Medicinal Chemistry
Polar functional groups such as aldehydes, ketones, and amines, possessing free electron pairs, form hydrogen bonds readily with ...
pharmacological reactions. Theoretically, there are no absolutely insoluble compounds; every molecule is soluble in both the aqu ...
The effect of solubility on drug action is, however, usually a question of equilibration of the drug between the aqueous phase a ...
All neutral lipid-soluble substances have depressant (anesthetic) properties. This activity is most pronounced in lipid-rich ce ...
partition coefficients, and to simplify the determination of P values for small molecules. The fragmental constants are determin ...
that are amphiphilic(i.e., containing hydrophobic as well as hydrophilic groups) will concentrate at surfaces and thereby influe ...
room his serum level of phenytoin was “undetectable”; six months earlier, a routine measurement had revealed a serum phenytoin l ...
(on the order of 4–8 kJ/mol), and is easily overcome by thermal motion unless the molecule is made rigid or because nonbonding i ...
is not conformationally constrained. Many publications have proposed receptor mapping techniques based on the distances between ...
cis/transisomerism without the presence of a double bond; the restriction on their rotation is ensured by the ring system itself ...
planar compounds sometimes have the capacity to insert themselves within nucleic acids, potentially inducing cancer-causing chan ...
stereoselective biotransformations may have far-reaching consequences. For instance, microsomal hydroxylation of the tranquilize ...
38 MEDICINAL CHEMISTRY Figure 1.11 Stereoisomers: a carbon atom bonded to four different substituents in a chiral carbon or a st ...
activity of the eutomer and distomer is called the eudismic ratio; the expression of the eudismic index is In a series of agonis ...
turn produces a nerve impulse that the brain perceives as vision. Without light, this cis/trans isomerization would take 1100 ye ...
effect of inter-ionic forces decreases by the square of the distance over which they act. Such inductive forces as van der Waals ...
contain many ionic species (phospholipids, proteins) that can repel or bind ionic drugs; and ion channels, usually lined with po ...
on submolecular biology, directed attention to charge-transfer complexes (see section 2.3.5). The energies of the highest occupi ...
Molecular modeling and quantum pharmacology calculations have emerged as extremely important techniques in modern medicinal chem ...
representing the energy and properties of an individual electron within the molecule, and where these unknown molecular orbitals ...
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