PMID- 34443670
OWN - NLM
STAT- MEDLINE
DCOM- 20210917
LR  - 20210917
IS  - 1420-3049 (Electronic)
IS  - 1420-3049 (Linking)
VI  - 26
IP  - 16
DP  - 2021 Aug 22
TI  - Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as 
      Potent Growth Inhibitors of Drug-Resistant Bacteria.
LID - 10.3390/molecules26165083 [doi]
LID - 5083
AB  - Enterococci and methicillin-resistant S. aureus (MRSA) are among the menacing 
      bacterial pathogens. Novel antibiotics are urgently needed to tackle these 
      antibiotic-resistant bacterial infections. This article reports the design, 
      synthesis, and antimicrobial studies of 30 novel pyrazole derivatives. Most of 
      the synthesized compounds are potent growth inhibitors of planktonic 
      Gram-positive bacteria with minimum inhibitory concertation (MIC) values as low 
      as 0.25 microg/mL. Further studies led to the discovery of several lead compounds, 
      which are bactericidal and potent against MRSA persisters. Compounds 11, 28, and 
      29 are potent against S. aureus biofilms with minimum biofilm eradication 
      concentration (MBEC) values as low as 1 microg/mL.
FAU - Alkhaibari, Ibrahim S
AU  - Alkhaibari IS
AD  - Department of Chemistry and Physics, The College of Sciences and Mathematics, 
      Arkansas State University, Jonesboro, AR 72401, USA.
FAU - Kc, Hansa Raj
AU  - Kc HR
AD  - Department of Chemistry and Physics, The College of Sciences and Mathematics, 
      Arkansas State University, Jonesboro, AR 72401, USA.
FAU - Roy, Subrata
AU  - Roy S
AD  - Department of Chemistry and Physics, The College of Sciences and Mathematics, 
      Arkansas State University, Jonesboro, AR 72401, USA.
FAU - Abu-Gazleh, Mohd K
AU  - Abu-Gazleh MK
AUID- ORCID: 0000-0001-6209-6405
AD  - Department of Chemistry and Physics, The College of Sciences and Mathematics, 
      Arkansas State University, Jonesboro, AR 72401, USA.
FAU - Gilmore, David F
AU  - Gilmore DF
AUID- ORCID: 0000-0003-4426-1299
AD  - Department of Biological Sciences, The College of Sciences and Mathematics, 
      Arkansas State University, Jonesboro, AR 72401, USA.
FAU - Alam, Mohammad A
AU  - Alam MA
AUID- ORCID: 0000-0003-0258-3732
AD  - Department of Chemistry and Physics, The College of Sciences and Mathematics, 
      Arkansas State University, Jonesboro, AR 72401, USA.
LA  - eng
GR  - P20 GM103429/GM/NIGMS NIH HHS/United States
GR  - Arkansas State University/Kays Foundation/
PT  - Journal Article
DEP - 20210822
PL  - Switzerland
TA  - Molecules
JT  - Molecules (Basel, Switzerland)
JID - 100964009
RN  - 0 (3,5-bis(trifluoromethyl)pyrazolate)
RN  - 0 (Growth Inhibitors)
RN  - 0 (Pyrazoles)
SB  - IM
MH  - Bacteria/drug effects/*growth & development
MH  - Biofilms/drug effects
MH  - Cell Death/drug effects
MH  - Drug Resistance, Bacterial/*drug effects
MH  - Enterococcus faecalis/drug effects/physiology
MH  - Growth Inhibitors/*chemical synthesis/chemistry/*pharmacology
MH  - HEK293 Cells
MH  - Humans
MH  - Methicillin-Resistant Staphylococcus aureus/drug effects/physiology
MH  - Microbial Sensitivity Tests
MH  - Pyrazoles/*chemical synthesis/chemistry/*pharmacology
PMC - PMC8398255
OTO - NOTNLM
OT  - Enterococcus faecalis
OT  - Enterococcus faecium
OT  - MRSA
OT  - Staphylococcus aureus
OT  - VRE
OT  - aniline
OT  - pyrazole
COIS- The authors declare no conflict of interest.
EDAT- 2021/08/28 06:00
MHDA- 2021/09/18 06:00
PMCR- 2021/08/22
CRDT- 2021/08/27 01:17
PHST- 2021/08/04 00:00 [received]
PHST- 2021/08/19 00:00 [revised]
PHST- 2021/08/19 00:00 [accepted]
PHST- 2021/08/27 01:17 [entrez]
PHST- 2021/08/28 06:00 [pubmed]
PHST- 2021/09/18 06:00 [medline]
PHST- 2021/08/22 00:00 [pmc-release]
AID - molecules26165083 [pii]
AID - molecules-26-05083 [pii]
AID - 10.3390/molecules26165083 [doi]
PST - epublish
SO  - Molecules. 2021 Aug 22;26(16):5083. doi: 10.3390/molecules26165083.