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The Medicinal Chemistry of Caffeine
Journal of Medicinal Chemistry, 2021The purine alkaloid caffeine is the most widely consumed psychostimulant drug in the world and has multiple beneficial pharmacological activities, for example, in neurodegenerative diseases. However, despite being an extensively studied bioactive natural product, the mechanistic understanding of caffeine's pharmacological effects is incomplete.
Giuseppe Faudone +2 more
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Metallocyclodextrins in Medicinal Chemistry
Future Medicinal Chemistry, 2018This review focuses on metal complexes of cyclodextrin (CyD) derivatives designed for application as therapeutics or diagnostics. We discuss examples of metalloprotein models (hemoglobin, superoxide dismutase and catalase) based on cyclodextrins. The hydrophobic microenvironment of CyDs stabilizes the Fe(II) porphyrin system that can reversibly bind O2
Valentina Oliveri, Graziella Vecchio
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Furazans in Medicinal Chemistry
Journal of Medicinal Chemistry, 2021Incorporation of heterocycles into drug molecules can enhance physical properties and biological activity. A variety of heterocyclic groups is available to medicinal chemists, many of which have been reviewed in detail elsewhere. Oxadiazoles are a class of heterocycle containing one oxygen and two nitrogen atoms, available in three isomeric forms ...
Ross S. Mancini +3 more
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Oxadiazoles in Medicinal Chemistry
Journal of Medicinal Chemistry, 2012Oxadiazoles are five-membered heteroaromatic rings containing two carbons, two nitrogens, and one oxygen atom, and they exist in different regioisomeric forms. Oxadiazoles are frequently occurring motifs in druglike molecules, and they are often used with the intention of being bioisosteric replacements for ester and amide functionalities.
Jonas, Boström +4 more
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Polyethylenimine In Medicinal Chemistry
Current Medicinal Chemistry, 2008Polyethylenimine (PEI), an organic branched or linear polyamine polymer, has been successfully used in the past for DNA complexation and transfection in vitro and in vivo into several cell lines and tissues. PEI was also applied in different fields from gene therapy and several studies have emphasized the importance of this polymer in medicinal ...
VICENNATI, PAOLA +3 more
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Drug Discovery Today, 2006
With the advent of high throughput technologies in biological screening in the 1980s, providing sufficient numbers of small molecules for screening became a bottleneck in the drug discovery process. Combinatorial chemistry was the first attempt by chemists to address this issue. However, since its first applications, combinatorial chemistry has evolved
Marcus, Koppitz, Knut, Eis
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With the advent of high throughput technologies in biological screening in the 1980s, providing sufficient numbers of small molecules for screening became a bottleneck in the drug discovery process. Combinatorial chemistry was the first attempt by chemists to address this issue. However, since its first applications, combinatorial chemistry has evolved
Marcus, Koppitz, Knut, Eis
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Fluorine in Medicinal Chemistry
ChemBioChem, 2004AbstractFluorinated compounds are synthesized in pharmaceutical research on a routine basis and many marketed compounds contain fluorine. The present review summarizes some of the most frequently employed strategies for using fluorine substituents in medicinal chemistry. Quite often, fluorine is introduced to improve the metabolic stability by blocking
Hans-Joachim, Böhm +7 more
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Venomics in Medicinal Chemistry
Future Medicinal Chemistry, 2014Venom peptides mainly target ion channels, but also GPCRs, transporters and enzymes with high affinity and exquisite selectivity. The intermediate size of these peptidic toxins and their proteinaceous nature make them particularly suited formedicinal chemistry.
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