Synthesis, characterization, and biological evaluation of novel diclofenac prodrugs.

21:09 EDT 4th September 2015 | BioPortfolio

Summary of "Synthesis, characterization, and biological evaluation of novel diclofenac prodrugs."

Diclofenac ester pro drugs (4, 5, 6) were synthesized and evaluated in vitro and in vivo for their potential use for oral delivery, with the aim of obtaining enzymatically labile and less ulceration drugs than the parent drug diclofenac sodium (1a). Prodrugs 4, 5, 6 were found to be potent anti-inflammatory drugs with less ulcerogenic potential than the parent diclofenac sodium. Prodrugs 4, 5, 6 rapidly underwent enzymatic hydrolysis to release the parent drug diclofenac in 30-60 min in rat liver microsomes (RLM) and rat plasma (RP). Prodrugs were found to be more lipophilic when the partition coefficient was measured in 1-octanol and buffer system at pH 7.4 and 3.0. Diclofenac prodrugs 4, 5, 6 were found to be crystalline in nature (analyzed by PXRD). Prodrug 4 was found to be a superior candidate for the treatment of chronic inflammatory diseases.

Affiliation

Medicinal Chemistry Research Laboratory, School of Chemical Sciences, Solapur University , Solapur 413 255, India.

Journal Details

This article was published in the following journal.

Name: Journal of medicinal chemistry
ISSN: 1520-4804
Pages: 1202-10

Links

PubMed Articles [19708 Associated PubMed Articles listed on BioPortfolio]

Diastereoselective synthesis of P-chirogenic phosphoramidate prodrugs of nucleoside analogues (ProTides) via copper catalysed reaction.

The first copper-catalysed diastereoselective synthesis of P-chiral phosphoramidate prodrugs (ProTides) is reported. This procedure allows the synthesis of diastereomeric-enriched mixtures of ProTides...

Design, synthesis and biological evaluation of 5-aminolaevulinic acid/3-hydroxypyridinone conjugates as potential photodynamic therapeutical agents.

5-Aminolaevulinic acid (ALA) prodrugs have been widely used in photodynamic therapy (PDT) as precursors to the natural photosensitizer, protoporphyrin IX (PpIX). The main disadvantage of this therapy ...

Dendrimeric anticancer prodrugs for targeted delivery of ursolic acid to folate receptor-expressing cancer cells: synthesis and biological evaluation.

The anticancer efficacy of ursolic acid (UA) was limited by poor water solubility, non-specific tumor distribution, and low bioavailability. To overcome this problem, polyamidoamine (PAMAM) conjugated...

Photoactivatable prodrugs of anti-melanoma agent vemurafenib.

In this study we report on novel photoactivatable caged prodrugs of vemurafenib. This kinase inhibitor was the first approved drug for the personalized treatment of BRAF-mutated melanoma and showed im...

Design, synthesis and biological evaluation of small molecules as potent glucosidase inhibitors.

Herein we have reported design, synthesis and in vitro biological evaluation of a library of bicyclic lactams that led to the discovery of compounds 6 and 7 as a novel class of α-glucosidase inhibit...

Clinical Trials [1943 Associated Clinical Trials listed on BioPortfolio]

Evaluation of the Efficacy and Safety of Diclofenac HPBCD 25, 50 mg/ml in the Treatment of Post-surgical Pain Following Dental Surgery

The present study is proposed to evaluate the efficacy and safety of single doses of Diclofenac HPBCD subcutaneous (s.c.) (25 mg/1 ml and 50 mg/1 ml) in the treatment of acute moderate-to-...

Study to Compare the Pharmacokinetics of IV Diclofenac Sodium (2 Doses)Versus Oral Diclofenac Potassium

The purpose of this study is to assess the pharmacokinetic parameters of intravenous diclofenac sodium (DIC075V) 18.75 mg and 37.5 mg following single- and multiple-dose administration, as...

Use of Etoricoxib Compared to Diclofenac in the Perioperative Treatment of Patients After Total Hip Arthroplasty

The primary aim of this study is to test if etoricoxib decreases the perioperative blood loss compared to diclofenac. Secondary questions to be explored are: - Does etoricoxib p...

Non Steroidal Anti Inflammatory Treatment for Post Operative Pericardial Effusion

The aim of the sudy is to evaluate, through clinical, biological and transthoracic echocardiography follow up, the evolution of post operative (cardiac surgery) pericardial effusion and m...

Adjuvant Treatment of Graves´ Ophthalmopathy With NSAID (aGO Study)

AGO study - adjuvant treatment, with NSAID, of endocrine ophthalmopathy in Graves´ disease Background - Already at diagnosis of Graves disease approximately 98% of the patients have ...

Medical and Biotech [MESH] Definitions

A field of biological research combining engineering in the formulation, design, and building (synthesis) of novel biological structures, functions, and systems.

A non-steroidal anti-inflammatory agent (NSAID) with antipyretic and analgesic actions. It is primarily available as the sodium salt.

Studies determining the effectiveness or value of processes, personnel, and equipment, or the material on conducting such studies. For drugs and devices, CLINICAL TRIALS AS TOPIC; DRUG EVALUATION; and DRUG EVALUATION, PRECLINICAL are available.

Preclinical testing of drugs in experimental animals or in vitro for their biological and toxic effects and potential clinical applications.

Studies designed to assess the efficacy of programs. They may include the evaluation of cost-effectiveness, the extent to which objectives are met, or impact.


Advertisement
 

Relevant Topics

Biological Therapy
Latest News Clinical Trials Research Drugs Reports Corporate
Biological therapy involves the use of living organisms, substances derived from living organisms, or laboratory-produced versions of such substances to treat disease. Some biological therapies for cancer use vaccines or bacteria to stimulate the body&rs...

Pharmacy
Latest News Clinical Trials Research Drugs Reports Corporate
Pharmacy is the science and technique of preparing as well as dispensing drugs and medicines. It is a health profession that links health sciences with chemical sciences and aims to ensure the safe and effective use of pharmaceutical drugs. The scope of...

Advertisement