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Title: Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors

Abstract

IRAK4 has been identified as potential therapeutic target for inflammatory and autoimmune diseases. Herein we report the identification and initial SAR studies of a new class of pyrazole containing IRAK4 inhibitors designed to expand chemical diversity and improve off target activity of a previously identified series. These compounds maintain potent IRAK4 activity and desirable ligand efficiency. Rat clearance and a variety of off target activities were also examined, resulting in encouraging data with tractable SAR.

Authors:
; ; ; ; ; ; ; ; ; ; ; ; ; ; ORCiD logo
Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
INDUSTRY
OSTI Identifier:
1404961
Resource Type:
Journal Article
Resource Relation:
Journal Name: Bioorganic and Medicinal Chemistry Letters; Journal Volume: 26; Journal Issue: 17
Country of Publication:
United States
Language:
ENGLISH
Subject:
37 INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY; 60 APPLIED LIFE SCIENCES

Citation Formats

Hanisak, Jennifer, Seganish, W. Michael, McElroy, William T., Tang, Haiquin, Zhang, Rui, Tsui, Hon-Chung, Fischmann, Theirry, Tulshian, Deen, Tata, James, Sondey, Christopher, Devito, Kristine, Fossetta, James, Garlisi, Charles G., Lundell, Daniel, and Niu, Xiaoda. Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors. United States: N. p., 2016. Web. doi:10.1016/j.bmcl.2016.07.048.
Hanisak, Jennifer, Seganish, W. Michael, McElroy, William T., Tang, Haiquin, Zhang, Rui, Tsui, Hon-Chung, Fischmann, Theirry, Tulshian, Deen, Tata, James, Sondey, Christopher, Devito, Kristine, Fossetta, James, Garlisi, Charles G., Lundell, Daniel, & Niu, Xiaoda. Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors. United States. doi:10.1016/j.bmcl.2016.07.048.
Hanisak, Jennifer, Seganish, W. Michael, McElroy, William T., Tang, Haiquin, Zhang, Rui, Tsui, Hon-Chung, Fischmann, Theirry, Tulshian, Deen, Tata, James, Sondey, Christopher, Devito, Kristine, Fossetta, James, Garlisi, Charles G., Lundell, Daniel, and Niu, Xiaoda. Thu . "Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors". United States. doi:10.1016/j.bmcl.2016.07.048.
@article{osti_1404961,
title = {Efforts towards the optimization of a bi-aryl class of potent IRAK4 inhibitors},
author = {Hanisak, Jennifer and Seganish, W. Michael and McElroy, William T. and Tang, Haiquin and Zhang, Rui and Tsui, Hon-Chung and Fischmann, Theirry and Tulshian, Deen and Tata, James and Sondey, Christopher and Devito, Kristine and Fossetta, James and Garlisi, Charles G. and Lundell, Daniel and Niu, Xiaoda},
abstractNote = {IRAK4 has been identified as potential therapeutic target for inflammatory and autoimmune diseases. Herein we report the identification and initial SAR studies of a new class of pyrazole containing IRAK4 inhibitors designed to expand chemical diversity and improve off target activity of a previously identified series. These compounds maintain potent IRAK4 activity and desirable ligand efficiency. Rat clearance and a variety of off target activities were also examined, resulting in encouraging data with tractable SAR.},
doi = {10.1016/j.bmcl.2016.07.048},
journal = {Bioorganic and Medicinal Chemistry Letters},
number = 17,
volume = 26,
place = {United States},
year = {Thu Sep 01 00:00:00 EDT 2016},
month = {Thu Sep 01 00:00:00 EDT 2016}
}