The health components of spices and herbs: The medicinal chemistry point of view

2021 ◽  
pp. 35-92
Author(s):  
Fernanda M.F. Roleira ◽  
Carla L. Varela ◽  
Ana R. Gomes ◽  
Saul C. Costa ◽  
Elisiário J. Tavares-da-Silva
Keyword(s):  
Medicinal Chemistry ◽  
Point Of View

scholarly journals Chiral Separations in Preparative Scale: A Medicinal Chemistry Point of View

Molecules ◽  
2020 ◽  
Vol 25 (8) ◽  
pp. 1931 ◽  
Author(s):  
Madalena M.M. Pinto ◽  
Carla Fernandes ◽  
Maria E. Tiritan
Keyword(s):  
Medicinal Chemistry ◽  
Scale Up ◽  
Enantiomeric Separation ◽  
Chiral Separations ◽  
Point Of View ◽  
Preparative Liquid Chromatography ◽  
Preparative Scale ◽  
Technical Developments ◽  
Chiral Drug ◽  
Counter Current

Enantiomeric separation is a key step in the development of a new chiral drug. Preparative liquid chromatography (LC) continues to be the technique of choice either during the drug discovery process, to achieve a few milligrams, or to a scale-up during the clinical trial, needing kilograms of material. However, in the last few years, instrumental and technical developments allowed an exponential increase of preparative enantioseparation using other techniques. Besides LC, supercritical fluid chromatography (SFC) and counter-current chromatography (CCC) have aroused interest for preparative chiral separation. This overview will highlight the importance to scale-up chiral separations in Medicinal Chemistry, especially in the early stages of the pipeline of drugs discovery and development. Few examples within different methodologies will be selected, emphasizing the trends in chiral preparative separation. The advantages and drawbacks will be critically discussed.

Broad‐Spectrum Flavivirus Inhibitors: a Medicinal Chemistry Point of View

ChemMedChem ◽  
2020 ◽  
Vol 15 (24) ◽  
pp. 2391-2419 ◽  
Author(s):  
Tommaso Felicetti ◽  
Giuseppe Manfroni ◽  
Violetta Cecchetti ◽  
Rolando Cannalire
Keyword(s):  
Broad Spectrum ◽  
Medicinal Chemistry ◽  
Point Of View

scholarly journals Chimeric Drug Design with a Noncharged Carrier for Mitochondrial Delivery

2020 ◽  
Author(s):  
Consuelo Ripoll ◽  
Pilar Herrero-Foncubierta ◽  
Virginia Puente-Muñoz ◽  
M. Carmen Gonzalez-Garcia ◽  
Delia Miguel ◽  
...  
Keyword(s):  
Drug Design ◽  
Medicinal Chemistry ◽  
Thiophene Ring ◽  
Point Of View ◽  
General Applicability ◽  
Mitochondrial Carrier ◽  
Fluorescent Markers ◽  
Starting Point ◽  
Thiophene Moiety

Recently, it was proposed that the thiophene ring is capable of promoting mitochondrial accumulation when linked to fluorescent markers. As a noncharged group, thiophene presents several advantages from a synthetic point of view, making it easier to incorporate such a side moiety into different molecules. Herein, we confirm the general applicability of thiophene group as mitochondrial carrier for drugs and fluorescent markers, based on a new concept of nonprotonable, noncharged transporters. We implemented this concept in a medicinal chemistry application by developing an anti-tumoral, metabolic chimeric drug, based on PDHK inhibitor dichloroacetate (DCA). The promising features of the thiophene moiety as a noncharged carrier for targeting mitochondria may represent a starting point for the design of new metabolism-aimed drugs.

scholarly journals Heterocycles in Medicinal Chemistry

Molecules ◽  
2019 ◽  
Vol 24 (21) ◽  
pp. 3839 ◽  
Author(s):  
Josef Jampilek
Keyword(s):  
Medicinal Chemistry ◽  
Point Of View ◽  
Active Pharmaceutical Ingredients ◽  
Common Fragment ◽  
Pharmaceutical Ingredients

Heteroatoms constitute a very common fragment of a number of active pharmaceutical ingredients as well as excipients; from the point of view of significance, it is all the same if these are isosterically/bioisosterically replaced carbons/carbon substructures in aliphatic structures or real heterocycles [...]

Phosphodiesterase 10 Inhibitors - Novel Perspectives for Psychiatric and Neurodegenerative Drug Discovery

2018 ◽  
Vol 25 (29) ◽  
pp. 3455-3481 ◽  
Author(s):  
Agnieszka Zagorska ◽  
Anna Partyka ◽  
Adam Bucki ◽  
Alicja Gawalskax ◽  
Anna Czopek ◽  
...  
Keyword(s):  
Drug Discovery ◽  
Neurodegenerative Diseases ◽  
Medicinal Chemistry ◽  
Point Of View ◽  
Medium Spiny Neurons ◽  
Lead Discovery ◽  
Spiny Neurons ◽  
Wide Range ◽  
The Brain

Background: The phosphodiesterase 10 (PDE10) family, identified in 1999, is mainly expressed in the brain, particularly in the striatum, within the medium spiny neurons, nucleus accumbens, and olfactory tubercle. Inhibitors of PDE10 (PDE10-Is) are a conceptually rational subject for medicinal chemistry with potential use in the treatment of psychiatric and neurodegenerative diseases. Objective: This review is based on peer-reviewed published articles, and summarizes the cellular and molecular biology of PDE10 as a rational target for psychiatric and neurodegenerative drug discovery. Here, we present the classification of PDE10-Is from a medicinal chemistry point of view across a wide range of different, drug-like chemotypes starting from theophylline and caffeine analogs, papaverine and dimethoxy catechol type PDE10-Is, TP-10, MP-10, MP-10/papaverine/quinazoline series inhibitors, and ending with the newest inhibitors obtained from fragment-based lead discovery (FBLD). The authors have collated recent research on inhibition of PDE10A as a promising therapeutic strategy for psychiatric and neurodegenerative diseases, based on its efficacy in animal models of schizophrenia, Parkinson’s, Huntington’s, and Alzheimer’s diseases. This review also presents pharmacological data on PDE10-Is as possible therapeutics for the treatment of cognitive deficits, obesity and depression. Moreover, it summarizes the current strategies for PDE10-Is drug discovery based on the results of clinical trials. The authors also present the latest studies on crystal structures of PDE10 complexes with novel inhibitors.

The Long and Winding Road to Convert an Antimicrobial Compound into an Antimicrobial Drug: An Overview from a Medicinal Chemistry Point of View

2017 ◽  
Vol 21 (18) ◽  
Author(s):  
Ricardo D. Enriz ◽  
Fernando D. Suvire ◽  
Sebastian A. Andujar ◽  
Maria A. Alvarez ◽  
Marcela Vettorazzi ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Antimicrobial Drug ◽  
Point Of View ◽  
Antimicrobial Compound

The Geosciences Applied to Lunar Exploration

1962 ◽  
Vol 14 ◽  
pp. 169-257 ◽  
Author(s):  
J. Green
Keyword(s):  
Lunar Surface ◽  
Probable Mechanism ◽  
Point Of View ◽  
Lunar Exploration ◽  
Geological Model ◽  
Apply Geophysics ◽  
Surface Features ◽  
The Impact

The term geo-sciences has been used here to include the disciplines geology, geophysics and geochemistry. However, in order to apply geophysics and geochemistry effectively one must begin with a geological model. Therefore, the science of geology should be used as the basis for lunar exploration. From an astronomical point of view, a lunar terrain heavily impacted with meteors appears the more reasonable; although from a geological standpoint, volcanism seems the more probable mechanism. A surface liberally marked with volcanic features has been advocated by such geologists as Bülow, Dana, Suess, von Wolff, Shaler, Spurr, and Kuno. In this paper, both the impact and volcanic hypotheses are considered in the application of the geo-sciences to manned lunar exploration. However, more emphasis is placed on the volcanic, or more correctly the defluidization, hypothesis to account for lunar surface features.

How a sheperd guides a sheep herd?

1984 ◽  
Vol 75 ◽  
pp. 331-337
Author(s):  
Richard Greenberg
Keyword(s):  
Point Of View ◽  
Single Ring ◽  
Damping Effects ◽  
Ring Particle

ABSTRACTThe mechanism by which a shepherd satellite exerts a confining torque on a ring is considered from the point of view of a single ring particle. It is still not clear how one might most meaningfully include damping effects and other collisional processes into this type of approach to the problem.

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