Diarylurea: A Privileged Scaffold in Drug Discovery and Therapeutic Development

2022 ◽  
Vol 29 ◽  
Author(s):  
Alessia Catalano
Keyword(s):  
Drug Discovery ◽  
Therapeutic Development ◽  
Privileged Scaffold

Natural thiopeptides as a privileged scaffold for drug discovery and therapeutic development

2019 ◽  
Vol 28 (8) ◽  
pp. 1063-1098 ◽  
Author(s):  
Xiaoqi Shen ◽  
Muhammad Mustafa ◽  
Yanyang Chen ◽  
Yingying Cao ◽  
Jiangtao Gao
Keyword(s):  
Drug Discovery ◽  
Therapeutic Development ◽  
Privileged Scaffold

Targeted D4 Dopamine Receptors: Implications for Drug Discovery and Therapeutic Development

2013 ◽  
Vol 14 (4) ◽  
pp. 507-512 ◽  
Author(s):  
Radek Ptacek ◽  
Hana Kuzelova ◽  
George B. Stefano ◽  
Jiri Raboch ◽  
Richard M. Kream
Keyword(s):  
Drug Discovery ◽  
Dopamine Receptors ◽  
Therapeutic Development

Triazol: a privileged scaffold for proteolysis targeting chimeras

2019 ◽  
Vol 11 (22) ◽  
pp. 2919-2973 ◽  
Author(s):  
Li-Wen Xia ◽  
Meng-Yu Ba ◽  
Wei Liu ◽  
Weyland Cheng ◽  
Chao-Ping Hu ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Anticancer Activity ◽  
Mode Of Action ◽  
Critical Analysis ◽  
Enzyme Inhibitors ◽  
Structure Activity Relationship ◽  
Target Protein ◽  
Activity Relationship ◽  
Structure Activity ◽  
Privileged Scaffold

Current traditional drugs such as enzyme inhibitors and receptor agonists/antagonists present inherent limitations due to occupancy-driven pharmacology as the mode of action. Proteolysis targeting chimeras (PROTACs) are composed of an E3 ligand, a connecting linker and a target protein ligand, and are an attractive approach to specifically knockdown-targeted proteins utilizing an event-driven mode of action. The length, hydrophilicity and rigidity of connecting linkers play important role in creating a successful PROTAC. Some PROTACs with a triazole linker have displayed promising anticancer activity. This review provides an overview of PROTACs with a triazole scaffold and discusses its structure–activity relationship. Important milestones in the development of PROTACs are addressed and a critical analysis of this drug discovery strategy is also presented.

scholarly journals Optimisation by Design of Experiment of Benzimidazol-2-One Synthesis under Flow Conditions

Molecules ◽  
2019 ◽  
Vol 24 (13) ◽  
pp. 2447 ◽  
Author(s):  
Serena Mostarda ◽  
Tugçe Gür Maz ◽  
Alessandro Piccinno ◽  
Bruno Cerra ◽  
Erden Banoglu
Keyword(s):  
Drug Discovery ◽  
Design Of Experiment ◽  
Model Reaction ◽  
High Yield ◽  
Flow Conditions ◽  
Inflammatory Drug ◽  
Drug Discovery Program ◽  
Scale Preparation ◽  
Privileged Scaffold ◽  
Set Up

A novel flow-based approach for the preparation of benzimidazol-2-one (1) scaffold by the 1,1′-carbonyldiimidazole (CDI)-promoted cyclocarbonylation of o-phenylenediamine (2) is reported. Starting from a preliminary batch screening, the model reaction was successfully translated under flow conditions and optimised by means of design of experiment (DoE). The method allowed the efficient preparation of this privileged scaffold and to set up a general protocol for the multigram-scale preparation in high yield, purity, and productivity, and was successfully applied for the multigram flow synthesis of N-(2-chlorobenzyl)-5-cyano-benzimidazol-2-one, which is a key synthon for hit-to-lead explorations in our anti-inflammatory drug discovery program.

2-Arylbenzothiazole as a Privileged Scaffold in Drug Discovery

2009 ◽  
Vol 16 (19) ◽  
pp. 2430-2440 ◽  
Author(s):  
A. Weekes ◽  
A. Westwell
Keyword(s):  
Drug Discovery ◽  
Privileged Scaffold

Solid-Phase Synthesis of Tetramic Acid via Resin-Bound Enol Ethers as a Privileged Scaffold in Drug Discovery

2018 ◽  
Vol 360 (19) ◽  
pp. 3693-3699 ◽  
Author(s):  
Eva Schütznerová ◽  
Allen G. Oliver ◽  
Adam Přibylka ◽  
Viktor Krchňák
Keyword(s):  
Drug Discovery ◽  
Solid Phase Synthesis ◽  
Solid Phase ◽  
Tetramic Acid ◽  
Enol Ethers ◽  
Phase Synthesis ◽  
Privileged Scaffold

Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances

2017 ◽  
Vol 60 (19) ◽  
pp. 7941-7957 ◽  
Author(s):  
Joana Reis ◽  
Alexandra Gaspar ◽  
Nuno Milhazes ◽  
Fernanda Borges
Keyword(s):  
Drug Discovery ◽  
Recent Advances ◽  
Privileged Scaffold

ChemInform Abstract: 2-Arylbenzothiazole as a Privileged Scaffold in Drug Discovery

ChemInform ◽  
2010 ◽  
Vol 41 (1) ◽  
pp. no-no
Author(s):  
A. A. Weekes ◽  
A. D. Westwell
Keyword(s):  
Drug Discovery ◽  
Privileged Scaffold
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