The Impact of Microwave-Assisted Organic Synthesis in Drug Discovery

ChemInform ◽  
2007 ◽  
Vol 38 (8) ◽  
Author(s):  
Farah Mavandadi ◽  
Aake Pilotti
2002 ◽  
Vol 7 (6) ◽  
pp. 373-380 ◽  
Author(s):  
Bernard Wathey ◽  
Jason Tierney ◽  
Pelle Lidström ◽  
Jacob Westman

ChemInform ◽  
2003 ◽  
Vol 34 (12) ◽  
Author(s):  
Bernard Wathey ◽  
Jason Tierney ◽  
Pelle Lidstrom ◽  
Jacob Westman

2013 ◽  
Vol 17 (5) ◽  
pp. 474-490 ◽  
Author(s):  
Amit Kumar Gupta ◽  
Neetu Singh ◽  
Krishna Nand Singh

2009 ◽  
Vol 9 (3) ◽  
pp. 340-358 ◽  
Author(s):  
V. Santagada ◽  
F. Frecentese ◽  
E. Perissutti ◽  
F. Fiorino ◽  
B. Severino ◽  
...  

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 892
Author(s):  
Elisa L. J. Moya ◽  
Elodie Vandenhaute ◽  
Eleonora Rizzi ◽  
Marie-Christine Boucau ◽  
Johan Hachani ◽  
...  

Central nervous system (CNS) diseases are one of the top causes of death worldwide. As there is a difficulty of drug penetration into the brain due to the blood–brain barrier (BBB), many CNS drugs treatments fail in clinical trials. Hence, there is a need to develop effective CNS drugs following strategies for delivery to the brain by better selecting them as early as possible during the drug discovery process. The use of in vitro BBB models has proved useful to evaluate the impact of drugs/compounds toxicity, BBB permeation rates and molecular transport mechanisms within the brain cells in academic research and early-stage drug discovery. However, these studies that require biological material (animal brain or human cells) are time-consuming and involve costly amounts of materials and plastic wastes due to the format of the models. Hence, to adapt to the high yields needed in early-stage drug discoveries for compound screenings, a patented well-established human in vitro BBB model was miniaturized and automated into a 96-well format. This replicate met all the BBB model reliability criteria to get predictive results, allowing a significant reduction in biological materials, waste and a higher screening capacity for being extensively used during early-stage drug discovery studies.


Proceedings ◽  
2020 ◽  
Vol 70 (1) ◽  
pp. 103
Author(s):  
Jin Mark D. G. Pagulayan ◽  
Aprille Suzette V. Mendoza ◽  
Fredelyn S. Gascon ◽  
Jan Carlo C. Aningat ◽  
Abigail S. Rustia ◽  
...  

The study aimed to evaluate the effects of process parameters (time and raw material weight (RMW)) of conventional (boiling for 10–45 min) and microwave-assisted (2–8 min) aqueous extraction on the color quality (i.e., lightness (L*), chroma (C*), and hue (H°) of anthocyanin –based colorants of red and Inubi sweet potato (Ipomoea batatas L.) leaves. Using response surface methodology, it was found that RMW and boiling time (BT) and microwave time (MT) generally had a significant (p < 0.05) effect on the color quality of the extract from both extraction methods. The effects were found to vary depending on the extraction method and variety of the leaves used. Both extraction methods produced a brown to brick-red extract from the Inubi variety that turned red-violet to pink when acidified. The red sweet potato leaves produced a deep violet colored extract that also turned red-violet when acidified. It is recommended that the anthocyanin content of the extracts be measured to validate the impact of the methods on the active agent. Nevertheless, the outcomes in this study may serve as baseline data for further studies on the potential of sweet potato leaf colorants (SPLC) as a colorant with functional properties.


Author(s):  
Danhua Ge ◽  
Xin Wang ◽  
Xue-Qiang Chu

The past decades have witnessed a boom in alkynylation mainly owing to the importance of alkynyl-containing molecules in organic synthesis, drug discovery, polymer chemistry, and materials science. Besides conventional strategies,...


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