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Literature DB >> 16249085

Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.

Laszlo Revesz¹, Ernst Blum, Franco E Di Padova, Thomas Buhl, Roland Feifel, Hermann Gram, Peter Hiestand, Ute Manning, Ulf Neumann, Gerard Rucklin.

Abstract

A test library with three novel p38alpha inhibitory scaffolds and a narrow set of substituents was prepared. Appropriate combination of substituent and scaffold generated potent p38alpha inhibitors, for example, pyrazolo[3,4-b]pyridine 9, pyrazolo[3,4-d]pyrimidine 18a and pyrazolo[3,4-b]pyrazine 23b with potent in vivo activity upon oral administration in animal models of rheumatoid arthritis.

Entities: Chemical Disease Gene

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Year: 2005 PMID： 16249085 DOI： 10.1016/j.bmcl.2005.10.015

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

6 in total

1. Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.

Authors: Jing Liu; Chao Yang; Catherine Simpson; Deborah Deryckere; Amy Van Deusen; Michael J Miley; Dmitri Kireev; Jacqueline Norris-Drouin; Susan Sather; Debra Hunter; Victoria K Korboukh; Hari S Patel; William P Janzen; Mischa Machius; Gary L Johnson; H Shelton Earp; Douglas K Graham; Stephen V Frye; Xiaodong Wang
Journal: ACS Med Chem Lett Date: 2012-02-09 Impact factor: 4.345

2. Solution-phase synthesis of a diverse library of benzisoxazoles utilizing the [3 + 2] cycloaddition of in situ-generated nitrile oxides and arynes.

Authors: Anton V Dubrovskiy; Prashi Jain; Feng Shi; Gerald H Lushington; Conrad Santini; Patrick Porubsky; Richard C Larock
Journal: ACS Comb Sci Date: 2013-03-08 Impact factor: 3.784

Pyrazoloheteroaryls: novel p38alpha MAP kinase inhibiting scaffolds with oral activity.

1. Discovery of Novel Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia.

2. Solution-phase synthesis of a diverse library of benzisoxazoles utilizing the [3 + 2] cycloaddition of in situ-generated nitrile oxides and arynes.

3. N-N bond-forming cyclization for the one-pot synthesis of N-aryl[3,4-d]pyrazolopyrimidines.

4. 5-(4-Chloro-phen-yl)-1-methyl-3-phenyl-3,6,8,9-tetra-hydro-pyrazolo-[3,4-b]thio-pyrano[4,3-d]pyridine.

5. Four-component bicyclization approaches to skeletally diverse pyrazolo[3,4-b]pyridine derivatives.

Review 6. 1H-Pyrazolo[3,4-b]pyridines: Synthesis and Biomedical Applications.