Fundamentals of Medicinal Chemistry

OH R R R O O Nu Enz Oxidation (Oxidoreductase) Michael type addition of Enz-Nu Michael type addition of Enz-Nu Elimination (Lyas ...

active site. Consequently, it has been proposed thatstable compounds with structures similar to those of these transition state ...

synthesis, which is the conversion of N-carbamoyl aspartatic acid to dihydrooro- tic acid. It was found that PALA bound 10 3 tim ...

new agonists is usually the structure of the endogenous ligand or its pharmaco- phore. This information is normally obtained fro ...

Response 0.0 Agonist s normal response (antagonist is absent) Antagonist, ideal case (agonist is absent) Concentration agonist % ...

the receptor. Furthermore, in order to bind to the receptor, the conformations and configuration of the new antagonist should be ...

an enzyme in the metabolic pathway in the cell. Both these types of intervention inhibit the targeted metabolic pathway to a lev ...

the biosynthesis of purines and pyrimidines (Figure 7.9). In addition, DHFR also catalyses the conversion of folic acid to DHF. ...

O N O N H F Deoxribose-5'-Phosphate O N O N H DNA Deoxyribose-5'-Phosphate O N Deoxribose-5'-Phosphate (dUMP) (dTMP) ON Various ...

of folic acid to DHF and DFH to THF (see Figures 7.9 and 7.12). Trimethoprim binds to bacterial DHFR but not human DHFR because ...

The insertion of an intercalation agent appears to occur via either the minor or major grooves of DNA. Compounds that act as int ...

Table 7.6 Some examples of the classes and compounds of anti-cancer agents that act by alkylation of nucleic acids. It is emphas ...

Antisense compounds were originally short lengths of nucleic acid chains that had base sequences that were complementary to thos ...

CONH 2 N CH 3 CONH 2 H H 2 N CH 3 NN NH N NH O NH CH 3 HO CH 3 HO CH 3 O O O NH O NH N S N S COR O O OH HO HO OH OCONH^2 OH OH B ...

CH 2 OCH 2 CH 2 O N N O H 2 N N HN Acyclovir O CH 3 O HN N HO O N 3 Zidovudine (AZT) Vidarabine HO HO HO NH 2 O N N N N Figure 7 ...

7.6.3 Inhibitors of viral protein synthesis The principal compounds that act as inhibitors of viral protein synthesis are the in ...

(continued) (5) Explain the meaning of the term ‘suicide inhibitor’. (6) Explain how the transition state of a reaction can be u ...

8 Pharmacokinetics 8.1 Introduction to pharmacokinetics The action of a drug is initially dependent on it reaching its site of a ...

(a) Plasma concentration Time Time 0 Concentration in the excreted urine 0 (b) Figure 8.2 Typical variations in the concentratio ...

not contain this structural function or have structures where it is sterically hindered. If, for example, the drug is rapidly me ...