PMID- 35544284
OWN - NLM
STAT- MEDLINE
DCOM- 20230113
LR  - 20230214
IS  - 1747-0285 (Electronic)
IS  - 1747-0277 (Linking)
VI  - 101
IP  - 2
DP  - 2023 Feb
TI  - Discovery of novel 1,3,5-triazines as potent antibacterial agent against urinary 
      tract infection-causing clinical isolates of Escherichia coli via inhibition of 
      DNA Gyrase.
PG  - 271-277
LID - 10.1111/cbdd.14066 [doi]
AB  - A novel series of 1,3,5-triazine-phenylthiazole-pyrazole derivatives were 
      synthesized and subsequently tested for Escherichia coli DNA Gyrase inhibitory 
      activity where they showed excellent inhibitory activity. The top-three ranked 
      DNA gyrase inhibitor (4e, 4g and 4h) were further subjected to antibacterial and 
      anti-biofilm activity against clinical isolates of resistant E. coli strains 
      obtained from Urinary Tract Infection (UTI) patients (CREC81, CREC106, CREC163). 
      Compound 4h was identified as most potent antibacterial agent in the above study. 
      The compound 4h was further evaluated in murine model of E. coli UTI in BALB/c 
      mice infected by transurethral injection of CREC106 strain. Results of the study 
      suggest that compound 4h reduces bacterial load of CREC106 in the treated mice 
      and found approximately equipotent to Novobiocin as standard.
CI  - (c) 2022 John Wiley & Sons Ltd.
FAU - Xia, Qier
AU  - Xia Q
AD  - Department of Urology, Shanghai Pudong New Area People's Hospital, Shanghai, 
      China.
FAU - Li, Jun
AU  - Li J
AD  - Department of Urology, Shanghai Pudong New Area People's Hospital, Shanghai, 
      China.
FAU - Yang, Zhenyu
AU  - Yang Z
AD  - Department of Urology, Shanghai Pudong New Area People's Hospital, Shanghai, 
      China.
FAU - Zhang, Dingguo
AU  - Zhang D
AD  - Department of Urology, Shanghai Pudong New Area People's Hospital, Shanghai, 
      China.
FAU - Tian, Jinjun
AU  - Tian J
AD  - Department of Urology, Shanghai Pudong New Area People's Hospital, Shanghai, 
      China.
FAU - Gu, Bin
AU  - Gu B
AD  - Department of Urology, Shanghai Pudong New Area People's Hospital, Shanghai, 
      China.
LA  - eng
PT  - Journal Article
DEP - 20221202
PL  - England
TA  - Chem Biol Drug Des
JT  - Chemical biology & drug design
JID - 101262549
RN  - EC 5.99.1.3 (DNA Gyrase)
RN  - 0 (Anti-Bacterial Agents)
RN  - 0 (Triazines)
RN  - 0 (Topoisomerase II Inhibitors)
SB  - IM
MH  - Animals
MH  - Mice
MH  - Escherichia coli
MH  - DNA Gyrase
MH  - Anti-Bacterial Agents/pharmacology
MH  - Triazines/pharmacology
MH  - *Escherichia coli Infections/drug therapy
MH  - *Urinary Tract Infections/drug therapy
MH  - Topoisomerase II Inhibitors/pharmacology
MH  - Microbial Sensitivity Tests
OTO - NOTNLM
OT  - E. coli
OT  - 1,3,5-triazine
OT  - BALB/c mice
OT  - DNA Gyrase
OT  - bacterial load
EDAT- 2022/05/12 06:00
MHDA- 2023/01/14 06:00
CRDT- 2022/05/11 11:46
PHST- 2022/04/23 00:00 [revised]
PHST- 2022/02/23 00:00 [received]
PHST- 2022/05/08 00:00 [accepted]
PHST- 2022/05/12 06:00 [pubmed]
PHST- 2023/01/14 06:00 [medline]
PHST- 2022/05/11 11:46 [entrez]
AID - 10.1111/cbdd.14066 [doi]
PST - ppublish
SO  - Chem Biol Drug Des. 2023 Feb;101(2):271-277. doi: 10.1111/cbdd.14066. Epub 2022 
      Dec 2.