Search Results - "Meanwell, Nicholas"

Fluorine and Fluorinated Motifs in the Design and Application of Bioisosteres for Drug Design by Meanwell, Nicholas A

“…The electronic properties and relatively small size of fluorine endow it with considerable versatility as a bioisostere and it has found application as a…”
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Applications of Bioisosteres in the Design of Biologically Active Compounds by Meanwell, Nicholas A

“…The design of bioisosteres represents a creative and productive approach to improve a molecule, including by enhancing potency, addressing pharmacokinetic…”
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Synopsis of Some Recent Tactical Application of Bioisosteres in Drug Design by Meanwell, Nicholas A

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Improving Drug Design: An Update on Recent Applications of Efficiency Metrics, Strategies for Replacing Problematic Elements, and Compounds in Nontraditional Drug Space by Meanwell, Nicholas A

“…Drug discovery and development is a complex and lengthy enterprise that suffers from high rates of candidate attrition at all stages of the process. The…”
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Bioisosteres of the Phenyl Ring: Recent Strategic Applications in Lead Optimization and Drug Design by Subbaiah, Murugaiah A. M, Meanwell, Nicholas A

“…The benzene moiety is the most prevalent ring system in marketed drugs, underscoring its historic popularity in drug design either as a pharmacophore or as a…”
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The expanding role of prodrugs in contemporary drug design and development by Rautio, Jarkko, Meanwell, Nicholas A., Di, Li, Hageman, Michael J.

“…Prodrug strategies can be used to overcome pharmacokinetic and pharmacodynamic issues in many therapeutic agents. Here, Rautio and colleagues discuss which…”
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Applications of Isosteres of Piperazine in the Design of Biologically Active Compounds: Part 1 by Meanwell, Nicholas A., Loiseleur, Olivier

“…Piperazine and homopiperazine are well-studied heterocycles in drug design that have found gainful application as scaffolds and terminal elements and for…”
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Metabolic and Pharmaceutical Aspects of Fluorinated Compounds by Johnson, Benjamin M, Shu, Yue-Zhong, Zhuo, Xiaoliang, Meanwell, Nicholas A

“…The applications of fluorine in drug design continue to expand, facilitated by an improved understanding of its effects on physicochemical properties and the…”
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The pyridazine heterocycle in molecular recognition and drug discovery by Meanwell, Nicholas A.

“…The pyridazine ring is endowed with unique physicochemical properties, characterized by weak basicity, a high dipole moment that subtends π-π stacking…”
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Applications of Isosteres of Piperazine in the Design of Biologically Active Compounds: Part 2 by Meanwell, Nicholas A., Loiseleur, Olivier

“…Applications of piperazine and homopiperazine in drug design are well-established, and these heterocycles have found use as both scaffolding and terminal…”
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Utilization of C(sp3)‐Carboxylic Acids and Their Redox‐Active Esters in Decarboxylative Carbon−Carbon Bond Formation by Karmakar, Sukhen, Silamkoti, Arundutt, Meanwell, Nicholas A., Mathur, Arvind, Gupta, Arun Kumar

“…Over the last several years, radical‐mediated decarboxylative cross‐coupling reactions employing alkyl carboxylic acids have emerged as a powerful tool for the…”
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Applications of Fluorine in Medicinal Chemistry by Gillis, Eric P, Eastman, Kyle J, Hill, Matthew D, Donnelly, David J, Meanwell, Nicholas A

“…The role of fluorine in drug design and development is expanding rapidly as we learn more about the unique properties associated with this unusual element and…”
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2015 Philip S. Portoghese Medicinal Chemistry Lectureship. Curing Hepatitis C Virus Infection with Direct-Acting Antiviral Agents: The Arc of a Medicinal Chemistry Triumph by Meanwell, Nicholas A

“…The development of direct-acting antiviral agents that can cure a chronic hepatitis C virus (HCV) infection after 8–12 weeks of daily, well-tolerated therapy…”
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Geminal Diheteroatomic Motifs: Some Applications of Acetals, Ketals, and Their Sulfur and Nitrogen Homologues in Medicinal Chemistry and Drug Design by Wu, Yong-Jin, Meanwell, Nicholas A

“…Acetals and ketals and their nitrogen and sulfur homologues are often considered to be unconventional and potentially problematic scaffolding elements or…”
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Sub-stoichiometric Modulation of Viral TargetsPotent Antiviral Agents That Exploit Target Vulnerability by Meanwell, Nicholas A.

“…The modulation of oligomeric viral targets at sub-stoichiometric ratios of drug to target has been advocated for its efficacy and potency, but there are only a…”
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A Survey of the Role of Noncovalent Sulfur Interactions in Drug Design by Beno, Brett R, Yeung, Kap-Sun, Bartberger, Michael D, Pennington, Lewis D, Meanwell, Nicholas A

“…Electron deficient, bivalent sulfur atoms have two areas of positive electrostatic potential, a consequence of the low-lying σ* orbitals of the C–S bond that…”
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Discovery of Daclatasvir, a Pan-Genotypic Hepatitis C Virus NS5A Replication Complex Inhibitor with Potent Clinical Effect by Belema, Makonen, Meanwell, Nicholas A

“…The discovery and development of the first-in-class hepatitis C virus (HCV) NS5A replication complex inhibitor daclatasvir (6) provides a compelling example of…”
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Anagrelide: A Clinically Effective cAMP Phosphodiesterase 3A Inhibitor with Molecular Glue Properties by Meanwell, Nicholas A.

“…The mode of action by which the orphan drug anagrelide (1), a potent cAMP phosphodiesterase 3A inhibitor, reduces blood platelet count in humans is not well…”
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Applications of fluorine-containing amino acids for drug design by Mei, Haibo, Han, Jianlin, Klika, Karel D., Izawa, Kunisuke, Sato, Tatsunori, Meanwell, Nicholas A., Soloshonok, Vadim A.

“…Fluorine-containing amino acids are becoming increasingly prominent in new drugs due to two general trends in the modern pharmaceutical industry. Firstly, the…”
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Tailor‐Made Amino Acids and Fluorinated Motifs as Prominent Traits in Modern Pharmaceuticals by Mei, Haibo, Han, Jianlin, White, Sarah, Graham, Daniel J., Izawa, Kunisuke, Sato, Tatsunori, Fustero, Santos, Meanwell, Nicholas A., Soloshonok, Vadim A.

“…Structural analysis of modern pharmaceutical practices allows for the identification of two rapidly growing trends: the introduction of tailor‐made amino acids…”
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