30129-57-8Relevant academic research and scientific papers
SUBSTITUTED PYRAZOLOPYRIMIDINONE COMPOUNDS AS PDE2 INHIBITORS
-
Page/Page column 63, (2018/07/29)
A chemical entity of Formula (I), wherein V, W, Y, and Z, have any of the values described herein, and compositions comprising such chemical entities, methods of making them; and their use in a wide range of methods, including metabolic and reaction kinetic studies; detection and imaging techniques, radioactive treatments; modulating and treating disorders mediated by PDE2 activity; treating neurological disorders, CNS disorders, dementia, cognitive disorders, neurodegenerative diseases, and trauma-dependent losses of function, enhancing the efficiency of cognitive and motor training, including in stroke or TBI rehabilitation; and treating peripheral disorders, including hematological, cardiovascular, gastroenterological, dermatoiogical, inflammatory, and pain disorders.
Synthesis, physicochemical properties of allopurinol derivatives and their biological activity against Trypanosoma cruzi
Raviolo,Solana,Novoa,Gualdesi,Alba-Soto,Bri?ón
, p. 455 - 464 (2013/10/22)
Chagas disease is caused by Trypanosoma cruzi (T. cruzi) leading to a huge number of infections and deaths per year, because in addition to many sufferers only having limited access to health services only an inefficient chemotherapy is available using drugs such as benznidazole and nifurtimox. Here, C6-alkyl (2a-c) and N1-acyl (3a-c) derivatives of Allopurinol (Allop, compound with activity against T. cruzi) were synthesized in good yields and their structures were unambiguously characterized. Only 2a, 2b and 3c showed inhibitory activity against the proliferative stages of the parasite when tested at 1 μg mL -1 with the 3c derivative exhibiting an IC50 value similar to that of Allop and not being toxic for mammalian cells. Relevant pharmaceutical physicochemical properties (pKa, stability, solubility, lipophilicity) were also determined as well by using Lipinski's rule, polar surface area and molecular rigidity. Taken together, the results demonstrated that the studied derivatives had optimal properties for bioavailability and oral absorption. For the stability studies, Micellar Liquid Chromatography was used as the analytical method which was fully validated according to the FDA guidelines and shown to be a suitable, sensitive and simple method for routine analysis of these Allop derivatives.
Bioisosteric transformations and permutations in the triazolopyrimidine scaffold to identify the minimum pharmacophore required for inhibitory activity against plasmodium falciparum dihydroorotate dehydrogenase
Marwaha, Alka,White, John,El-mazouni, Farah,Creason, Sharon A,Kokkonda, Sreekanth,Buckner, Frederick S.,Charman, Susan A.,Phillips, Margaret A.,Rathod, Pradipsinh K.
, p. 7425 - 7436 (2012/11/07)
Plasmodium falciparum causes approximately 1 million deaths annually. However, increasing resistance imposes a continuous threat to existing drug therapies. We previously reported a number of potent and selective triazolopyrimidine-based inhibitors of P.
A facile one-pot synthesis of 1-arylpyrazolo[3,4-d]pyrimidin- 4-ones
Zhang, Xiaohong,Lin, Qiulian,Zhong, Ping
experimental part, p. 3079 - 3086 (2010/09/04)
One pot synthesis of 1-arylpyrazolo[3,4-d]pyrimidin-4-ones by the reaction of 5-amino-N-substituted-1H-pyrazole-4-carbonitrile with different lower aliphatic acids in the presence of POCl3 has been developed. The structures of all the title compounds have been confirmed by IR, 1H-NMR, 13C-NMR, and elemental analyses. Moreover, the structures of one of these compounds, 2c, was confirmed by single-crystal X-ray diffraction.
KINASE MODULATORS AND METHODS OF USE
-
Page/Page column 100, (2010/02/15)
The present invention relates to compounds of the Formula I and II wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
Synthesis of pyrazolo 3,4-d pyrimidine analogues of the potent agent N-4-2-2-amino-4 3H-oxo-7H-pyrrolo 2,3-d pyrimidin-5-yl ethylbenzoyl-L-glutamic acid (LY231514)
Taylor, Edward C.,Patel, Hemantkumar H.
, p. 8089 - 8100 (2007/10/02)
Several pyrazolo[3,4-d]pyrimidine analogues of the potent antitumor agent N-{4-[2-(2-amino-4(3 H)-oxo-7H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L-glutamic acid (LY231514, 5) have been prepared. A principal synthetic step proved to be a palladium-cata
Versatile synthesis of 6-alkyl/aryl-1H-pyrazolopyrimidin-4-ones
Reddy, K Hemender,Reddy, A Panduranga,Veeranagaiah, V
, p. 163 - 166 (2007/10/02)
Condensation of 5-amino-1H-pyrazole-4-carboxamide (1a) with various aromatic aldehydes furnishes 6-substituted-1H-pyrazolepyrimidin-4(5H)-ones (4a-f) via the intermediates 5-(N-arylideneamino)pyrazole-4-carboxamides (3a-f).Compounds 4a-f have also
