Asymmetric organocatalysis: an enabling technology for medicinal chemistry

2021 ◽  
Vol 50 (3) ◽  
pp. 1522-1586
Author(s):  
Bo Han ◽  
Xiang-Hong He ◽  
Yan-Qing Liu ◽  
Gu He ◽  
Cheng Peng ◽  
...  

This review provides a comprehensive overview of the recent applications of organocatalytic strategies in pharmaceutical synthesis, with a focus on the preparation of antiviral, anticancer, neuroprotective, cardiovascular, antibacterial and antiparasitic agents.

2013 ◽  
Vol 42 (2) ◽  
pp. 774-793 ◽  
Author(s):  
José Alemán ◽  
Silvia Cabrera

Author(s):  
Arif Mermer

: After the clinical use of epalrestat that contains a rhodanine ring, in type II diabetes mellitus and diabetic complications, rhodanin-based compounds have become an important class of heterocyclic in the field of medicinal chemistry. Various modifications to the rhodanine ring have led to a broad spectrum of biological activity of these compounds. Synthesis of rhodanine derivatives, depended on advenced throughput scanning hits, frequently causes to potent and selective modulators of targeted enzymes or receptors, which apply their pharmacological activities through different mechanisms of action. Rhodanine-based compounds will likely stay a privileged scaffold in drug discovery because of different probability of chemical modifications of the rhodanine ring. We have therefore reviewed their biological activities and structure activity relationship.


2014 ◽  
Vol 2014 ◽  
pp. 1-29 ◽  
Author(s):  
Alfredo Ricci

The application of the most representative and up-to-date examples of homogeneous asymmetric organocatalysis to the synthesis of molecules of interest in medicinal chemistry is reported. The use of different types of organocatalysts operative via noncovalent and covalent interactions is critically reviewed and the possibility of running some of these reactions on large or industrial scale is described. A comparison between the organo- and metal-catalysed methodologies is offered in several cases, thus highlighting the merits and drawbacks of these two complementary approaches to the obtainment of very popular on market drugs or of related key scaffolds.


2017 ◽  
Vol 46 (10) ◽  
pp. 3060-3094 ◽  
Author(s):  
Thomas Mathew ◽  
Attila Á. Papp ◽  
Farzaneh Paknia ◽  
Santos Fustero ◽  
G. K. Surya Prakash

This review provides a comprehensive overview of the recent developments in synthetic strategies for benzodiazines, important scaffolds in medicinal chemistry.


2020 ◽  
Vol 49 (8) ◽  
pp. 2426-2480 ◽  
Author(s):  
Kaitlind C. Howard ◽  
Emily K. Dennis ◽  
David S. Watt ◽  
Sylvie Garneau-Tsodikova

The emergence of new fungal pathogens makes the development of new antifungal drugs a medical imperative that in recent years motivates the talents of numerous investigators across the world.


2021 ◽  
Author(s):  
Yuanhong Ma ◽  
Shao-Jie Lou ◽  
Zhaomin Hou

This review article provides a comprehensive overview to recognise the current status of electron-deficient boron-based catalysis in C–H functionalisations.


Crisis ◽  
2011 ◽  
Vol 32 (4) ◽  
pp. 178-185 ◽  
Author(s):  
Maurizio Pompili ◽  
Marco Innamorati ◽  
Monica Vichi ◽  
Maria Masocco ◽  
Nicola Vanacore ◽  
...  

Background: Suicide is a major cause of premature death in Italy and occurs at different rates in the various regions. Aims: The aim of the present study was to provide a comprehensive overview of suicide in the Italian population aged 15 years and older for the years 1980–2006. Methods: Mortality data were extracted from the Italian Mortality Database. Results: Mortality rates for suicide in Italy reached a peak in 1985 and declined thereafter. The different patterns observed by age and sex indicated that the decrease in the suicide rate in Italy was initially the result of declining rates in those aged 45+ while, from 1997 on, the decrease was attributable principally to a reduction in suicide rates among the younger age groups. It was found that socioeconomic factors underlined major differences in the suicide rate across regions. Conclusions: The present study confirmed that suicide is a multifaceted phenomenon that may be determined by an array of factors. Suicide prevention should, therefore, be targeted to identifiable high-risk sociocultural groups in each country.


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