Medicinal Chemistry of Antifungal Drugs

November 23rd, 2015

In this section, we offer a comprehensive assessment of the medicinal chemistry of antifungal drugs. Their medicinal chemistry could not be more important, not least because fungal skin infections are now the fourth most common disease in the world today – afflicting up to 1 billion people. We begin by explaining the structural features that […]

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Medicinal Chemistry of Macrolides

October 18th, 2015

Macrolide antibiotics are of immense importance in the battle against bacterial infections today – even with the ever present rise of resistance. Here, we take a comprehensive glance at the medicinal chemistry of macrolides – a bacteriostatic group of drugs whose structure tells us much about how they work. About Macrolides As the name suggests, […]

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Medicinal Chemistry of Anticancer Drugs I

October 12th, 2015

This section will describe the medicinal chemistry of anticancer drugs. Sometimes called antineoplastic agents, these drugs are of immense importance to society. This section will focus on, specifically, DNA-interactive drugs. Cancer and Chemotherapy Contrary to popular belief, cancer is not a single disease. Cancer is the generic term used to describe a large group of […]

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Medicinal Chemistry of Antiviral Drugs

December 3rd, 2014

This section takes a look at the medicinal chemistry of antiviral drugs – looking at their fundamental structures to elucidate more about their functional properties. Viruses are infectious agents that are capable of replicating only when inside the living cells of living organisms. Diseases such as influenza (flu), measles, mumps, rubella, SARS, AIDS, and chicken […]

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Medicinal Chemistry of Antimalarial Drugs

December 3rd, 2014

The following article looks at the medicinal chemistry of antimalarial drugs. It will look at – in detail – quinine and quinine-related drugs. In a previous article, we briefly described malaria and artemisinin as a lead compound for new antimalarials. We now turn our attention to the other antimalarial drugs. Understanding the chemistry of these […]

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Medicinal Chemistry of Beta-Lactam Antibiotics

December 3rd, 2014

This section focuses on the medicinal chemistry of beta-lactam antibiotics; the second part of our series on the medicinal chemistry of antibacterial compounds. Penicillin derivatives, cephalosporins, monobactams and carbapenems all belong to this popular class of drugs. A four-membered lactam ring, known as a β-lactam ring, is a common structural feature of this class (see […]

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Medicinal Chemistry of Antibacterial Drugs

December 3rd, 2014

The medicinal chemistry of antibacterial drugs is, like many fields of the subject, a rapidly evolving subject – not least because of the ever-present rise of resistance. Here, we take a quick but comprehensive glance at some of the main classes and what structural features elicit their antibacterial properties. Antibacterial drugs are compounds that are […]

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Medicinal Chemistry of Vitamins — Water Soluble

December 3rd, 2014

This section takes a detailed look at the medicinal chemistry of vitamins; specifically analysing the water-soluble vitamins and how they are used in a therapeutic context. The water-soluble group of vitamins include the B vitamins and Vitamin C. Excretion is generally more facile compared to the fat-soluble vitamins. Although these vitamins are structurally diverse, they […]

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Medicinal Chemistry of Vitamins — Fat Soluble

December 3rd, 2014

This section takes a detailed look at the medicinal chemistry of vitamins – this time focussing on fat-soluble vitamins. Vitamins are organic compounds required by an organism as vital nutrients in certain quantities in order to survive. These compounds have many roles. They are involved in biochemical processes such as metabolism and gene expression.  Hypovitaminosis […]

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Medicinal Chemistry of Radiopharmaceuticals

December 3rd, 2014

This section presents an overview of the medicinal chemistry of radiopharmaceuticals – those that are typically used in nuclear medicine. Radiopharmaceuticals are pharmaceuticals that contain a radioactive nuclide, sometimes referred to as radionuclides or radioisotopes. Radiopharmacology is the branch of pharmacology concerned with the study of radiopharmaceuticals. The field nuclear medicine is a branch of […]

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Medicinal Chemistry of Herbs

December 3rd, 2014

This section takes a look at the medicinal chemistry of herbs; introducing you to the very basics of phytochemistry. Introduction to Phytochemistry We begin this section of medicinal chemistry of herbs by understanding the intrinsic properties of plants. Plants are known good sources of pharmacologically active compounds and lead structures. Artemisinin is an example of […]

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Medicinal Chemistry — Understanding Drug Metabolism

December 3rd, 2014

This section is a continuation of a previous article on drug metabolism. This article focusses on structural changes that occur when drugs undergo biotransformation, as well as its importance in drug design and medicinal chemistry. Following entry to the body, drug molecules undergo metabolic transformations to derivatives known as metabolites. These metabolic transformations are sometimes […]

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Medicinal Chemistry — Understanding Enzyme Kinetics

December 2nd, 2014

Here, we continue our understanding of drug targets, this time focusing on enzyme kinetics. Enzymes are biological macromolecules that act as catalysts in biochemical reactions. The metabolic processes and chemical reactions that sustain life often involve enzymes. Enzymes basically decrease the Gibbs free energy of activation (ΔG‡), accelerating the rate of reaction. The majority of […]

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Medicinal Chemistry — Understanding Drug Targets

December 2nd, 2014

This section will go over drug targets in biological systems from a medicinal chemistry perspective. The purpose of this section is to give an overview of the molecular structures of major macromolecular targets in the body. The main drug targets in the body are normally large molecules. Macromolecule is the word used to describe large […]

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Medicinal Chemistry Glossary

December 2nd, 2014

Covering structural features such as functional groups, cyclic aliphatic compounds, and heterocycles found in organic compounds that are used as drugs – this medicinal chemistry glossary is the complete resource for your studies. The first half of this extensive medicinal chemistry glossary will focus on some of the most important nomenclature that one comes across […]

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Drug Design — A Special Case Study on Malaria

December 2nd, 2014

Human malaria continues to be a major parasitic disease affecting nearly half of the human population. This case study explores the discovery of the lead compound, artemisinin. Looking back on previous articles, drug design techniques used to produce derivatives of the lead compound will be discussed. Malaria Malaria is an infectious disease known since ancient […]

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Drug Design — The Complete Pharmacokinetics Guide

December 2nd, 2014

The following article builds on previous drug design articles. This article mainly focuses on the drug design techniques used by medicinal chemists to improve the pharmacokinetic properties of lead compounds and drugs. Drug design strategies used to optimise binding site interactions of modified lead compounds were described earlier. However, a compound with good binding site […]

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Drug Design: Structure — Activity Relationships

December 2nd, 2014

This is the third medicinal chemistry article, with previous sections focussing on lead compounds as well as providing a general overview of the subject of medicinal chemistry. This section takes a step forward in describing in more detail what we mean by structure-activity relationships and how it affects drug design. Possible sources of lead compounds […]

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Modern Drug Discovery — Lead Identification

December 2nd, 2014

This section follows on from our overview of medicinal chemistry by focussing its attention on lead identification in modern drug discovery. In this regard, the article is going to look at the stages of drug development as well as the possible sources of lead compounds and novel drugs in modern times. Drug discovery and development […]

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Introduction to Medicinal Chemistry

December 2nd, 2014

This is the first section in our series on medicinal chemistry – it introduces the subject as well as providing you with an introduction to medicinal chemistry by looking at drug targets and intermolecular interactions. Medicinal chemistry is an interdisciplinary field of study combining aspects of organic chemistry, physical chemistry, pharmacology, microbiology, biochemistry, as well […]

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