- BCL6-targeting aromatic ring five-membered aromatic heterocyclic micromolecular organic compound and derivative and application thereof
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The invention discloses an aromatic ring five-membered aromatic heterocyclic micromolecular organic compound or related analogues or pharmaceutically acceptable salts thereof. The structures of the compound are shown as formulas (I-IX). The invention also
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Paragraph 0171-0173; 0175
(2021/03/24)
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- Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: Optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches
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In our arduous efforts to develop new potent HIV-1 non-nucleoside reverse transcriptase (RT) inhibitors (NNRTIs), novel piperidine-linked [1,2,4]triazolo[1,5-a]pyrimidine derivatives were designed, synthesized and evaluated for their antiviral activities
- Huang, Boshi,Li, Cuicui,Chen, Wenmin,Liu, Tao,Yu, Mingyan,Fu, Lu,Sun, Yueyue,Liu, Huiqing,De Clercq, Erik,Pannecouque, Christophe,Balzarini, Jan,Zhan, Peng,Liu, Xinyong
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p. 754 - 765
(2015/02/05)
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- Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 2: Discovery of novel [1,2,4]Triazolo[1,5-a]pyrimidines using a structure-guided core-refining approach
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Guided by crystal structures of HIV-1 RT/DAPY complex and molecular modeling studies, a series of novel [1,2,4]triazolo[1,5-a]pyrimidine derivatives were rationally designed via structure-based core refining approach, synthesized through the readily acces
- Wang, Liu,Tian, Ye,Chen, Wenmin,Liu, Hong,Zhan, Peng,Li, Dongyue,Liu, Huiqing,De Clercq, Erik,Pannecouque, Christophe,Liu, Xinyong
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p. 293 - 303
(2014/08/18)
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- The identification of GPR3 inverse agonist AF64394; The first small molecule inhibitor of GPR3 receptor function
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The identification of the novel and selective GPR3 inverse agonist AF64394, the first small molecule inhibitor of GPR3 receptor function, is described. Structure activity relationships and syntheses based around AF64394 are reported.
- Jensen, Thomas,Elster, Lisbeth,Nielsen, Soren Moller,Poda, Suresh Babu,Loechel, Frosty,Volbracht, Christiane,Klewe, Ib Vestergaard,David, Laurent,Watson, Stephen P.
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p. 5195 - 5198
(2014/12/11)
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- Lead optimization of aryl and aralkyl amine-based triazolopyrimidine inhibitors of plasmodium falciparum dihydroorotate dehydrogenase with antimalarial activity in mice
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Malaria is one of the leading causes of severe infectious disease worldwide; yet, our ability to maintain effective therapy to combat the illness is continually challenged by the emergence of drug resistance.We previously reported identification of a new class of triazolopyrimidine-based Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitors with antimalarial activity, leading to the discovery of a new lead series and novel target for drug development. Active compounds from the series contained a triazolopyrimidine ring attached to an aromatic group through a bridging nitrogen atom. Herein, we describe systematic efforts to optimize the aromatic functionality with the goal of improving potency and in vivo properties of compounds from the series. These studies led to the identification of two new substituted aniline moieties (4-SF5-Ph and 3,5-Di-F-4- CF 3-Ph), which, when coupled to the triazolopyrimidine ring, showed good plasma exposure and better efficacy in the Plasmodium berghei mouse model of the disease than previously reported compounds from the series.
- Gujjar, Ramesh,El Mazouni, Farah,White, Karen L.,White, John,Creason, Sharon,Shackleford, David M.,Deng, Xiaoyi,Charman, William N.,Bathurst, Ian,Burrows, Jeremy,Floyd, David M.,Matthews, David,Buckner, Frederick S.,Charman, Susan A.,Phillips, Margaret A.,Rathod, Pradipsinh K.
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experimental part
p. 3935 - 3949
(2011/07/31)
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- Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF1) receptor antagonists
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To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a] pyrimidines, imidazo[1,2-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines were designed, synthesized and evaluated as CRF1 receptor antagonists. Compounds 2-27 showed binding affinity (IC50 = 4.2-418 nM) and antagonist activity (EC50 = 4.0-889 nM). Compound 5 was found to show oral efficacy in an Elevated Plus Maze test in rats. Further chemical modification of them led us to discovery of the tricyclic core antagonists pyrazolo[1,5-a]pyrrolo[3,2-e] pyrimidines. The discovery process of these compounds is presented, as is the study of the structure-activity relationship.
- Saito, Tetsuji,Obitsu, Tetsuo,Minamoto, Chiaki,Sugiura, Tsuneyuki,Matsumura, Naoya,Ueno, Sonoko,Kishi, Akihiro,Katsumata, Seishi,Nakai, Hisao,Toda, Masaaki
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scheme or table
p. 5955 - 5966
(2011/11/04)
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- AROMATIC COMPOUND
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An aromatic compound represented by the following formula or a pharmaceutically acceptable salt thereof: , wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., G1, G2, G3, G4 and G5 are CH or N, X is -NH-, -O-, -CH2-, etc., Y is - CH2-,-CO-,-SO2- etc., Z is a single bond, -CO-, -SO2-, -NH-, -O-, -S-, -CONH-,-SO2NH-, etc., R2 is hydrogen, alkyl, alkoxy, halogen, etc., and R3 is carbocyclic group, heterocyclic group, alkyl, etc., is useful as a controlling agent of the function of CCR4 useful for the treatment or therapy for bronchial asthma, atopic dermatitis, etc.
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Page/Page column 79
(2008/12/07)
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- ALICYCLIC HETEROCYCLIC COMPOUND
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An alicyclic heterocyclic compound represented by the following formula or a pharmaceutically acceptable salt thereof: wherein ring A is a heterocyclic ring, ring B is a carbocyclic ring, a heterocyclic ring etc., P1 and P2 are CH or N, q and r are 0 to 2, X is -NH-, -O-, -CH2-, etc., Y is -CH2-, -CO-, -SO2-, etc., Z is -CO-, -SO2-, etc., and R3 is carbocyclic group, heterocyclic group, hydroxyl, alkoxy or amino, is useful as a controlling agent of the function of CCR4 useful for the prevention or treatment for bronchial asthma, atopic dermatitis, etc.
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Page/Page column 107
(2008/12/08)
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