Delving into the Latest Updates on FR-180102 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target-

Action-

Mechanism-

Therapeutic Areas

Infectious Diseases

Active Indication-

Inactive Indication

Helicobacter pylori infection

Originator Organization

Fujisawa Pharmaceutical Co., Ltd.

Active Organization-

Inactive Organization

Fujisawa Pharmaceutical Co., Ltd.

License Organization-

Drug Highest PhasePendingPreclinical

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC18H14Cl2N2O2

InChIKeyYXVRCTRMIKAODR-UHFFFAOYSA-N

CAS Registry206882-50-0

The synthesis and optimization of the anti-Helicobacter pylori activity of a novel series of benzyloxyisoquinoline derivatives that was discovered by a random screening process, are described. In the in vitro assay, compound 10c containing a 3-acetamido-2,6-dichlorobenzyl substituent was found to have extremely potent activity against H. pylori and no activity against other common bacteria. The anti-H. pylori activity of 10c was superior to that of amoxicillin (AMPC) (1) and clarithromycin (CAM) (2). However, 10c did not show in vivo efficacy in a mouse infection model; a feature attributed to the lack of strong bactericidal activity at short contact times.

01 Jul 1998·Bioorganic & Medicinal Chemistry LettersQ4 · MEDICINE

Discovery of a novel benzyloxyisoquinoline derivative with potent anti-Helicobacter pylori activity

Q4 · MEDICINE

Article

Author: Chizu Morinaga ; Hidenori Azami ; Yoshimi Matsumoto ; David Barrett ; Hisashi Takasugi ; Yoshiki Yoshida

The synthesis and in vitro optimization of the anti-Helicobacter pylori activity of a novel series of benzyloxyisoquinoline derivatives discovered by a random screening process, are described. FR180102 (7f), having a 3-acetamido-2,6-dichlorobenzyl moiety, was found to have extremely potent activity against H. pylori and no effect against a series of common Gram-positive and Gram-negative bacteria.

100 Deals associated with FR-180102

Login to view more data