About: Synthesis, structure–activity relationship and antiviral activity of 3′-N,N-dimethylamino-2′,3′-dideoxythymidine and its prodrugs

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About: Synthesis, structure–activity relationship and antiviral activity of 3′-N,N-dimethylamino-2′,3′-dideoxythymidine and its prodrugs 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, structure–activity relationship and antiviral activity of 3′-N,N-dimethylamino-2′,3′-dideoxythymidine and its prodrugs
Creator	Rai, Diwakar Yadav, Dipti De Clercq, Erik Kumari, Garima Pannecouque, C Singh, Ramendra
Source	Elsevier; Medline; PMC
abstract	Abstract A probable NRTI molecule, viz. 3′-N,N-dimethylamino-2′,3′-dideoxythymidine (4) and its 5′-O-carboxyl ester prodrugs – 5′-(N-α-BOC-l-phenylalanyl)-3′-N,N-dimethylamino-2′,3′-dideoxythymidine (5), 5′-l-phenylalanyl-3′-N,N-dimethylamino-2′,3′-dideoxythymidine (6) and 5′-decanoyl-3′-N,N-dimethylamino-2′,3′-dideoxythymidine (7) have been synthesized and screened against HIV, HSV-1 and 2, parainfluenza-3, vesicular stomatitis and several other viruses. The compound 6 showed good antiviral activity with EC50 value 0.03μM (SI=8) against VSV in Hela and HEL cell lines. However, the lead compound 4 and its derivatives 5, 6 and 7 showed no remarkable activity against HIV-1 and other viruses. Molecular docking studies with HIV-1 RT using DS 2.5 and pymol softwares have shown marked differences in the interaction patterns between the lead compound 4 and AZT.
has issue date	2010-09-30(xsd:dateTime)
bibo:doi	10.1016/j.ejmech.2010.05.028
bibo:pmid	20538384
has license	els-covid
sha1sum (hex)	be3a41cd12211017865f94cf873f2f19fdc4fc51
schema:url	https://doi.org/10.1016/j.ejmech.2010.05.028
resource representing a document's title	Synthesis, structure–activity relationship and antiviral activity of 3′-N,N-dimethylamino-2′,3′-dideoxythymidine and its prodrugs
has PubMed Central identifier	PMC7127469
has PubMed identifier	20538384
schema:publication	European Journal of Medicinal Chemistry
resource representing a document's body	covid:be3a41cd12211017865f94cf873f2f19fdc4fc51#body_text
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