Active site directed inhibitors of replication-specific bacterial DNA polymerases.
7-Substituted-N(2)-(3,4-dichlorobenzyl)guanines potently and competitively inhibit DNA polymerases IIIC and IIIE from Gram(+) bacteria. Certain derivatives are also competitive inhibitors of DNA polymerase IIIE from Gram(-) bacteria.
Wright
George E
GE
GLSynthesis Inc., One Innovation Drive, Worcester, MA 01605, USA. george.wright@glsynthesis.com
Brown
Neal C
NC
Xu
Wei-Chu
WC
Long
Zheng-Yu
ZY
Zhi
Chengxin
C
Gambino
Joseph J
JJ
Barnes
Marjorie H
MH
Butler
Michelle M
MM
D001426:Bacterial Proteins / Q000037:antagonists & inhibitors*; D001665:Binding Sites; D001667:Binding, Competitive; D004258:DNA Polymerase III / Q000037:antagonists & inhibitors; D004261:DNA Replication / Q000187:drug effects; D006090:Gram-Negative Bacteria / Q000201:enzymology; D006094:Gram-Positive Bacteria / Q000201:enzymology; D006147:Guanine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D019384:Nucleic Acid Synthesis Inhibitors; D013329:Structure-Activity Relationship; D014498:Uracil / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D001426:Bacterial Proteins; D019384:Nucleic Acid Synthesis Inhibitors; D014498:Uracil; D006147:Guanine; D004258:DNA Polymerase III