PMID- 36838642
OWN - NLM
STAT- MEDLINE
DCOM- 20230228
LR  - 20230301
IS  - 1420-3049 (Electronic)
IS  - 1420-3049 (Linking)
VI  - 28
IP  - 4
DP  - 2023 Feb 9
TI  - (S)-N-Benzyl-1-phenyl-3,4-dihydroisoqunoline-2(1H)-carboxamide Derivatives, 
      Multi-Target Inhibitors of Monoamine Oxidase and Cholinesterase: Design, 
      Synthesis, and Biological Activity.
LID - 10.3390/molecules28041654 [doi]
LID - 1654
AB  - A series of (S)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxamide derivatives 
      was synthesized and evaluated for inhibitory activity against monoamine oxidase 
      (MAO)-A and-B, acetylcholine esterase (AChE), and butyrylcholine esterase (BChE). 
      Four compounds (2i, 2p, 2t, and 2v) showed good inhibitory activity against both 
      MAO-A and MAO-B, and two compounds (2d and 2j) showed selective inhibitory 
      activity against MAO-A, with IC(50) values of 1.38 and 2.48 microM, respectively. 
      None of the compounds showed inhibitory activity against AChE; however, 12 
      compounds showed inhibitory activity against BChE. None of the active compounds 
      showed cytotoxicity against L929cells. Molecular docking revealed several 
      important interactions between the active analogs and amino acid residues of the 
      protein receptors. This research paves the way for further study aimed at 
      designing MAO and ChE inhibitors for the treatment of depression and 
      neurodegenerative disorders.
FAU - Jin, Qing-Hao
AU  - Jin QH
AD  - College of Nursing, Zhejiang Pharmaceutical University, Ningbo 315153, China.
FAU - Zhang, Li-Ping
AU  - Zhang LP
AD  - College of Nursing, Zhejiang Pharmaceutical University, Ningbo 315153, China.
FAU - Zhang, Shan-Shan
AU  - Zhang SS
AD  - Food and Pharmacy College, Zhejiang Ocean University, Zhoushan 316022, China.
FAU - Zhuang, Dai-Na
AU  - Zhuang DN
AD  - College of Nursing, Zhejiang Pharmaceutical University, Ningbo 315153, China.
FAU - Zhang, Chu-Yu
AU  - Zhang CY
AD  - College of Nursing, Zhejiang Pharmaceutical University, Ningbo 315153, China.
FAU - Zheng, Zhou-Jun
AU  - Zheng ZJ
AD  - College of Nursing, Zhejiang Pharmaceutical University, Ningbo 315153, China.
FAU - Guan, Li-Ping
AU  - Guan LP
AUID- ORCID: 0000-0002-8606-9257
AD  - Food and Pharmacy College, Zhejiang Ocean University, Zhoushan 316022, China.
LA  - eng
PT  - Journal Article
DEP - 20230209
PL  - Switzerland
TA  - Molecules
JT  - Molecules (Basel, Switzerland)
JID - 100964009
RN  - EC 1.4.3.4 (Monoamine Oxidase)
RN  - EC 3.1.1.8 (Cholinesterases)
RN  - 0 (Monoamine Oxidase Inhibitors)
RN  - 0 (Cholinesterase Inhibitors)
RN  - EC 3.1.1.7 (Acetylcholinesterase)
SB  - IM
MH  - *Monoamine Oxidase/metabolism
MH  - *Cholinesterases/metabolism
MH  - Monoamine Oxidase Inhibitors/pharmacology
MH  - Molecular Docking Simulation
MH  - Structure-Activity Relationship
MH  - Cholinesterase Inhibitors/chemistry
MH  - Acetylcholinesterase/metabolism
PMC - PMC9967051
OTO - NOTNLM
OT  - 3,4-dihydroisoquinoline
OT  - carboxamide derivatives
OT  - cholinesterase
OT  - cytotoxicity
OT  - molecular docking
OT  - monoamine oxidase
COIS- The authors declare that they have no known competing financial interest or 
      personal relationship that could have appeared to influence the work reported in 
      this paper.
EDAT- 2023/02/26 06:00
MHDA- 2023/03/03 06:00
PMCR- 2023/02/09
CRDT- 2023/02/25 03:55
PHST- 2022/12/31 00:00 [received]
PHST- 2023/01/28 00:00 [revised]
PHST- 2023/02/02 00:00 [accepted]
PHST- 2023/02/25 03:55 [entrez]
PHST- 2023/02/26 06:00 [pubmed]
PHST- 2023/03/03 06:00 [medline]
PHST- 2023/02/09 00:00 [pmc-release]
AID - molecules28041654 [pii]
AID - molecules-28-01654 [pii]
AID - 10.3390/molecules28041654 [doi]
PST - epublish
SO  - Molecules. 2023 Feb 9;28(4):1654. doi: 10.3390/molecules28041654.