Delving into the Latest Updates on Compound 12e(Shandong University) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms-

Target

Influenza A neuraminidase

Action

inhibitors

Mechanism

neuraminidase inhibitors(Influenza A Neuraminidase inhibitors)

Therapeutic Areas

Infectious DiseasesRespiratory Diseases

Active Indication

Influenza, Human

Inactive Indication-

Originator Organization

Shandong University

Active Organization

Shandong University

Inactive Organization-

License Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

With our continuous endeavors in seeking neuraminidase (NA) inhibitors, we reported herein three series of novel oseltamivir amino derivatives with the goal of exploring the druggable chemical space inside the 150-cavity of influenza virus NAs. Among them, around half of the compounds in series C were demonstrated to be better inhibitors against both wild-type and oseltamivir-resistant group-1 NAs than oseltamivir carboxylate (OSC). Notably, compounds 12d, 12e, 15e, and 15i showed more potent or equipotent antiviral activity against H1N1, H5N1, and H5N8 viruses compared to OSC in cellular assays. Furthermore, compounds 12e and 15e exhibited high metabolic stability in human liver microsomes (HLMs) and low inhibitory effect on main cytochrome P450 (CYP) enzymes, as well as low acute/subacute toxicity and certain antiviral efficacy in vivo. Also, pharmacokinetic (PK) and molecular docking studies were performed. Overall, 12e and 15e possess great potential to serve as anti-influenza candidates and are worthy of further investigation.

100 Deals associated with Compound 12e(Shandong University)

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