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OH
OH
O
H HO
O
O
H HO
NH
O
NH
O
N
N
N
N
N
O
O
N
N
N
HN
HN
HN
NH
NH
HN
O
O
O
O
O
O
O
O
HN
HN
NH
NH
O
O
O
HN
NH 2
O
O
O
HN
NH 2
NH
HN
OO
NH
HN
OO
NH
NH
O
O
H 2 N
H 2 N
O
O
H 2 N
H 2 N
OH
OH
29
30
FIGURE 12.12
Tyrocidine based potent glycopeptide antibiotics Tyc4PG-14 (73) and
Tyc4PG-15.
synthesized analogs of drug zanamivir, a neuraminidase inhibitor used in the treatment
and prophylaxis of avian influenza (H5N1) caused by influenza A viruses [56]. The
neuraminidase enzyme stimulates cleavage of sialic acid from glycoproteins and
glycolipids of the host cells, which is a key step for replication of influenza virus.
A library of 16 C -4 triazole substituted zanamivir analogs were synthesized using
R
N
OH NH 2
R = COOH
N
O
N
OH
CH 3
O
OH
O
O
HO
O
HO
Cl
O
OH
OH
Cl
O
O
O
O
HO
OH
Cl
O
HO
OH
O
O
N
N
N
Cl
O
O
O
O
N
N
N
H
H
N
H
O
HO
O
H
NH
O
H
H
O
O
NH
O
HO
O
NH 2
O
NH 2
OH
OH
O
OH
OH
HO
HO
31
32
Vancomycin
Twice as potent as Vancomycin
FIGURE 12.13
Vancomycin analouge.
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