From Saquinavir to Darunavir: The Impact of 10 Years of Medicinal Chemistry on a Lethal Disease

Author(s):  
Marie-Pierre de Béthune ◽  
Anik Peeters ◽  
Piet Wigerinck
2020 ◽  
Vol 38 (2) ◽  
pp. 146-146 ◽  
Author(s):  
Alex Zhavoronkov ◽  
Alán Aspuru-Guzik

2020 ◽  
Vol 37 (11) ◽  
pp. 1511-1531
Author(s):  
Zhi-Chen Wu ◽  
Dale L. Boger

This review summarizes and highlights recent advances in medicinal chemistry of natural products enabled by total synthesis that provide “supernatural products” with improved properties superseding the natural products themselves.


2008 ◽  
Vol 13 (10) ◽  
pp. 999-1006 ◽  
Author(s):  
Caroline Engeloch ◽  
Ulrich Schopfer ◽  
Ingo Muckenschnabel ◽  
Francois Le Goff ◽  
Hervé Mees ◽  
...  

The impact of storage conditions on compound stability and compound solubility has been debated intensely over the past 5 years. At Novartis, the authors decided to opt for a storage concept that can be considered controversial because they are using a DMSO/water (90/10) mixture as standard solvent. To assess the effect of water in DMSO stocks on compound stability, the authors monitored the purity of a subset of 1404 compounds from ongoing medicinal chemistry projects over several months. The study demonstrated that 85% of the compounds were stable in wet DMSO over a 2-year period at 4 °C. This result validates the storage concept developed at Novartis as a pragmatic approach that takes advantage of the benefits of DMSO/water mixtures while mediating the disadvantages. In addition, the authors describe how purity data collected over the course of the chemical validation of high-throughput screening actives are used to improve the analytical quality of the Novartis screening deck. ( Journal of Biomolecular Screening 2008:999-1006)


1998 ◽  
Vol 70 (2) ◽  
pp. 359-363 ◽  
Author(s):  
B. W. Metcalf

2021 ◽  
Vol 37 (1) ◽  
pp. 01-24
Author(s):  
Ashutosh Pal ◽  
Krishnanka Shekhar Gayen

The present review collects an update of the reactions in the area of medicinal chemistry using microwave irradiation. This review come up with an overview of most salient reactions performed under microwave irradiation in the field of drug discovery. Moreover, chemists are preferring to use this reaction rapidly in the academic as well as pharmaceutical laboratory during their drug discovery and making library of compounds. This reaction is much greener using less amount and readily recyclable solvents or sometimes reaction process without solvents and product become much cleaner, often yields are better than the conventional heating. Microwave irradiation is now very robust instrument used in company in the field of drug discovery, due to reduce the reaction time from hour to minute or even second and efficiently creation of compound libraries through combinatorial methodology associated with drug discovery so that new therapeutic agents bring to the market quicker. Hopefully, we will observe in the future the use of microwave irradiation drugs for the patients and this technology will utilize increase in number extensively in the field of medicinal chemistry. As this is an exceedingly rapid evolution area, this review offers significant expertise to the interested readers.


2015 ◽  
Vol 7 (10) ◽  
pp. 1285-1303 ◽  
Author(s):  
György G Ferenczy ◽  
György M Keserű

2008 ◽  
Vol 8 (13) ◽  
pp. 1128-1139 ◽  
Author(s):  
Ian Bell ◽  
Mark Bilodeau

2020 ◽  
Vol 38 (2) ◽  
pp. 143-145 ◽  
Author(s):  
W. Patrick Walters ◽  
Mark Murcko

Sign in / Sign up

Export Citation Format

Share Document