Unknown

Dataset Information

0

Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors.


ABSTRACT: SAR studies on an azetidine-containing dipeptide prototype inhibitor of HCMV are described. Three series of structurally modified analogues, involving substitutions at the N- and C-terminus, and at the C-terminal side-chain were synthesized and evaluated for antiviral activity. Aliphatic or no substituents at the C-carboxamide group, an aliphatic C-terminal side-chain, as well as a benzyloxycarbonyl moiety at the N-terminus were absolute requirements for anti-HCMV activity. The conformational restriction induced by the 2-azetidine residue into the dipeptide derivatives, identified by (1)H NMR as a γ-type reverse turn, seems to have influence on the activity of these molecules.

SUBMITTER: Perez-Faginas P 

PROVIDER: S-EPMC7127091 | biostudies-literature |

REPOSITORIES: biostudies-literature

Similar Datasets

| S-EPMC8217302 | biostudies-literature
| S-EPMC3966491 | biostudies-literature
| S-EPMC3164827 | biostudies-literature
| S-EPMC2956582 | biostudies-literature
| S-EPMC6160994 | biostudies-literature
| S-EPMC6755904 | biostudies-literature
| S-EPMC4266361 | biostudies-literature
| S-EPMC4233352 | biostudies-literature
| S-EPMC8037530 | biostudies-literature
| S-EPMC2888690 | biostudies-literature