5-(2,4-Difluorophenyl)salicylic acid, diflunisal (25), is the best compound, in terms of both efficacy and safety, from over 500 salicylates investigated in our laboratories. It is a chemically distinct, nonacetylating salicylic acid, more active than aspirin as an analgesic and antiinflammatory agent and superior in duration of action and therapeutic index. Some recent clinical and biochemical observations are briefly discussed.
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http://dx.doi.org/10.1021/jm00209a001 | DOI Listing |
Bioorg Chem
October 2021
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, PO Box 2457, Riyadh 11451, Saudi Arabia. Electronic address:
Nitrogen heterocyclic rings have participated to constitute most of the drugs and several pharmacologically related compounds. The existence of such hetero atoms/groups in heterocyclic systems privileged specificities in their biological objectives. Particularly, quinazoline and triazole are biologically imperative platforms known to be linked with various pharmacological activities.
View Article and Find Full Text PDFIndian J Pharm Sci
July 2009
Department of Pharmaceutical Chemistry, C. L. Baid Mehta College of Pharmacy, Jyothi Nagar, Old Mahabaliupuram Road, Thoraipakkam, Chennai-600 096, India.
In the present study, a novel series of 4-(2-aminophenyl)morpholines were synthesized and characterized by IR, (1)H-NMR, (13)C NMR and mass spectral analysis. The synthesized compounds were screened for analgesic (100 and 200 mg/kg), antiinflammatory (200 and 400 mg/kg), antibacterial (Bacillus subtilis, Bacillus cereus, Staphylococcus epidermidis, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa and Escherichia coli) and antifungal (Candida albicans and Aspergillus niger) activities. The minimum inhibitory concentrations of the compounds were also ascertained by agar streak dilution method.
View Article and Find Full Text PDFCurr Pharm Des
May 2009
New Drug Discovery, R & D Center, Matrix Laboratories Limited, Anrich Industrial Estate, Bollaram, Jinnaram Mandal, Medak District, Andhra Pradesh, India.
Neuropathic pain affects 26 million patients worldwide resulting in a worldwide healthcare cost over $ 3 billion per year. Despite the availability of an impressive arsenal of powerful drugs for the effective management of pain, there remains a great medical need for new medicines to treat pain. While little is known about the proteins that detect noxious stimuli (especially those of a physical nature), vanilloid receptor, an excitatory ion channel expressed by nociceptors, has been identified as molecular target for the development of recent therapies to treat pain.
View Article and Find Full Text PDFCurr Opin Anaesthesiol
August 2008
Department of Anesthesiology, LSU School of Medicine, New Orleans, Louisiana 70112, USA.
Purpose Of Review: NSAIDs have served as analgesic, antiinflammatory, and antipyretic medicines for over a century. A novel class of NSAIDs, cyclooxygenase-2 inhibitors, was introduced in 1999. All NSAIDs and aspirin inhibit active sites of cyclooxygenase-1 and cyclooxygenase-2.
View Article and Find Full Text PDFJ Comput Chem
November 2008
Physico-Chemical Molecular Research Unit, Department of Organic Chemistry, Faculty of Pharmacy, University of Porto, 4150-047 Porto, Portugal.
Up to now, very few reports have been published concerning the application of multiobjective optimization (MOOP) techniques to quantitative structure-activity relationship (QSAR) studies. However, none reports the optimization of objectives related directly to the desired pharmaceutical profile of the drug. In this work, for the first time, it is proposed a MOOP method based on Derringer's desirability function that allows conducting global QSAR studies considering simultaneously the pharmacological, pharmacokinetic and toxicological profile of a set of molecule candidates.
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