110299-41-7Relevant academic research and scientific papers
Identification, design and synthesis of novel pyrazolopyridine influenza virus nonstructural protein 1 antagonists
Patnaik, Samarjit,Basu, Dipanwita,Southall, Noel,Dehdashti, Seameen,Wan, Kanny K.,Zheng, Wei,Ferrer, Marc,Taylor, Mercedes,Engel, Daniel A.,Marugan, Juan Jose
supporting information, p. 1113 - 1119 (2019/03/08)
Nonstructural protein 1 (NS1) plays a crucial function in the replication, spread, and pathogenesis of influenza virus by inhibiting the host innate immune response. Here we report the discovery and optimization of novel pyrazolopyridine NS1 antagonists that can potently inhibit influenza A/PR/8/34 replication in MDCK cells, rescue MDCK cells from cytopathic effects of seasonal influenza A strains, reverse NS1-dependent inhibition of IFN-β gene expression, and suppress the slow growth phenotype in NS1-expressing yeast. These pyrazolopyridines will enable researchers to investigate NS1 function during infection and how antagonists can be utilized in the next generation of treatments for influenza infection.
Synthesis of Fused Pyrimidinone and Quinolone Derivatives in an Automated High-Temperature and High-Pressure Flow Reactor
Tsoung, Jennifer,Bogdan, Andrew R.,Kantor, Stanislaw,Wang, Ying,Charaschanya, Manwika,Djuric, Stevan W.
, p. 1073 - 1084 (2018/06/18)
Fused pyrimidinone and quinolone derivatives that are of potential interest to pharmaceutical research were synthesized within minutes in up to 96% yield in an automated Phoenix high-temperature and high-pressure continuous flow reactor. Heterocyclic scaffolds that are either hard to synthesize or require multisteps are readily accessible using a common set of reaction conditions. The use of low-boiling solvents along with the high conversions of these reactions allowed for facile workup and isolation. The methods reported herein are highly amenable for fast and efficient heterocycle synthesis as well as compound scale-ups.
PYRAZOLOPYRIMIDINES AS INHIBITORS OF GLUCOCORTICOID RECEPTOR TRANSLOCATION
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Paragraph 00291, (2016/08/23)
Provided herein are compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of Glucocorticoid Receptor (GR) translocation. Furthermore, the subject compounds and compositions are useful for the treatment of diseases involved in the hypothalamic-pituitary-adrenal (HPA) axis.
Synthesis and characterization of new 1H-pyrazolo[3,4-b]pyridine phosphoramidate derivatives
Pedrosa, Leandro F.,De Macedo, William P.,Furtado, Antonia C.R.,Guedes, Guilherme P.,Borges, Julio C.,Resende, Jackson A.L.C.,Vaz, Maria G.F.,Bernardino, Alice M.R.,De Souza, Marcos C.
, p. 38 - 50 (2014/04/17)
Twelve new 1H-pyrazolo[3,4-b]pyridine phosphoramidate derivatives were synthesized under mild conditions by nucleophilic aromatic substitution reaction of aminoalkylphosphoramidates over 4-Cl substituted pyrazolo[3,4-b]pyridine in good yields. The new com
Discovery of new orally active phosphodiesterase (PDE4) inhibitors
Ochiai, Hiroshi,Ishida, Akiharu,Ohtani, Tazumi,Kusumi, Kensuke,Kishikawa, Katuya,Yamamoto, Susumu,Takeda, Hiroshi,Obata, Takaaki,Nakai, Hisao,Toda, Masaaki
, p. 1098 - 1104 (2007/10/03)
A series of 4-anilinopyrazolopyridine derivatives were synthesized and biologically evaluated as inhibitors of phosphodiesterase (PDE4). Chemical modification of 3, a structurally new chemical lead that was found in our in-house library, was focused on 1- and 3-substituents. Full details of the discovery of a new orally active chemical lead 5 are presented. Structure-activity relationship data, pharmacological evaluation, and the subtype selectivity study are also presented.
Preparation and use of acetylenic ortho-sulfonamido and phosphinic acid amido bicyclic heteroaryl hydroxamic acids as TACE inhibitors
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Page/Page column 23, (2010/01/31)
Compounds of the formula which are useful in disease conditions mediated by TNF-α, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
New tetracyclic heteroaromatic ring system 3H-benzo[b]pyrazolo[3, 4-h]-1, 6-naphthyridines
De Azevedo, Alexandre Reis,Frugulhetti, Izabel C.P.P.,Khan, Misbahul Ain,Khakwani, Samia,Bernardino, Alice M. Rolim
, p. 47 - 54 (2007/10/03)
Various derivatives of the tetracyclic ring system 3H-Benzo[b]pyrazolo[3,4-h]-1,6-naphthyridine were prepared from 4-anilino-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acids by intramolecular cyclization employing phophoryl chloride. 1H NMR spectra of the various derivatives were recorder.
Synthesis and analgesic properties of 5-acyl-arylhydrazone 1-H pyrazolo pyridine derivatives
Dias, Luiza Rosaria S.,Alvim, Maria Jose F.,Freitas, Antonio Carlos C.,Barreiro, Eliezer J.,Miranda, Ana Luisa P.
, p. 163 - 169 (2007/10/02)
A series of 5-acyl-arylhydrazone 1-H pyrazolo pyridine derivatives (1), planned by applying classical ring isosterism, were synthesized in order to evaluate the structure-activity relationship (SAR), especially the participation of the structural
