TABLE 1.
Building blocks used in the bicyclic guanidine PS-SCLa
No. | Building block
|
||
---|---|---|---|
R1 | R2 | R3 | |
1 | 3-Phenylbutyric acid | l-Alanine | l-Alanine |
2 | m-Tolylacetic acid | l-Phenylalanine | l-Phenylalanine |
3 | 3-Fluorophenylacetic acid | Glycine | l-Isoleucine |
4 | p-Tolylacetic acid | l-Isoleucine | l-Lysine |
5 | 4-Fluorophenylacetic acid | l-Lysine | l-Leucine |
6 | 3-Metoxyphenylacetic acid | l-Leucine | l-Methionine |
7 | 4-Metoxyphenylacetic acid | l-Methionine | l-Arginine |
8 | 4-Ethoxyphenylacetic acid | l-Arginine | l-Valine |
9 | 3-(3,4-Dimethoxyphenyl)-propionic acid | l-Valine | l-Tyrosine |
10 | 4-Biphenylacetic acid | l-Tyrosine | d-Alanine |
11 | 3,4-Dimethoxyphenylacetic acid | d-Alanine | d-Phenylalanine |
12 | Phenylacetic acid | d-Phenylalanine | d-Isoleucine |
13 | Hydrocinnamic acid | d-Isoleucine | d-Lysine |
14 | 4-Phenylbutyric acid | d-Lysine | d-Leucine |
15 | Butyric acid | d-Leucine | d-Arginine |
16 | Heptanoic acid | d-Arginine | d-Valine |
17 | Isobutyric acid | d-Valine | d-Tyrosine |
18 | (+/−)-2-Methylbutyric acid | d-Tyrosine | l-α-Aminobutyric acid |
19 | Isovaleric acid | l-α-Aminobutyric acid | α-Aminoisobutyric acid |
20 | 3-Methylvaleric acid | l-Norvaline | l-Norvaline |
21 | 4-Methylvaleric acid | d-Norvaline | d-Norvaline |
22 | t-Butylacetic acid | l-Norleucine | l-Norleucine |
23 | Cyclohexanecarboxylic acid | d-Norleucine | d-Norleucine |
24 | Cyclohexylacetic acid | l-Ornithine | l-Ornithine |
25 | Cyclohexylbutyric acid | l-3-(2-Naphthyl)-alanine | l-3-(2-Naphthyl)-alanine |
26 | Cycloheptanecarboxylic acid | d-3-(2-Naphthyl)-alanine | d-3-(2-Naphthyl)-alanine |
27 | Lactic acid | l-Cyclohexylalanine | l-Cyclohexylalanine |
28 | Acetic acid | d-Cyclohexylalanine | d-Cyclohexylalanine |
29 | Cyclobutanecarboxylic acid | l-Methionine sulfone | l-Methionine sulfone |
30 | Cyclopentanecarboxylic acid | l-p-Nitrophenylalanine | l-p-Nitrophenylalanine |
31 | 3-Cyclopentylpropionic acid | d-p-Nitrophenylalanine | l-p-Nitrophenylalanine |
32 | 3-Cyclohexylpropionic acid | l-p-Chlorophenylalanine | l-p-Chlorophenylalanine |
33 | 4-Methyl-cyclohexanecarboxylic acid | d-p-Chlorophenylalanine | d-p-Chlorophenylalanine |
34 | 4-t-Butyl-cyclohexanecarboxylic acid | l-p-Fluorophenylalanine | l-p-Fluorophenylalanine |
35 | 2-Norbornaneacetic acid | d-p-Fluorophenylalanine | d-p-Fluorophenylalanine |
36 | 1-Adamantaneacetic acid | l-ɛ-Acetyl-lysine | l-ɛ-Acetyl-lysine |
37 | 2-Ethylbutyric acid | l-3-Pyridyl-alanine | l-3-Pyridyl-alanine |
38 | 3,3-Diphenylpropionic acid | d-3-Pyridyl-alanine | d-3-Pyridyl-alanine |
39 | 2-Methyl-4-nitroimidazolepropionic acid | l-Cyclohexylglycine | l-Cyclohexylglycine |
40 | Cyclopentylacetic acid | d-Cyclohexylglycine | d-Cyclohexylglycine |
41 | Indole-3-acetic acid | l-t-Glycine | l-t-Butyl-glycine |
42 | pFmoc-amino-l-phenylalanineb | p-Fmoc-amino-l-phenylalanine | |
43 | p-Fmoc-amino-d-phenylalanine | p-Fmoc-amino-d-phenylalanine | |
44 | O-Ethyl-l-tyrosine | O-Ethyl-l-tyrosine | |
45 | O-Ethyl-d-tyrosine | O-Ethyl-d-tyrosine | |
46 | l-Aspartic acid-β-fluorenylmethyl ester | p-Iodo-l-phenylalanine | |
47 | d-Aspartic acid-β-fluorenylmethyl ester | p-Iodo-d-phenylalanine | |
48 | p-Iodo-l-phenylalanine | O-Methyl-l-tyrosine | |
49 | p-Iodo-d-phenylalanine | O-Methyl-d-tyrosine | |
50 | O-Methyl-l-tyrosine | ||
51 | O-Methyl-d-tyrosine |
See reference 22.
Fmoc, 9-fluorenylmethoxycarbonyl.