Antitrypanosomal, Antileishmanial, and Antimalarial Activities of Quaternary Arylalkylammonium 2-Amino-4-Chlorophenyl Phenyl Sulfides, a New Class of Trypanothione Reductase Inhibitor, and ofN-Acyl Derivatives of 2-Amino-4-Chlorophenyl Phenyl Sulfide

2005 ◽  
Vol 48 (25) ◽  
pp. 8087-8097 ◽  
Author(s):  
Seheli Parveen ◽  
Mohammed O. F. Khan ◽  
Susan E. Austin ◽  
Simon L. Croft ◽  
Vanessa Yardley ◽  
...  
Keyword(s):  
Reductase Inhibitor ◽  
Trypanothione Reductase ◽  
Phenyl Sulfide ◽  
New Class ◽  
Derivatives Of ◽  
Acyl Derivatives

scholarly journals Benzobicyclo[3.2.1]octene Derivatives as a New Class of Cholinesterase Inhibitors

Molecules ◽  
2020 ◽  
Vol 25 (21) ◽  
pp. 4872
Author(s):  
Tena Čadež ◽  
Ana Grgičević ◽  
Ramiza Ahmetović ◽  
Danijela Barić ◽  
Nikolina Maček Hrvat ◽  
...  
Keyword(s):  
Ring Opening ◽  
Structural Adjustment ◽  
Cholinesterase Inhibitors ◽  
Furan Ring ◽  
Phenyl Substituent ◽  
Oxime Ether ◽  
New Class ◽  
Further Development ◽  
Derivatives Of ◽  
Acyl Derivatives

A library of amine, oxime, ether, epoxy and acyl derivatives of the benzobicyclo[3.2.1]octene were synthesized and evaluated as inhibitors of both human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). The majority of the tested compounds exhibited higher selectivity for BChE. Structural adjustment for AChE seems to have been achieved by acylation, and the furan ring opening of furo-benzobicyclo[3.2.1]octadiene results for compound 51 with the highest AChE affinity (IC50 = 8.3 µM). Interestingly, its analogue, an oxime ether with a benzobicyclo[3.2.1]-skeleton, compound 32 was one of the most potent BChE inhibitors in this study (IC50 = 31 µM), but not as potent as endo-43, an ether derivative of the benzobicyclo[3.2.1]octene with an additional phenyl substituent (IC50 = 17 µM). Therefore, we identified several cholinesterase inhibitors with a potential for further development as potential drugs for the treatment of neurodegenerative diseases.

Searching for New NO-Donor Aspirin-like Molecules: A New Class of Nitrooxy-acyl Derivatives of Salicylic Acid†

2008 ◽  
Vol 51 (6) ◽  
pp. 1894-1903 ◽  
Author(s):  
Loretta Lazzarato ◽  
Monica Donnola ◽  
Barbara Rolando ◽  
Elisabetta Marini ◽  
Clara Cena ◽  
...  
Keyword(s):  
Salicylic Acid ◽  
No Donor ◽  
New Class ◽  
Derivatives Of ◽  
Acyl Derivatives

scholarly journals Discovery of 2-iminobenzimidazoles as a new class of trypanothione reductase inhibitor by high-throughput screening

2007 ◽  
Vol 17 (5) ◽  
pp. 1422-1427 ◽  
Author(s):  
Georgina A. Holloway ◽  
Jonathan B. Baell ◽  
Alan H. Fairlamb ◽  
Patrizia M. Novello ◽  
John P. Parisot ◽  
...  
Keyword(s):  
High Throughput ◽  
High Throughput Screening ◽  
Reductase Inhibitor ◽  
Trypanothione Reductase ◽  
New Class

scholarly journals Synthesis, Antiproliferative Activity and Radical Scavenging Ability of 5-O-Acyl Derivatives of Quercetin

Molecules ◽  
2021 ◽  
Vol 26 (6) ◽  
pp. 1608
Author(s):  
Stephen Lo ◽  
Euphemia Leung ◽  
Bruno Fedrizzi ◽  
David Barker
Keyword(s):  
Antiproliferative Activity ◽  
Biological Activities ◽  
Radical Scavenging Activity ◽  
Radical Scavenging ◽  
Breast Cancer Cell Lines ◽  
Scavenging Activity ◽  
Plant Materials ◽  
Wide Range ◽  
Derivatives Of ◽  
Acyl Derivatives

Quercetin is a flavonoid that is found in many plant materials, including commonly eaten fruits and vegetables. The compound is well known for its wide range of biological activities. In this study, 5-O-acyl derivatives of quercetin were synthesised and assessed for their antiproliferative activity against the HCT116 colon cancer and MDA-MB-231 breast cancer cell lines; and their radical scavenging activity against the 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical cation and 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical species. Four derivatives were found to have improved the antiproliferative activity compared to quercetin whilst retaining radical scavenging activity.

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