- Synthesis and evaluation of highly selective quinazoline-2,4-dione ligands for sphingosine-1-phosphate receptor 2
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A series of twenty-nine new quinazoline-2,4-dione compounds were synthesized and their IC50 values for binding toward sphingosine-1-phosphate receptor 2 (S1PR2) were determined using a [32P]S1P binding assay. Seven compounds 2a, 2g, 2h, 2i, 2j, 2k, and 5h exhibit high S1PR2 binding potencies (IC50 values 98%), and high molar activity (153-222 GBq μmol-1, at the end of bombardment). [11C]2a and [11C]2i were further evaluated by the ex vivo biodistribution study. The results showed that both tracers have low brain uptake, preventing their potential for neuroimaging application. Further explorations of this class of S1PR2 PET tracers in peripheral tissue diseases are underway. This journal is
- Gropler, Robert J.,Klein, Robyn S.,Liu, Hui,Luo, Zonghua,Tu, Zhude,Yu, Yanbo
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p. 202 - 207
(2022/03/30)
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- Sequential Oxidative Fragmentation and Skeletal Rearrangement of Peroxides for the Synthesis of Quinazolinone Derivatives
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For the first time, the sequential reaction of peroxyoxindole that involves base-promoted oxidative fragmentation to isocyanate formation and primary amine or amino alcohol accelerated skeletal rearrangement to synthesize exo-olefinic-substituted quinazolinone or oxazoloquinazolinone is reported. The advantages of this new reaction include a broad substrate scope and transition-metal-free and room-temperature conditions. The formation of the isocyanate as a key intermediate that accelerates oxidative skeletal rearrangement has been confirmed by trapping experiments and spectroscopic evidence.
- Gnanaprakasam, Boopathy,Shaikh, Moseen A.,Ubale, Akash S.
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p. 9621 - 9636
(2021/07/28)
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- 2,4-DIOXO-QUINAZOLINE-6-SULFONAMIDE DERIVATIVES AS INHIBITORS OF PARG
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The present invention relates to compounds of formula I that function as inhibitors of PARG (Poly ADP-ribose glycohydrolase) enzyme activity wherein R1a, R1b, R1c, R1d, R1e, W, X1, X2, X3, X4, X5, X6, X7, c are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which PARG activity is implicated.
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Paragraph 00199; 00200
(2016/07/05)
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- Synthesis of novel quinazoline-4-one derivatives and their acyclonucleoside analogs
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A number of quinazolin-4-one derivatives were synthesized. Reaction of the 2-hydrazonoquinazoline-4-one derivatives with aldoses afforded the corresponding sugar hydrazones which on treatment with ferric chloride to afford the corresponding acyclic nucleoside analogues.
- Zahran, Magdy A.-H.,Ali, Omar M.,Zeid, Ibrahim F.,Rageb, Elham
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p. 2121 - 2124
(2012/08/28)
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- Molybdenum-mediated synthesis of quinazolin-4(3H)-ones via cyclocarbonylation using microwave irradiation
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A new, efficient and practical synthesis of quinazolin-4(3H)-ones is reported via molybdenum-mediated cyclocarbonylation using microwave irradiation. These methods allow access to a wide range of quinazolin-4(3H)-ones in reasonable yields without the need for gaseous carbon monoxide and palladium catalysts. A range of reactions illustrating the wide scope of this chemistry was carried out and all proceeded in reasonable yields.
- Roberts, Bryan,Liptrot, David,Luker, Tim,Stocks, Michael J.,Barber, Catherine,Webb, Nicola,Dods, Robert,Martin, Barrie
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supporting information; experimental part
p. 3793 - 3796
(2011/08/06)
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- Metal and phosgene-free synthesis of 1H-quinazoline-2,4-diones by selenium-catalyzed carbonylation of o-nitrobenzamides
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1H-Quinazoline-2,4-diones were efficiently synthesized by selenium-catalyzed carbonylation of o-nitrobenzamides under relatively mild conditions. In situ-generated carbonyl selenide (SeCO) is proposed to initiate the catalytic carbonylation. Thus, a concise transition metal and phosgene-free synthetic route to potentially bioactive-substituted 1H-quinazoline-2,4-dione derivatives has been developed.
- Wu, Xiaowei,Yu, Zhengkun
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experimental part
p. 1500 - 1503
(2010/04/29)
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- Convenient Preparation of N-substituted 2-Amino-4H-3,1-benzoxazin-4-ones and 3-Substituted 2,4(1H,3H)-Quinazolinediones
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Room temperature of 2-(3-arylureido)benzoic acids (1) and methyl2-(3-alkyl-, or 3-arylureido)-benzoates (2) with concentrated sulfuric acid leads to N-substituted 2-amino-4H-3,1-benzoxazin-4-ones (3) in generally very good yields.The isomeric 3-substitute
- Papadopoulos, E. P.,Torres, C. D.
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p. 269 - 272
(2007/10/02)
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