Novel indole-based inhibitors of IMPDH: introduction of hydrogen bond acceptors at indole C-3.
The development of a series of novel indole-based inhibitors of 5'-inosine monophosphate dehydrogenase (IMPDH) is described. Various hydrogen bond acceptors at C-3 of the indole were explored. The synthesis and the structure-activity relationships (SARs) derived from in vitro studies are outlined.
Watterson
Scott H
SH
Bristol-Myers Squibb PRI, Princeton, NJ 08543-4000, USA. scott.watterson@bms.com
Dhar
T G Murali
TG
Ballentine
Shelley K
SK
Shen
Zhongqi
Z
Barrish
Joel C
JC
Cheney
Daniel
D
Fleener
Catherine A
CA
Rouleau
Katherine A
KA
Townsend
Robert
R
Hollenbaugh
Diane L
DL
Iwanowicz
Edwin J
EJ
D002455:Cell Division / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D020719:Glucuronides / Q000378:metabolism; D006801:Humans; D006860:Hydrogen Bonding; D007168:IMP Dehydrogenase / Q000037:antagonists & inhibitors*; D007107:Immune System / Q000187:drug effects; D007211:Indoles / Q000737:chemistry*; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D008934:Mitogens / Q000494:pharmacology; D015363:Quinolones / Q000138:chemical synthesis / Q000494:pharmacology; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D020719:Glucuronides; D007211:Indoles; D007527:Isoenzymes; D008934:Mitogens; D015363:Quinolones; D007168:IMP Dehydrogenase