Crafting Your Next Medicinal Chemistry Article: Key Metrics and Author Guidelines for Industrial Researchers

Although this editorial is slightly dated, it offers valuable perspectives for medicinal chemists and drug designers.

CHIRALITY: The Vital Role in Modern Drug Discovery

Source: Narmatha Senkuttuvan, et al., The significance of chirality in contemporary drug discovery-a mini review. https://lnkd.in/gNKfDCWf https://lnkd.in/g53PJHXQ

Cross-Coupling Reactions: From Established Principles to Emerging Innovations

I'm confident this editorial will captivate organic and medicinal chemists and drug discovery enthusiasts, far and wide.

Strategies for the Synthesis of Enantiopure Mechanically Chiral Molecules

Source: https://lnkd.in/ghDHFhFG

Resolving Exceptions and Paradoxes in Chemical Reactivity

This critical perspective sheds light on a thinking framework, offering one of many paths to harness anomalies for scientific advancement.

Enantioselective analysis of pesticides in food, biological, and environmental samples by chromatographic techniques and capillary electrophoresis

Source: https://lnkd.in/ed45QZmV https://lnkd.in/e9z_M2k9

Heterocycles: Essential Pillars in the Evolution of Modern Drug Discovery

I believe Medicinal Chemists and Drug Designers will find this editorial illuminating, as it underscores the pivotal role of heterocycles in pharmaceutical research and patient care advancements.

One-Pot Three-Component Synthesis of Biologically Promising Indenoquinoxaline Fused Spiroheterocycles Starting from 11H-indeno[1,2-b]quinoxalin-11-ones

Source: https://lnkd.in/g9GB5mE6 | https://lnkd.in/gsVPQn-q

This article is sure to capture the interest of R&D Chemists and Engineers.

Enantioselective Behaviors of Chiral Pesticides and Enantiomeric Signatures in Foods and the Environment

Source: J. Agric. Food Chem. 2023, 71, 33, 12372–12389 https://lnkd.in/eUPZuJr5

Inhibitory potential of nitrogen, oxygen and sulfur containing heterocyclic scaffolds against acetylcholinesterase and butyrylcholinesterase

Heterocycles play a crucial role in organic chemistry due to their vast applications in biology, chemistry, and pharmaceuticals. These compounds are essential in nature, medicine, and innovation. Most commonly, they include pure nitrogen heterocycles or combinations of nitrogen, oxygen, and sulfur in five or six-membered rings.

An axial-to-axial chirality transfer strategy for atroposelective construction of C–N axial chirality

by Ze-Shui Liu et al | Source: https://lnkd.in/gQ5FtASZ | https://lnkd.in/gAuBtgps

Bioinspired chiral inorganic nanomaterials

Source: Cho, N.H. et al. Bioinspired chiral inorganic nanomaterials. Nat Rev Bioeng 1, 88–106 (2023). https://lnkd.in/eFwUZPns | https://lnkd.in/ef4FMKRQ

UNLOCKING THE POWER OF CHIRALITY: 3D Chemical Space Exploration and Modern Drug Discovery Breakthroughs

Source: Silvestri IP, Colbon PJJ. The Growing Importance of Chirality in 3D Chemical Space Exploration and Modern Drug Discovery Approaches for Hit-ID: Topical Innovations. ACS Med Chem Lett. 2021 Jul 16;12(8):1220-1229. doi: 10.1021/acsmedchemlett.1c00251. https://lnkd.in/gnPuJmWQ

If you look around you right now, everything is made from a chemical reaction

To all science aficionados: Delve into the enlightening 2021 hashtag#NobelPrize lecture by chemistry laureate David MacMillan on Asymmetric Organocatalysis. Discover the essence of catalysis and its profound impact on modern chemistry. If you haven't seen it yet, it's a must-watch: https://bit.ly/3FW9NBz.

Revolutionizing Synthesis: Asymmetric Reactions for Chiral Cyclic and Heterocyclic Alcohols

Chiral cyclic and heterocyclic alcohols are crucial for fine chemicals, agrochemicals, and chiral pharmaceuticals like ladostigil, imbruvica, and sulopenem.

Powerhouse Inhibitor: Geldanamycin, the Natural Hsp90 Blocker and Medicinal Chemistry Pioneer

Geldanamycin continues to be a key player in Hsp90 inhibition, even 50 years after its discovery. This perspective highlights the benzoquinone ring’s ability to undergo various functionalization reactions.

Chirality communications between inorganic and organic compounds

Chirality bridges the gap between inorganic and organic compounds, creating a unique communication channel between different materials. This transfer primarily occurs through material hybridization and asymmetric synthesis. Recognition usually happens through enantioselective adsorption of organic compounds on inorganic surfaces.

Revolutionizing Drug Discovery: Cutting-Edge Computational Approaches for Small Molecules

2024 has been an extraordinary year for computational sciences. The Nobel Prize in Physics was awarded for “artificial neural network,” and the Nobel Prize in Chemistry for “protein structure prediction and design.”

Breaking New Ground: Advances in Enantioselective Radical Desymmetrization

Enantioselective desymmetrization of prochiral and meso compounds is an efficient way to create complex enantioenriched molecules in one step.

Green Power in Pharma: Nanocarrier Biocatalysts Redefining Medicine through Eco-Friendly Synthesis

Nanobiocatalysts (NBCs) merge the strengths of enzymes and nanomaterials, creating a promising new class of biocatalysts.

AI and Human Ingenuity Unite: Redefining Drug Design in the Modern Era

I'm pleased to share this perspective titled 'Rethinking Drug Design in the Artificial Intelligence Era,' published in Nature Reviews Drug Discovery in 2019. Though it's a bit dated, I believe it's still a compelling read for all medicinal chemists and drug designers. I hope you find it insightful.

Revolutionizing Early Drug Development: Advances in Metabolomics Analysis

The pharmaceutical industry was quick to adopt proteomics and other 'omics technologies for drug research. While metabolomics initially lagged behind, it has now become a widely accepted approach in early drug development.

Advancing Chiral Chemistry: Organocatalytic Enantioselective Sulfur Alkylation of Sulfenamides for Sulfilimines Synthesis

In recent years, asymmetric synthetic methods for sulfur stereogenic centers have seen rapid development, significantly impacting drug discovery. Replacing carbon atoms with nitrogen in drug molecules has become a popular optimization strategy, as nitrogen can greatly enhance pharmacological properties. This is evident in the growing importance of chiral sulfoximines, the aza-analogs of sulfones. Nitrogen substitution at the sulfur center generates intrinsic chirality and provides additional modification sites. The nitrogen's lone pair also promotes favorable hydrogen bonding and coordination.

Breaking New Ground: Sulfonated Molecules Revolutionize Biomaterials

This review explores the latest applications of sulfonated molecules in biomaterials. Sulfonation, the process of adding sulfonic acid groups, enhances the properties of these materials.

Enantioselective reduction of sulfur-containing cyclic imines through biocatalysis

The 3-thiazolidine ring is vital in life sciences, but reducing 3-thiazolines has been a challenge with most chemical methods.

Pioneering Silver-Catalyzed Epoxide to Cyclopropane Conversion with N-Triftosylhydrazones

Epoxides are vital small ring O-heterocycles and pivotal in medicinal chemistry. Traditional O-to-C replacements often require high temperatures with low yields, posing a challenge.

Application of Chiral Piperidine Scaffolds in Drug Design

Chiral piperidine scaffolds are common in many pharmaceuticals. This review highlights their diversity in newly approved drugs, as well as in leading and candidate drugs. It discusses their crucial role in drug design. Adding chiral piperidine scaffolds to small molecules can improve drug-like properties, such as:

Recent Advances in Catalytic Desymmetrization for the Synthesis of Axially Chiral Biaryls

Atropisomeric compounds are important in pharmaceuticals and materials science. Their enantioselective synthesis has garnered significant attention. Desymmetrization is a robust method for creating axially chiral biaryls. It's simpler than other strategies due to easier substrate design. However, challenges like forming achiral products and distant reaction sites exist.

Phonon-Induced Geometric Chirality

Chiral properties are making waves in emerging fields like chiral quantum optics, plasmonics, and phononics. While manipulating the chirality of light and lattice vibrations has been achieved, controlling material chirality on demand has remained elusive.

Advances on Greener Asymmetric Synthesis of Antiviral Drugs via Organocatalysis

Viral infections are a leading cause of severe human diseases and high mortality rates. This article underscores the critical efforts by academia and the pharmaceutical industry to discover new antiviral compounds.

Recent Developments Towards the Synthesis of Triazole Derivatives: A Review

Triazoles are a key part of heterocyclic chemistry, acting as essential building blocks in organic synthesis, materials science, and medicinal chemistry. They form a five-membered ring with three nitrogen and two carbon atoms and exist in two isomeric forms: 1,2,3-triazole and 1,2,4-triazole.

Prescribed drugs containing nitrogen heterocycles: an overview

Heteroatoms and heterocyclic scaffolds are common in many active pharmaceuticals and natural products. Over 85% of biologically active compounds contain these structures, especially nitrogen heterocycles. This highlights their crucial role in modern drug design and discovery.

Atropisomerism in the Pharmaceutically Relevant Realm

Atropisomerism, where there's restricted rotation around a bond leading to conformational chirality, is found in many drug structures like biaryls and heterobiaryls. These atropisomers vary in stability, with some being suitable for drug development.

Synthesis at the Interface of Chemistry and Biology

Chemical synthesis controls the structure and properties of matter, from fine chemicals and polymers to drugs and materials. Traditional tools fall short with larger molecules, but Mother Nature's strategies offer new possibilities. By merging natural and modern chemical tools, it's possible to create new macromolecules and even organisms with novel properties.

Enzymatic DNA Synthesis: Going to Great Lengths

The demand for DNA is at an all-time high, driven by fields such as cell and gene therapy, vaccine development, protein engineering, data storage, and biomanufacturing. To meet these demands, researchers are developing innovative ways to customize and mass-produce synthetic DNA, sidestepping the limitations and low yields of extracting it from natural sources.

Photochemical Synthesis of Chiral Heterocycles via Asymmetric Carbon-Heteroatom Bond Formation

This article focuses on the recent developments in photochemical synthesis of chiral heterocyclic compounds, which are essential in pharmaceuticals, materials science, and agrochemicals. Over the past 15 years, photochemical asymmetric transformations have garnered significant attention, particularly for their role in drug discovery and development.

Going Chiral: Breakthrough in Synthesizing Carbon Nanotubes with Precise Chirality

Researchers have made a major breakthrough in carbon nanotube (CNT) synthesis with a new catalyst that precisely controls their atomic arrangement, known as chirality. This development opens up new possibilities for innovative semiconductor devices, solving a challenge that's been unresolved for over 30 years.

Escape from Flatland: 2D to 3D Molecules via Dearomatization

Many organic molecules in medicinal chemistry are quite flat due to aromatic rings. However, over the last few decades, diversity-oriented synthesis (DOS) has developed new strategies to increase the complexity and three-dimensionality of drug candidates.

Design, Synthesis, and Utility of Defined Molecular Scaffolds

In modern chemistry, creating functional molecules by joining organic building blocks is a major theme. This involves using various 'scaffolds,' or structural frameworks, made from 'hubs' like triazine and lysine.

Biocatalysis: A smart and green tool for the preparation of chiral drugs

This review highlights the innovative use of biocatalysis in synthesizing chiral drugs and their intermediates. Over the past decades, biocatalysis has garnered significant interest due to its high efficiency, yield, and eco-friendly processes. It has proven particularly effective in preparing chiral molecules.

Basic Nitrogen (BaN) Is a Key Property of Antimalarial Chemical Space

The perspective paper highlights the essential role of basic nitrogen (BaN) in antimalarial drugs. Although BaN is a key component in most antimalarials, its role hasn't been systematically studied.

Recent Advances in the Enantioselective Synthesis of Chiral Amines via Transition Metal-Catalyzed Asymmetric Hydrogenation

Chiral amines are crucial components found in many natural products, medicines, and biologically active substances. Over the past decade, significant progress has been made in creating chiral amines, especially through a process called catalytic asymmetric hydrogenation (AH).

New 'chiral vortex' of light allows chemists to 'see' molecules through the mirror

This paper focuses on enhancing the efficiency and robustness of chiral optical discrimination by embedding topological properties into the enantiosensitive optical response of chiral molecules.

Seven-membered N-heterocycles as approved drugs and promising leads in medicinal chemistry as well as the metal-free domino access to their scaffolds

Azepanes and azepines are key structures in numerous drugs, drug candidates, and tested lead compounds. Despite the frequent occurrence of N-heterocyclic 7-membered rings in nature, such as in alkaloids, naturally occurring compounds of this type are seldom approved as therapeutics.

Asymmetric Synthesis and Applications of Chiral Organoselenium Compounds: A Review

This paper reviews the development and application of organoselenium compounds, highlighting their significance in medicine, materials, and organic synthesis. It focuses particularly on chiral organoselenium compounds, essential for these fields. Despite their importance, producing these compounds in an ecofriendly manner remains a challenge.

Challenges and innovations in chiral drugs in an environmental and bioanalysis perspective

This review explores the advancements in chiral analysis for environmental, forensic, and bioanalytical applications. It highlights the challenges and innovations in chiral screening technologies, emphasizing higher detectability and lower sample volumes. Various methods and their applications, particularly in forensic analysis, are discussed.

Chiral Drug Analysis in Forensic Chemistry: An Overview

This paper explores how chiral analysis is used in both biological and environmental contexts, emphasizing its importance in forensic science.

Chirality: The Backbone of Chemistry as a Natural Science

This paper highlights the crucial role of chiral dissymmetry in the chemical evolution toward life. Chemistry, as a natural science, spans a vast range of scales, from the formation of atoms and molecules to the development of proto-life systems capable of catalytic synthesis, replication, and Darwinian evolution.

Widened Scope of Drug Repurposing/Chiral Switches, Elements of Secondary Pharmaceuticals: The Quinine/Quinidine Case

This perspective article explores drug repurposing and chiral switches, focusing on the antimalarial quinine and the antiarrhythmic quinidine. It highlights how these drugs, with histories dating back to 1638, have been repurposed for new medical uses.

Biocatalysis

This excellent primer delves into the latest methodologies in the field, covering aspects such as route design, enzyme discovery, protein engineering, and the industrial implementation of biocatalysis.

A Look at the Importance of Chirality in Drug Activity: Some Significative Examples

An excellent review that provides a brief overview of the most common chiral drugs used in therapy for treating various diseases.

Ynamides: Versatile Tools in Organic Synthesis

This review highlights the major developments in the field of ynamides. They offer unique opportunities to add nitrogen-based functionalities to organic molecules, making them incredibly useful and versatile building blocks for organic synthesis.

Umpolung strategies for the functionalization of peptides and proteins

This perspective highlights the innovative use of umpolung strategies for peptide and protein functionalizations.

Demystifying racemic natural products in the homochiral world

This review aims to explore the structural complexity, diversity, and chirality of natural products and their significant impact on drug discovery.

Stereochemical diversity as a source of discovery in chemical biology

This review examines how chirality provides valuable chemical information at the chemistry-biology interface. It also looks at the chemical information density of FDA-approved drugs and the impact of stereochemistry on molecular complexity, with discussions on axial chirality and atroposelectivity as potential expansions.

Breaking Molecular Symmetry through Biocatalytic Reactions to Gain Access to Valuable Chiral Synthons

This interesting review highlights recent advancements in using biocatalytic reactions to break the symmetry of meso-compounds and symmetric prochiral molecules. Since 2015, research shows that lipases remain the go-to enzymes for these reactions due to their versatility, stability under various conditions, and easy availability.

Chiral pharmaceuticals: Environment sources, potential human health impacts, remediation technologies and future perspective

This paper focuses on the widespread use and environmental impact of chiral pharmaceuticals, including NSAIDs, β-blockers, and some agrochemicals.

These compounds often end up as pollutants in soil and water due to industrial waste, improper storage, and animal waste. Human exposure, primarily through medical treatments and environmental contamination, can lead to serious health issues, including cancer.

The Quest for Secondary Pharmaceuticals: Drug Repurposing/Chiral-Switches Combination Strategy

This perspective introduces a new strategy that combines drug repurposing and chiral switches. It highlights examples like ketamine, flurbiprofen, fenfluramine, and milnacipran that has undergone this combination strategy. Also discusses a variation involving deuterium-enabled chiral switches of thalidomide analogs.

Expanding the medicinal chemistry synthetic toolbox

This perspective aims to identify opportunities for expanding the synthetic toolbox of medicinal chemists to enhance future drug discovery. Also highlights the limitations of current reaction parameters, synthesis design tools, and strategies. It also identifies opportunities to expand the synthetic toolbox of medicinal chemists.

Property-Based Drug Design Merits a Nobel Prize

This interesting editorial highlights the most significant advancements in property-based drug design and its profound impact on oral small molecule drug discovery over the past 25 years. While not a comprehensive review, it underscores how this approach, combined with other techniques, has led to the development of more innovative and complex drugs, targeting challenging therapeutic areas and treating complicated diseases.

Chirality in Insecticide Design and Efficacy

This review delves into the latest advancements in chiral insecticides, including neonicotinoids, isoxazolines, and sulfiliminyls.

It explores their stereochemistry, synthesis, mode of action, and environmental behavior, highlighting the crucial role of chirality in enhancing insecticidal properties. The review underscores the need for ongoing research into new chiral compounds and advanced synthesis methods to improve effectiveness, reduce toxicity to non-target organisms, and promote environmental sustainability.

Globally Approved EGFR Inhibitors: Insights into Their Syntheses, Target Kinases, Biological Activities, Receptor Interactions, and Metabolism

This is an interesting review that discusses the development and clinical use of fourteen FDA-approved EGFR inhibitors for cancer therapy. It covers their chemical structures, target kinases, synthetic routes, crystal structures, binding interactions, cytotoxicity, and metabolism.

The Exploration of Chirality for Improved Druggability within the Human Kinome

This perspective explores how chirality can enhance the druggability of kinases, offering a valuable resource for developing innovative kinase inhibitors to meet current therapeutic needs.

Chiral Switch: Between Therapeutical Benefit and Marketing Strategy

This excellent review explores the evolution of the chiral switch concept over the past 25 years. Initially, it was believed that existing racemates would provide a rich source of new single enantiomer drugs, but this has proven challenging. However, in some cases, chiral switches have allowed racemate owners to extend their product lines, especially if marketed before the racemate’s patent expires.

Chirality: a key parameter in chemical probes

The article highlights how crucial it is to get chirality right in the pharmaceutical industry. Remember the thalidomide tragedy? It’s a stark reminder of what can go wrong when different isomers of a drug have different biological effects. The authors stress that developers and manufacturers need to be meticulous about chiral identity and purity to avoid wasting time and resources.

New Drugs Approved by FDA in 2023

This review article offers a fascinating look at the clinical applications and production methods of 29 new chemical entities (NCEs) approved by the FDA in 2023.

It provides a thorough understanding of the synthetic techniques used to create these drugs, hoping to inspire the development of new, efficient, and practical synthetic methods.

Biocatalysis

This fascinating paper delves specifically into the pivotal role of biocatalysis in asymmetric synthesis and its significant impact on intellectual property activities during the period 2014 to 2019.

The interdisciplinary nature of biocatalysis brings together various fields like biology, chemistry, engineering, and business, fostering innovation through their synergy. To highlight the inventive and innovative steps, only patents granted during this period are considered.

Chirality of New Drug Approvals (2013−2022): Trends and Perspectives

An interesting paper that critically examines the trends in chirality in new drug approvals over the past decade (2013−2022), tells why the study is of prominence and offers valuable suggestion for regulators.

2021 Nobal Price in Chemistry

In 2021, Benjamin List and David W.C. MacMillan were honored with the Nobel Prize in Chemistry for their pioneering work in developing asymmetric organocatalysis, a revolutionary tool for building molecules.

Asymmetric Synthesis of US-FDA Approved Drugs over Five Years (2016–2020): A Recapitulation of Chirality

An excellent review highlights the techniques used to synthesis FDA-approved chiral drugs from 2016 to 2020, focusing on asymmetric synthesis methods like chiral induction, resolution, and using chiral pools.

Interface Chirality: From Biological Effects to Biomedical Applications

A brilliant review that focus on the latest discoveries and advancements in chiral bio-interfaces. It delves into how interface chirality influences cell fate, tissue repair, and immune responses in organisms. Biological applications of interface chirality, such as drug delivery, antibacterial, antiviral, and antitumor activities, as well as biological signal detection are explored. Further, the challenges and potential applications of chiral bio-interfaces in the biomedical field are also discussed.