Discovery of New Lead Compounds as Inhibitors of Allene Oxide Snnthase Based on Ozagrel Scaffold

2016 ◽  
Vol 5 (1) ◽  
pp. 45-48
Author(s):  
Keimei Oh ◽  
Yuina Todate ◽  
Yuko Yoshizawa
Keyword(s):  
Allene Oxide ◽  
Lead Compounds

Electrolytic Lead Compounds

1909 ◽  
Vol 67 (1744supp) ◽  
pp. 367-367
Author(s):  
Carl Duvivier
Keyword(s):  
Lead Compounds

Marine endoperoxides as antiprotozoan lead compounds

Planta Medica ◽  
2012 ◽  
Vol 78 (11) ◽  
Author(s):  
G Chianese ◽  
E Fattorusso ◽  
C Fattorusso ◽  
M Persico ◽  
D Taramelli ◽  
...  
Keyword(s):  
Lead Compounds

Discovery of anticancer lead compounds from plants of Vietnam

Planta Medica ◽  
2014 ◽  
Vol 80 (10) ◽  
Author(s):  
D Djendoel Soejarto ◽  
L Bueno Pérez ◽  
Y Ren ◽  
L Pan ◽  
U Muñoz Acuña ◽  
...  
Keyword(s):  
Lead Compounds

New strategy to search lead compounds with unique structures from plants

Planta Medica ◽  
2015 ◽  
Vol 81 (11) ◽  
Author(s):  
T Villani ◽  
K Gustafson ◽  
J Zhen ◽  
JE Simon ◽  
Q Wu
Keyword(s):  
Lead Compounds ◽  
New Strategy

PENENTUAN NILAI PARAMETER LIPOFILITAS SENYAWA 4-KLOROBENZOILTIOUREA DAN UJI POTENSIASI TERHADAP TIOPENTAL PADA MENCIT PUTIH (Mus musculus)

2019 ◽  
Vol 4 (1) ◽  
pp. 1
Author(s):  
Dini Kesuma
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Electronic Properties ◽  
Mus Musculus ◽  
Log P ◽  
P Value ◽  
Lead Compounds ◽  
Significant Difference ◽  
Central Nervous System Depressant ◽  
The Central Nervous System

Synthesis of the 4-chlorobenzoylthiourea compound was carried out by acylating thiourea with 4-chlorobenzoyl chloride. The 4-chlorobenzoylthiourea compound  will increase the lipophilic and the electronic properties other than the lead compounds of benzoylthiourea in order to, by expectation, raise the central nervous system depressant as well. The lipophilic would affect the ability of the compounds in penetrating biological membranes, which is highly dependent on the solubility of the drug within lipid/water. Log P is the most common method used in determining the parameter value. This experiment was to mix two dissolvents (octanol and water) which are immissible. The both levels of the compounds were carefully observed by a spectrophotometer UV-Vis. From the test, the result of log P value of the 4-chlorobenzoylthiourea compound was 2.32, while the theoretical log P value of the compounds, by using the π Hansch-Fujita method is 1.62 and the f Rekker-Mannhold method is 2.225. Consequently, the result of the test shows that there is a significant difference between the progress experiment and both theoretical log P methods. Moreover, in the test of the central nervous system depressant through the potentiation test to thiopental using mice indicates that the 4-chlorobenzoylthiourea compound have potentiation effects to thiopental compared to the lead compounds of benzoylthiourea.

In situ transformation of labile lead compounds to pyromorphites

2007 ◽  
Vol 15 (4) ◽  
pp. 453-458 ◽  
Author(s):  
J. Yang ◽  
B. L. Deng ◽  
Y.L. Li ◽  
C.L. Zhang
Keyword(s):  
Lead Compounds

Synthesis and Biological Evaluation of the Antimicrobial Natural Product Lipoxazolidinone A

2018 ◽  
Author(s):  
Jonathan J. Mills ◽  
Kaylib R. Robinson ◽  
Troy E. Zehnder ◽  
Joshua G. Pierce
Keyword(s):  
Natural Products ◽  
Natural Product ◽  
Mechanism Of Action ◽  
Marine Natural Products ◽  
Biological Evaluation ◽  
Lead Compounds ◽  
Follow Up Studies ◽  
Initial Resistance ◽  
Synthesis And Biological Evaluation

The lipoxazolidinone family of marine natural products, with an unusual 4-oxazolidinone heterocycle at their core, represents a new scaffold for antimicrobial discovery; however, questions regarding their mechanism of action and high lipophilicity have likely slowed follow-up studies. Herein, we report the first synthesis of lipoxazolidinone A, 15 structural analogs to explore its active pharmacophore, and initial resistance and mechanism of action studies. These results suggest that 4-oxazolidinones are valuable scaffolds for antimicrobial development and reveal simplified lead compounds for further optimization.

PHOTACs Enable Optical Control of Protein Degradation

2019 ◽  
Author(s):  
Martin Reynders ◽  
Bryan Matsuura ◽  
Marleen Bérouti ◽  
Daniele Simoneschi ◽  
Antonio Marzio ◽  
...  
Keyword(s):  
Protein Degradation ◽  
E3 Ligase ◽  
Optical Control ◽  
Cellular Proteins ◽  
Bifunctional Molecules ◽  
Protein Levels ◽  
Lead Compounds ◽  
Subsequent Degradation ◽  
Temporal And Spatial ◽  
Precision Therapeutics

<p><i>PROTACs (proteolysis targeting chimeras) are bifunctional molecules that tag proteins for ubiquitylation by an E3 ligase complex and subsequent degradation by the proteasome. They have emerged as powerful tools to control the levels of specific cellular proteins and are on the verge of being clinically used. We now introduce photoswitchable PROTACs that can be activated with the temporal and spatial precision that light provides. These trifunctional molecules, which we named PHOTACs, consist of a ligand for an E3 ligase, a photoswitch, and a ligand for a protein of interest. We demonstrate this concept by using PHOTACs that target either BET family proteins (BRD2,3,4) or FKBP12. Our lead compounds display little or no activity in the dark but can be reversibly activated to varying degrees with different wavelengths of light. Our modular and generalizable approach provides a method for the optical control of protein levels with photopharmacology and could lead to new types of precision therapeutics that avoid undesired systemic toxicity.</i><b></b></p>

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