Parallel Synthesis Technologies in Lead Discovery and Optimization: Strategies and Applications

2004 ◽  
pp. 109-118 ◽  
Author(s):  
Robert J. Pasteris
Keyword(s):  
Parallel Synthesis ◽  
Lead Discovery

Accelerating drug lead discovery from nature by high-resolution bioactivity profiling combined with HPLC-HRMS-SPE-NMR

Planta Medica ◽  
2016 ◽  
Vol 81 (S 01) ◽  
pp. S1-S381
Author(s):  
KT Kongstad ◽  
NT Nyberg ◽  
SG Wubshet ◽  
D Staerk
Keyword(s):  
High Resolution ◽  
Lead Discovery ◽  
Drug Lead

Parallel Synthesis of a Biased Library of Thiazolidinones as Novel Sodium Channel Antagonists

2003 ◽  
Vol 6 (5) ◽  
pp. 481-488 ◽  
Author(s):  
Qun Sun ◽  
Laykea Tafesse ◽  
James Limberis ◽  
Khondekar Islam ◽  
Donald Kyle
Keyword(s):  
Sodium Channel ◽  
Parallel Synthesis

Unraveling the action mechanism of Buyang Huanwu Tang (BYHWT) for Cerebral Ischemia by Systematic Pharmacological Methodology

2020 ◽  
Vol 23 ◽  
Author(s):  
Shi-tang Ma ◽  
Ning Zhang ◽  
Ge Hong ◽  
Cheng-tao Feng ◽  
Sheng-wei Hong ◽  
...  
Keyword(s):  
Cerebral Ischemia ◽  
Virtual Screening ◽  
Signaling Pathways ◽  
Bioactive Compounds ◽  
Enrichment Analysis ◽  
Material Base ◽  
Lead Discovery ◽  
Binding Effect ◽  
Bioactive Ingredients ◽  
Compound Target

Background: Buyang Huanwu Tang (BYHWT) and relevant Traditional Chinese medicine (TCM) has its unique advantages in the treatment of cerebral ischemia. However, its pharmacological mechanism have not been fully explained. Objective: Base on the multi-component, also the entire disease network targets, the present study set out to identify major bioactive ingredients, key disease targets, and pathways of BYHWT against cerebral ischemia disease by systematic pharmacological methodology. Methods: Both the bioactive compounds from the BYHWT and the positive drugs against cerebral ischemia were fully investigated. The binding targets of the positive drugs were then obtained. A virtual screening protocol was then used to highlight the compound-target interaction. And network was constructed to visual the compound-target binding effect after docking analysis. Moreover，the targets enrichment analysis for biological processes and pathways were revealed to further explore the function of bio-targets protein gene and its role in the signal pathway. Results: A total of 382 active ingredients of the BYHWT and 23 candidate disease targets were identified. Virtual screening results indicated that multiple bioactive compounds targeted multiple proteins. Each compounds act on one or more targets. The mechanisms were linked to 20 signaling pathways, and the key mechanism was related to serotonergic synapse, calcium signaling pathway and camp signaling pathways. Conclusion: The present study explored the bioactive ingredients and mechanisms of BYHWT against cerebral ischemia by systematic pharmacological methodology. the novel methodology would provide a reference for the lead discovery of precursors, disease mechanism and material base for TCM.

Solution-Phase Parallel Synthesis of N-Substituted Isoquinuclidines

2004 ◽  
Vol 1 (4) ◽  
pp. 384-386 ◽  
Author(s):  
M. Levi ◽  
M. Khan ◽  
R. Borne
Keyword(s):  
Parallel Synthesis ◽  
Solution Phase
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