DM
Chambers
C L
CL
Davies
P I
PI
Dawson
J
J
Drysdale
M J
MJ
Franzman
K W
KW
French
C
C
Hodgson
S T
ST
Hodson
H F
HF
Kleanthous
S
S
Rider
P
P
Sanders
D
D
Sawyer
D A
DA
Scott
K J
KJ
Shearer
B G
BG
Stocker
R
R
Smith
S
S
Tackley
M C
MC
Knowles
R G
RG
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D007202:Indicators and Reagents; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D008239:Lysine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D019001:Nitric Oxide Synthase / Q000037:antagonists & inhibitors*; D052247:Nitric Oxide Synthase Type II; D009952:Ornithine / Q000031:analogs & derivatives / Q000494:pharmacology; D013440:Sulfides / Q000494:pharmacology; D013450:Sulfones / Q000494:pharmacology
D000081:Acetamides; D004791:Enzyme Inhibitors; C409003:GW 273629; D007202:Indicators and Reagents; D007527:Isoenzymes; D013440:Sulfides; D013450:Sulfones; C409004:GW 274150; D009952:Ornithine; C496319:NOS2 protein, human; D019001:Nitric Oxide Synthase; D052247:Nitric Oxide Synthase Type II; D008239:Lysine