PMID- 11836124
OWN - NLM
STAT- MEDLINE
DCOM- 20020911
LR  - 20190901
IS  - 0968-0896 (Print)
IS  - 0968-0896 (Linking)
VI  - 10
IP  - 4
DP  - 2002 Apr
TI  - SAR directed design and synthesis of novel beta(1-4)-glucosyltransferase 
      inhibitors and their in vitro inhibition studies.
PG  - 1129-36
AB  - This paper describes SAR directed design and synthesis of novel 
      beta(1-4)-glucosyltransferase (BGT) inhibitors. The designed inhibitors 1-5 
      provide conformational mimicry of the transition-state in glucosyltransfer 
      reactions. The compounds were tested for in vitro inhibitory activity against 
      (BGT) and the inhibition kinetics were examined. Three of the designed molecules 
      were found to be potential inhibitors of BGT having IC50 values in micromolar 
      (microM) range. Useful structure-activity relationships were established, which 
      provide guidelines for the design of future generations of inhibitors of BGT.
FAU - Bhattacharya, Asish K
AU  - Bhattacharya AK
AD  - Fachbereich Chemie, Universitat Konstanz, Fach M725, D-78457, Konstanz, Germany.
FAU - Stolz, Florian
AU  - Stolz F
FAU - Kurzeck, Jurgen
AU  - Kurzeck J
FAU - Ruger, Wolfgang
AU  - Ruger W
FAU - Schmidt, Richard R
AU  - Schmidt RR
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
PL  - England
TA  - Bioorg Med Chem
JT  - Bioorganic & medicinal chemistry
JID - 9413298
RN  - 0 (Enzyme Inhibitors)
RN  - 0 (Radioactive Tracers)
RN  - 58-98-0 (Uridine Diphosphate)
RN  - EC 2.4.1.- (Glucosyltransferases)
SB  - IM
MH  - Bacteriophage T4/enzymology
MH  - Catalytic Domain
MH  - *Drug Design
MH  - Enzyme Inhibitors/*chemical synthesis/chemistry/pharmacology
MH  - Glucosyltransferases/*antagonists & inhibitors
MH  - Inhibitory Concentration 50
MH  - Kinetics
MH  - Molecular Mimicry
MH  - Radioactive Tracers
MH  - Structure-Activity Relationship
MH  - Uridine Diphosphate/analogs & derivatives/chemistry/pharmacology
EDAT- 2002/02/12 10:00
MHDA- 2002/09/12 10:01
CRDT- 2002/02/12 10:00
PHST- 2002/02/12 10:00 [pubmed]
PHST- 2002/09/12 10:01 [medline]
PHST- 2002/02/12 10:00 [entrez]
AID - S0968089601003716 [pii]
AID - 10.1016/s0968-0896(01)00371-6 [doi]
PST - ppublish
SO  - Bioorg Med Chem. 2002 Apr;10(4):1129-36. doi: 10.1016/s0968-0896(01)00371-6.