Fundamentals of Medicinal Chemistry

The introduction or removal of charged groups or groups that can form ions into or out of a structure may also have a marked aff ...

2.4 Sources of drugs and lead compounds The discovery of a new drug is part luck and part structured investigation (see section ...

O O H H CH 2 OH O H OH O H H H OCH 3 H H OH H CH 3 H OH CH 3 OH CH 3 OH O O HO Figure 2.1 The common foxglove and the structure ...

as there is no doubt that they will yield further useful therapeutic agents in the future. 2.4.2 Drug synthesis The most popular ...

and target system. Unfortunately, classifying drugs according to their chemical structural type has the disadvantage that member ...

ENTERAL route, e.g. via oral administration. Other sites EXCRETION KIDNEY (urine) LUNGS exhaled gases Membrane Desired biologica ...

Consequently, at an appropriately early stage in its development, the design of a drug should also take into account the nature ...

2.7 Introduction to drug action The action of a drug is believed to be due to the interaction of that drug with endogenous and e ...

that a drug molecule has the correct balance between its polar (hydrophilic) and nonpolar (hydrophobic) groups. Drugs that are t ...

is of particular importance in that serum proteins can act as enzymes that catalyse the breakdown of the drug. Decompositions su ...

CH 3 CH 3 CH 3 CH 3 CH 2 CH 3 CH 2 CH 3 CH 3 NH 2 CH 3 NHCOCH 2 N CH 2 CH 3 NHCOCH 2 N H CH 3 CH 3 CH 2 CH 3 NHCOCH 2 N HO CH 3 ...

Drugs are eliminated in the kidneys by eitherglomerular filtrationortubular secretion. However, some of the species lost by thes ...

its polarity and its relative solubilities in aqueous media and lipids. The stereo- chemistry of the drug is particularly import ...

2.8 Questions (1) Explainthemeaningoftheterms(a)leadcompound,(b)excipient,(c)parenteral administration, (d) pharmacophore and (e ...

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3 An Introduction to Drug Discovery 3.1 Introduction Drug discovery is part luck and part structured investigation. At the begin ...

Basic research into the disease process and its causes. Assessment of the biochemical and biological processes of the disease an ...

3.2 Stereochemistry and drug design It is now well established that the shape of a molecule is normally one of the most importan ...

3.2.2 Conformation Early work in the 1950s and early 1960s by Schueler and Archer suggested that the flexibility of the structur ...

NH HN N Histamine N N H NH 2 C HN N H H NH 2 H H H Steric hindrance between the H atoms Conformational restriction by the use of ...