- Toward structurally novel and metabolically stable HIV-1 capsid-targeting small molecules
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HIV-1 capsid protein (CA) plays an important role in many steps of viral replication and represents an appealing antiviral target. Several CA-targeting small molecules of various chemotypes have been studied, but the peptidomimetic PF74 has drawn particul
- Casey, Mary C.,Du, Haijuan,Kankanala, Jayakanth,Kirby, Karen A.,Lalji Sahani, Rajkumar,Sarafianos, Stefan G.,Tedbury, Philip R.,Vernekar, Sanjeev Kumar V.,Wang, Lei,Wang, Zhengqiang,Xie, Jiashu,Zhang, Huanchun
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- COMPOSITIONS OF SPHINGOSINE-1-PHOSPHATE RECEPTOR 2 (S1PR2) BINDING AGENTS AND USES THEREOF
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Described are compounds for the binding of S1PR2, and imaging agents and pharmaceutical compositions including said compounds. Also described are methods employing the compounds, imaging agents, and pharmaceutical compositions. These methods include imaging and/or treatment of diseases associated with S1PR2.
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Paragraph 0187
(2020/12/08)
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- Synthesis, in vivo and in silico anticonvulsant activity studies of new derivatives of 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)acetamide
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In order to expand the arsenal of biologically active substances of anticonvulsive action by the interaction of 2-(2,4-dioxo-1,4-dihydroquinazolin-3(2H)-yl)acetic acid with the corresponding amines in the presence of N,N′-carbonyldiimidazole in the dioxan
- El Kayal, Wassim Mokhamad,Shtrygol, Sergiy Yu,Zalevskyi, Sergiy V.,Shark, Amjad abu,Tsyvunin, Vadim V.,Kovalenko, Sergiy M.,Bunyatyan, Natalya D.,Perekhoda, Lina O.,Severina, Hanna I.,Georgiyants, Victoriya A.
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p. 134 - 142
(2019/07/12)
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- A series of 2,4(1H,3H)-quinazolinedione derivatives: Synthesis and biological evaluation as potential anticancer agents
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A series of 6,7-disubstituted-3-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}quinazoline-2,4(1H,3H)-dione derivatives (7-34) were synthesized and their structures were elucidated on the basis of analytical and spectral (UV, IR, 1H-NMR, 13
- Akgun, Hulya,Yilmaz, Demet Us,Atalay, Rengul Cetin,Gozen, Damla
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- A Series of 2,4(1H,3H)-Quinazolinedione derivatives: Synthesis and biological evaluation as potential anticancer agents
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A series of 6,7-disubstituted-3-{2-[4-(substituted)piperazin-1-yl]-2-oxoethyl}quinazoline- 2,4(1H,3H)-dione derivatives (7-34) were synthesized and their structures were elucidated on the basis of analytical and spectral (UV, IR, 1H-NMR, 1
- Akgun, Hulya,Yilmaz, Demet Us,Atalay, Rengul Cetin,Gozen, Damla
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- Application of the 'direct amide cyclization' to peptides containing an anthranilic acid residue
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The 2,2-disubstituted 2H-azirin-3-amines 7a-7c were used as amino acid synthons to prepare linear peptides derived from anthranilic acid. These linear peptides, which contain α,α-disubstituted α-amino acids, were synthesized by using the 'azirine/oxazolon
- Philipova, Irena,Linden, Anthony,Heimgartner, Heinz
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p. 1711 - 1733
(2007/10/03)
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- Synthesis of 3-dipeptidyl-2,4(1H,3H)-quinazolinediones as potential anti-hypertensive agents
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Ouinazolinediones bearing a dipeptide side chain have been synthesized as potential anti-hypertensive agents.
- Rivero,Somanathan,Hellberg
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p. 2077 - 2086
(2007/10/03)
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- Solid phase synthesis of chiral 3-substituted quinazoline-2,4-diones
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The synthesis of chiral 3-substituted quinazoline-2,4-diones was performed starting from N-urethane anthranilamides. This synthetic pathway was applied in solid phase, from commercially available anthranilic acid that was bound to hydroxymethyl polystyrene resin via a carbamate linker. In both cases, cyclisation occurred under basic conditions to afford non-racemized quinazolinediones in high purity.
- Gouilleux, Laurent,Fehrentz, Jean-Alain,Winternitz,Martinez, Jean
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p. 7031 - 7034
(2007/10/03)
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- SYNTHESIS OF CHIRAL 3-SUBSTITUTED 2,4-(1H,3H)-QUINAZOLINEDIONES
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2-Carbomethoxyphenyl isocyanate and 6-nitro-2-carbomethoxyphenyl isocyanate were generated in situ from half-esters and then converted into the corresponding quainazolinediones using α-amino acids.This useful annelation process was found to be a general m
- Canonne, Persephone,Akssira, Mohamed,Dahdouh, Abdelaziz,Kasmi, Hicham,Boumzebra, Mohamed
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p. 1305 - 1314
(2007/10/02)
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- Reactions of o-Aminonitriles with Isocyanates. 2. A Facile Synthesis of Imidazoquinazoline-2,5-(3H,6H)dione
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Anthranilonitrile reacts with ethyl isocyanatoacetate to form 2-(3-ethoxycarbonylmethylureido)benzonitrile (3b) which, upon heating, or treatment with a base, undergoes a double cyclization to yield imidazo-quinazoline-2,5-(3H,6H)dione (5) in excel
- Papadopoulos, Eleftherios Paul
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p. 515 - 518
(2007/10/02)
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