Fundamentals of Medicinal Chemistry

Resin beads B C B A A D The bonding of the initial building blocks to the resin beads. Step ONE in the synthetic pathway. E F A− ...

6.3 Encoding methods A wide variety of encoding methods have been developed to record the history of a bead used in the Furka mi ...

Table 6.2 The use of oligonucleotides to encode amino acids in peptide synthesis Amino acid Structure Oligonucleotide code Glyci ...

Synthesis site Linker Primer (P) Tag site (1) Gly Divide into two aliquots (2) CACATG Gly (1) Met (2) ACGGTA (P)-CACATG Met (P)- ...

NO 2 C OO−C O O−(CH 2 )n−O−Ar RESIN−O Aryl halide tag Photolabile carbonate linker T1 T2 T3 T4 T5 T6 0 Cl Cl Cl Cl Cl Cl Cl Cl C ...

a synthesis. The silicon chip and beads are placed in a container known as acan that is porous to the reagents used in the synth ...

The acid chloride based set: The amine based set: A^1 + (B^1 ,B^2 ,B^3 ,B^4 ,B^5 ,B^6 ,B^7 ,B^8 ,B^9 ,B^10 ) A^2 + (B^1 ,B^2 ,B^ ...

to assess the components of the library. A key problem with very large com- binatorial libraries of mixtures is the large amount ...

synthesis and biological testing but using groups of nine reactants for the first step will give the amino acid that occupies th ...

7 Selected Examples of Drug Action at some Common Target Areas 7.1 Introduction The action of drugs and the sites at which they ...

and numerous channels connecting the intracellular fluid with the extracellular fluid. These channels allow ions and other small ...

Table 7.1 Some of the classes of compound that are used as antifungal agents. Note the common structural features. Class General ...

act by inhibiting cytochrome P-450 enzymes, in particular those that are essen- tial for the biosynthesis of ergosterol, the mai ...

7. 2. 1. 3 Phenols There are numerous phenolic antifungal agents (Table 7.1). They are believed to destroy sections of the cell ...

C-Terminus Two N-Termini Ions Channel C-Terminus (a) (b) (HOOC)Val−Gly−Ala−Leu−Ala−Val−Val−Val−Trp−Leu HOCH 2 CH 2 NHTrp−Leu−Trp ...

Table 7.2 Examples of drugs that inhibit the formation of cell wall synthesis Compound/Active against Structure Mode of action D ...

Vancomycin O O O Cl HOCH 2 R 2 O H NH H NH−COCHNHCOCHNHCOCHNHCOCHNHCOCH CHOH NHCH 3 CH 2 CH(CH 3 ) 2 HO OH OH H HOOC O CH 2 CONH ...

usually bind to an enzyme by strong covalent bonds. However, in both revers- ible and irreversible inhibition the inhibitor does ...

Uncompetitive inhibitorsare believed to form a complex with the enzyme– substrate complex. The formation of this complex prevent ...

COOH COOH OOH O O NHCOCHNHCO NHCOCHNHCO NHCOCHNHCO CH 2 OH CH (^2) CH 2 COOH O C O CH 3 O COOH O C− CH 3 O COOH O C O CH 3 O H ...