Delving into the Latest Updates on Esaprazole hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Esaprazole, Hexaprazol

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Target-

Action-

Mechanism-

Therapeutic Areas

Digestive System Disorders

Active Indication

Peptic Ulcer

Inactive Indication-

Originator Organization

Camillo Corvi

Active Organization

Camillo Corvi

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date

Italy (12 Jun 1995),

Peptic Ulcer

Regulation-

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Structure/Sequence

Molecular FormulaC12H23N3O

InChIKeyRTFADALJKSFJDZ-UHFFFAOYSA-N

CAS Registry64204-55-3

View All Structures (2)

The main purpose of In two kinds of fasting and postprandial Chinese healthy subjects with Boehringer represent Ingelheim company production of hydrochloric acid Pramipexole zyban (specification: 0.26 mg/piece, in Pramipexole, commodity name: Siforl ®) as the reference preparation, study a single oral dose of macro crown biological pharmaceutical co., LTD. Production of Pramipexole Dihydrochloride Sustained Release Tablets (specification:The pharmacokinetic parameters of the drug were calculated after the time course of the drug in vivo (0.375mg/ tablet, as measured by pramipexole hydrochloride), and the human relative bioavailability of the two preparations were compared to evaluate their bioequivalence.
A secondary purpose To evaluate the safety of fasting and postprandial oral test preparations and reference preparations.

Start Date24 Jul 2020

Sponsor / Collaborator

The First Affiliated Hospital, Zhejiang University Sch of Med

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100 Clinical Results associated with Esaprazole hydrochloride

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100 Translational Medicine associated with Esaprazole hydrochloride

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100 Patents (Medical) associated with Esaprazole hydrochloride

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24

Literatures (Medical) associated with Esaprazole hydrochloride

01 Jul 2023·The Journal of general virology

Inhibition of phosphodiesterase 12 results in antiviral activity against several RNA viruses including SARS-CoV-2.

Article

Author: Thomas, Howard ; Wand, Matthew ; Beasley, David W C ; Carroll, Miles W ; Dejnirattisai, Wanwissa ; Tree, Julia A ; Mongkolsapaya, Juthathip ; Karayiannis, Peter ; Sadiq, Fouzia ; Thursz, Mark ; Screaton, Gavin ; Matthews, Ian ; Elmore, Michael J

The 2',5'- oligoadenylate synthetase (OAS) - ribonuclease L (RNAseL) - phosphodiesterase 12 (PDE12) pathway is an essential interferon-induced effector mechanism against RNA virus infection. Inhibition of PDE12 leads to selective amplification of RNAseL activity in infected cells. We aimed to investigate PDE12 as a potential pan-RNA virus antiviral drug target and develop PDE12 inhibitors that elicit antiviral activity against a range of viruses. A library of 18 000 small molecules was screened for PDE12 inhibitor activity using a fluorescent probe specific for PDE12. The lead compounds (CO-17 or CO-63) were tested in cell-based antiviral assays using encephalomyocarditis virus (EMCV), hepatitis C virus (HCV), dengue virus (DENV), West Nile virus (WNV) and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), in vitro. Cross reactivity of PDE12 inhibitors with other PDEs and in vivo toxicity were measured. In EMCV assays, CO-17 potentiated the effect of IFNα by 3 log₁₀. The compounds were selective for PDE12 when tested against a panel of other PDEs and non-toxic at up to 42 mg kg^-1 in rats in vivo. Thus, we have identified PDE12 inhibitors (CO-17 and CO-63), and established the principle that inhibitors of PDE12 have antiviral properties. Early studies suggest these PDE12 inhibitors are well tolerated at the therapeutic range, and reduce viral load in studies of DENV, HCV, WNV and SARS-CoV-2 in human cells and WNV in a mouse model.

23 Jun 2016·Journal of Medicinal Chemistry

Monothiocarbamates Strongly Inhibit Carbonic Anhydrases in Vitro and Possess Intraocular Pressure Lowering Activity in an Animal Model of Glaucoma

Article

Author: Supuran, Claudiu T. ; Cosconati, Sandro ; Carta, Fabrizio ; Di Leva, Francesco Saverio ; Masini, Emanuela ; Novellino, Ettore ; Vullo, Daniela ; Durante, Mariaconcetta ; Scozzafava, Andrea

A series of monothiocarbamates (MTCs) were prepared from primary/secondary amines and COS as potential carbonic anhydrase (CA, EC 4.2.1.1) inhibitors, using the dithiocarbamates, the xanthates, and the trithiocarbonates as lead compounds. The MTCs effectively inhibited the pharmacologically relevant human (h) hCAs isoforms I, II, IX, and XII in vitro and showed KIs spanning between the low and medium nanomolar range. By means of a computational study, the MTC moiety binding mode on the CAs was explained. Furthermore, a selection of MTCs were evaluated in a normotensive glaucoma rabbit model for their intraocular pressure (IOP) lowering effects and showed interesting activity.

02 Jan 2016·Journal of Enzyme Inhibition and Medicinal ChemistryQ2 · MEDICINE

Dithiocarbamates with potent inhibitory activity against theSaccharomyces cerevisiaeβ-carbonic anhydrase

Q2 · MEDICINE

ArticleOA

Author: Isik, Semra ; Scozzafava, Andrea ; Supuran, Claudiu T ; Carta, Fabrizio ; Vullo, Daniela ; AlOthman, Zeid ; Osman, Sameh M ; Bozdag, Murat

Dithiocarbamates (DTCs) prepared from primary or secondary amines, which incorporated amino/hydroxyl-alkyl, mono-/bicyclic aliphatic/heterocyclic rings based on the quinuclidine, piperidine, hydroxy-/carboxy-/amino-substituted piperidine, morpholine and piperazine scaffolds, were investigated for the inhibition of α- and β-carbonic anhydrases (CAs, EC 4.2.1.1) of pharmacologic relevance, such as the human (h) isoform hCA I and II, as well as the Saccharomyces cerevisiae β-CA, scCA. The yeast and its β-CA were shown earlier to be useful models of pathogenic fungal infections. The DTCs investigated here were medium potency hCA I inhibitors (K(I)s of 66.5-910 nM), were more effective as hCA II inhibitors (K(I)s of 8.9-107 nM) and some of them showed excellent, low nanomolar activity against the yeast enzyme, with inhibition constants ranging between 6.4 and 259 nM. The detailed structure activity relationship for inhibition of the yeast and human enzymes is discussed. Several of the investigated DTCs showed excellent selectivity ratios for inhibiting the yeast over the human cytosolic CA isoforms.

100 Deals associated with Esaprazole hydrochloride

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