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Details

Stereochemistry ACHIRAL
Molecular Formula C35H32N6O4
Molecular Weight 600.6664
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 2
Charge 0

SHOW SMILES / InChI
Structure of DERSALAZINE

SMILES

CC1=NC2=CN=CC=C2N1CC3CCN(CC3)C(=O)\C=C(\C4=CC=CC=C4)C5=CC=C(C=C5)\N=N\C6=CC(C(O)=O)=C(O)C=C6

InChI

InChIKey=AYEAMZDTWLXZIJ-RKOUKRECSA-N
InChI=1S/C35H32N6O4/c1-23-37-31-21-36-16-13-32(31)41(23)22-24-14-17-40(18-15-24)34(43)20-29(25-5-3-2-4-6-25)26-7-9-27(10-8-26)38-39-28-11-12-33(42)30(19-28)35(44)45/h2-13,16,19-21,24,42H,14-15,17-18,22H2,1H3,(H,44,45)/b29-20-,39-38+

HIDE SMILES / InChI

Description

Dersalazine is a locally-acting compound. It is a potent platelet activating factor (PAF)-antagonist. Dersalazine inhibited IL-1beta or TNF-alpha production in THP-1 or U937 cells, respectively. Dersalazine sodium reduced colonic proinflammatory cytokines IL-1b, IL-6, and IL-17 in dextran sodium sulphate (DSS)–induced colitis. After oral administration, dersalazine sodium is mostly unabsorbed until it reaches the large bowel where the azo bond is reduced by bacteria releasing the active compound. Dersalazine had been in phase I clinical trial for the treatment of ulcerative colitis. No serious adverse reactions were detected in clinical trial. However, no recent development has been reported.

Approval Year

Sample Use Guides

In Vivo Use Guide
1200 mg/12 h for 4 weeks
Route of Administration: Oral