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

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About: Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors Goto Sponge NotDistinct Permalink

An Entity of Type : schema:ScholarlyArticle, within Data Space : wasabi.inria.fr associated with source document(s)

Attributes	Values
type	Academic Article research paper schema:ScholarlyArticle
isDefinedBy	Covid-on-the-Web dataset
has title	Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors
Creator	Balzarini, Jan Andrei, Graciela Snoeck, Robert González-Muñiz, Rosario Pérez-Faginas, Paula Aranda, M Teresa García-López, M
Source	Elsevier; Medline; PMC
abstract	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 1H NMR as a γ-type reverse turn, seems to have influence on the activity of these molecules.
has issue date	2011-02-01(xsd:dateTime)
bibo:doi	10.1016/j.bmc.2010.12.052
bibo:pmid	21256035
has license	els-covid
sha1sum (hex)	d7f31ab2a2fddfcf28f5a3a16c2d81aac494f6d7
schema:url	https://doi.org/10.1016/j.bmc.2010.12.052
resource representing a document's title	Synthesis and SAR studies on azetidine-containing dipeptides as HCMV inhibitors
has PubMed Central identifier	PMC7127091
has PubMed identifier	21256035
schema:publication	Bioorganic & Medicinal Chemistry
resource representing a document's body	covid:d7f31ab2a2fddfcf28f5a3a16c2d81aac494f6d7#body_text
is schema:about of	named entity 'C-terminal' named entity 'azetidine' named entity 'dipeptide' named entity 'C-terminal' named entity 'reverse turn' named entity 'HCMV' named entity 'SYNTHESIS' named entity 'RESTRICTION' named entity 'DIPEPTIDE' covid:arg/d7f31ab2a2fddfcf28f5a3a16c2d81aac494f6d7 named entity 'RESIDUE' named entity 'N-TERMINUS' named entity 'CONTAINING' named entity 'HCMV' named entity 'AZETIDINE' named entity 'STUDIES' named entity 'HAVE' named entity 'TYPE' named entity 'SAR' named entity 'C-TERMINUS' named entity 'INHIBITORS' named entity 'DIPEPTIDES' named entity '1 H' named entity 'SYNTHESIZED' named entity 'ACTIVITY' named entity 'C-TERMINAL SIDE' named entity 'ABSOLUTE' named entity 'MOIETY' named entity 'MODIFIED' named entity 'REQUIREMENTS' named entity 'REVERSE TURN' named entity 'INDUCED' named entity 'CONTAINING' named entity 'NMR' named entity 'ANTIVIRAL ACTIVITY' named entity 'ALIPHATIC' named entity 'CARBOXAMIDE GROUP' named entity 'IDENTIFIED BY' named entity 'CHAIN' named entity 'INVOLVING' named entity 'SAR' named entity 'THESE' named entity 'PROTOTYPE' named entity 'EVALUATED' named entity 'SERIES' named entity 'HCMV' named entity 'STUDIES' named entity 'DESCRIBED' named entity 'INHIBITOR' named entity 'AZETIDINE' named entity 'INFLUENCE' named entity 'MOLECULES' named entity 'Aliphatic' named entity 'structurally' named entity 'activity' named entity 'HCMV' named entity 'side-chain' named entity 'C-terminus' named entity 'dipeptide' named entity 'dipeptide' named entity 'H NMR' named entity 'azetidine' named entity 'C-terminal' named entity 'benzyloxycarbonyl' named entity 'azetidine' named entity 'HCMV' named entity 'dipeptides' named entity 'SAR studies' named entity 'NMR' named entity 'sulfonyl' named entity 'MeOH' named entity 'protons' named entity 'DIC' named entity 'azetidine' named entity 'ethanol'

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