𝔖 Bobbio Scriptorium
✦   LIBER   ✦

Synthesis and pharmacological evaluation of 1,1,3-substituted urea derivatives as potent TNF-α production inhibitors

✍ Scribed by Hiroshi Enomoto; Ayako Sawa; Hiroshi Suhara; Noriyoshi Yamamoto; Hiroyuki Inoue; Chikako Setoguchi; Fumio Tsuji; Masahiro Okamoto; Yoshimasa Sasabuchi; Masato Horiuchi; Masakazu Ban

Publisher
Elsevier Science
Year
2010
Tongue
English
Weight
335 KB
Volume
20
Category
Article
ISSN
0960-894X

No coin nor oath required. For personal study only.

✦ Synopsis

A three substituted urea derivative, SA13353 (compound 1a), exhibited potent inhibitory activity against lipopolysaccharide (LPS)-induced TNF-alpha production. We focused on the 1,1-substituted moiety (R(1) and R(2)) of SA13353 and investigated substituent effects of this moiety on LPS-induced TNF-alpha production by oral administration in rats. The synthesis of the urea derivatives was performed rapidly in a one-pot manner using a manual synthesizer. Several compounds containing hydrophobic substituents at this moiety showed more potent inhibitory activities than SA13353.

📜 SIMILAR VOLUMES

ChemInform Abstract: Synthesis and Evalu
ChemInform Abstract: Synthesis and Evaluation of Substituted Benzoisoquinolinones as Potent Inhibitors of Chk1 Kinase.
✍ Robert M. Garbaccio; et al. et al. 📂 Article 📅 2008 🏛 John Wiley and Sons ⚖ 21 KB 👁 1 views

## Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable v

Synthesis and Cytotoxic Evaluation of Su
Synthesis and Cytotoxic Evaluation of Substituted Urea Derivatives as Inhibitors of Human-Leukemia K562 Cells
✍ Ping Cao; Xian-Feng Huang; Hui Ding; Hui-Ming Ge; Huan-Qiu Li; Ban-Feng Ruan; Ha 📂 Article 📅 2007 🏛 John Wiley and Sons 🌐 English ⚖ 73 KB 👁 2 views

## Abstract A series of substituted urea derivatives, compounds **1**–**14**, were synthesized and evaluated for their cytotoxic activities against the human‐leukemia K562 cell line. Two structurally simple compounds, **7** and **12**, both incorporating a morpholine ring, were found to be highly a

Design, synthesis and biological evaluat
Design, synthesis and biological evaluation of new thalidomide analogues as TNF-α and IL-6 production inhibitors
✍ Charlotte Chaulet; Cécile Croix; David Alagille; Sylvain Normand; Adriana Delwai 📂 Article 📅 2011 🏛 Elsevier Science 🌐 English ⚖ 620 KB

Several thalidomide analogues were synthesized and compared to thalidomide and its more active analogue, lenalidomide, for their ability to inhibit the production of the pro-inflammatory cytokine tumour necrosis factor (TNF)-α and interleukin (IL)-6 by LPS-activated peripheral blood mononuclear cell