- Synthesis of new di- And triamides as potential organocatalysts for asymmetric aldol reaction in water
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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
- Aydogan, Feray,Keskin, Elif,Yolacan, Cigdem
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p. 1014 - 1023
(2021/06/07)
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- A novel approach for the synthesis of functionalized hydroxylamino derivative of dihydroquinazolinones
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A new metal-free and modular approach for the synthesis of various functionalized dihydroquinazolinones has been developed from isatoic anhydride, amines, 4-chloro-N-hydroxybenzimidoylchloride to yield up to 71%. The reaction has been screened in various bases, solvents at different temperatures. The substrate scope of the reaction has been studied with various amines and the possible reaction mechanism for this reaction has also been proposed.
- Jaganmohan, Chikkanti,Vinay Kumar,Venkateshwarlu,Mohanty, Sandeep,Kumar, Jaydeep,Venkateswara Rao,Raghunadh, Akula,Tadiparthi, Krishnaji
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supporting information
p. 2163 - 2170
(2020/06/10)
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- Structural optimization of a retrograde trafficking inhibitor that protects cells from infections by human polyoma- and papillomaviruses
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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.
- 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.
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p. 4836 - 4847
(2014/10/16)
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- Sirtuin Inhibiting Compounds
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Provided herein are compositions and methods for treating or preventing cancer and autoimmune diseases. Compositions comprise a sirtuin inhibitory compound that decreases the activity of a sirtuin, such as SIRT1 or Sir2. Exemplary methods comprise contact
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Page/Page column 30; 32
(2009/06/27)
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- Synthesis of 2,3-dihydro-4(1H)-quinazolinones
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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
- Escalante, Jaime,Flores, Patricia,Priego, Jaime M.
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p. 2019 - 2032
(2007/10/03)
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- Synthesis of enantiopure cis- and trans-2-aminocyclohexane-1-carboxylic acids from octahydroquinazolin-4-ones
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The chemoselective and diastereoselective hydrogenation of 2,3-dihydro-3-[(S)-α-methylbenzyl]-4-quinazolinone 2 affords octahydroquinazolinones cis-3 and cis-4. Epimerization of cis-3 and cis-4 using t-BuO-K+ produces trans-5 and tra
- Priego, Jaime,Flores, Patricia,Ortiz-Nava, Claudia,Escalante, Jaime
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p. 3545 - 3549
(2007/10/03)
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- Synthesis and structure of chiral 2,6-bis[(2-carbamoyl- phenyl)carbamoyl]pyridine ligands
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The synthesis and structure of a series of enantiomerically pure 2,6- bis[(2-carbamoylphenyl)carbamoyl]pyridine ligands (H22a-c) are described. Appended from the aryl groups are optically active groups which provide a chiral environment around
- Yu, Qiang,Baroni, Timothy E.,Liable-Sands, Louise,Rheingold, Arnold L.,Borovik
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p. 6831 - 6834
(2007/10/03)
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