Literature DB >> 12901923

Synthesis and structure-activity relationship of 2-amino-3-heteroaryl-quinoxalines as non-peptide, small-molecule antagonists for interleukin-8 receptor.

Jie Jack Li1, Kenneth G Carson, Bharat K Trivedi, Wen Song Yue, Qing Ye, Roberta A Glynn, Steven R Miller, David T Connor, Bruce D Roth, Jay R Luly, Joseph E Low, David J Heilig, Weixing Yang, Shixin Qin, Stephen Hunt.   

Abstract

Interleukin-8 modulation is implicated in many inflammatory and cancer diseases. Starting from a mass-screening hit, the synthesis and structure-activity relationship of 2-amino-3-heteroarylquinoxalines as non-peptide, small molecule interleukine-8 receptor antagonists have been developed. The optimized derivatives, PD 0210293 (13y) and PD 0220245 (13r), show inhibition of both IL-8 receptor binding and IL-8-mediated neutrophil chemotaxis.

Entities:  

Mesh:

Substances:

Year:  2003        PMID: 12901923     DOI: 10.1016/s0968-0896(03)00399-7

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  3 in total

Review 1.  Therapy for chronic obstructive pulmonary disease in the 21st century.

Authors:  Louise E Donnelly; Duncan F Rogers
Journal:  Drugs       Date:  2003       Impact factor: 9.546

2.  Boronic acid-containing aminopyridine- and aminopyrimidinecarboxamide CXCR1/2 antagonists: Optimization of aqueous solubility and oral bioavailability.

Authors:  Aaron D Schuler; Courtney A Engles; Dean Y Maeda; Mark T Quinn; Liliya N Kirpotina; Winston N Wicomb; S Nicholas Mason; Richard L Auten; John A Zebala
Journal:  Bioorg Med Chem Lett       Date:  2015-07-30       Impact factor: 2.823

3.  Furan- and Thiophene-2-Carbonyl Amino Acid Derivatives Activate Hypoxia-Inducible Factor via Inhibition of Factor Inhibiting Hypoxia-Inducible Factor-1.

Authors:  Shin-Ichi Kawaguchi; Yuhei Gonda; Takuya Yamamoto; Yuki Sato; Hiroyuki Shinohara; Yohsuke Kobiki; Atsuhiko Ichimura; Takashi Dan; Motohiro Sonoda; Toshio Miyata; Akiya Ogawa; Tadayuki Tsujita
Journal:  Molecules       Date:  2018-04-11       Impact factor: 4.411

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.