783371-72-2Relevant articles and documents
Synthesis of new di- And triamides as potential organocatalysts for asymmetric aldol reaction in water
Aydogan, Feray,Keskin, Elif,Yolacan, Cigdem
, p. 1014 - 1023 (2021/06/07)
New di- or triamide organocatalysts derived from (L)-proline were synthesized and successfully used in the direct asymmetric aldol reaction of aliphatic ketones and aromatic aldehydes in water at 0 °C in the presence of benzoic acid as co-catalyst. (S)-me
Structural optimization of a retrograde trafficking inhibitor that protects cells from infections by human polyoma- and papillomaviruses
Carney, Daniel W.,Nelson, Christian D.S.,Ferris, Bennett D.,Stevens, Julia P.,Lipovsky, Alex,Kazakov, Teymur,Dimaio, Daniel,Atwood, Walter J.,Sello, Jason K.
, p. 4836 - 4847 (2014/10/16)
Human polyoma- and papillomaviruses are non-enveloped DNA viruses that cause severe pathologies and mortalities. Under circumstances of immunosuppression, JC polyomavirus causes a fatal demyelinating disease called progressive multifocal leukoencephalopathy (PML) and the BK polyomavirus is the etiological agent of polyomavirus-induced nephropathy and hemorrhagic cystitis. Human papillomavirus type 16, another non-enveloped DNA virus, is associated with the development of cancers in tissues like the uterine cervix and oropharynx. Currently, there are no approved drugs or vaccines to treat or prevent polyomavirus infections. We recently discovered that the small molecule Retro-2cycl, an inhibitor of host retrograde trafficking, blocked infection by several human and monkey polyomaviruses. Here, we report diversity-oriented syntheses of Retro-2cycl and evaluation of the resulting analogs using an assay of human cell infections by JC polyomavirus. We defined structure-activity relationships and also discovered analogs with significantly improved potency as suppressors of human polyoma- and papillomavirus infection in vitro. Our findings represent an advance in the development of drug candidates that can broadly protect humans from non-enveloped DNA viruses and toxins that exploit retrograde trafficking as a means for cell entry.
Synthesis of 2,3-dihydro-4(1H)-quinazolinones
Escalante, Jaime,Flores, Patricia,Priego, Jaime M.
, p. 2019 - 2032 (2007/10/03)
An improved procedure for the synthesis of 2-substituted 2,3-dihydro-4(1H)-quinazolinones through diastereomer separation of the corresponding quinazolinones derivatives is presented. The determination of their absolute configurations was obtained by X-Ra