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Evolution of nonsteroidal anti-inflammatory drugs (NSAIDs): cyclooxygenase (COX) inhibition and beyond.
  • P. Rao, E. Knaus
  • Medicine
  • Journal of pharmacy & pharmaceutical sciences : a…
  • 20 September 2008
This review traces the origins of NSAIDs, their mechanism of action at the molecular level such as cyclooxygenase (COX) inhibition, development of selective COX-2 inhibitors, their adverse cardiovascular effects, and some recent developments targeted to the design of effective anti-inflammatory agents with reduced side effects. Expand
Design and synthesis of celecoxib and rofecoxib analogues as selective cyclooxygenase-2 (COX-2) inhibitors: replacement of sulfonamide and methylsulfonyl pharmacophores by an azido bioisostere.
Celecoxib and rofecoxib analogues, in which the respective SO2NH2 and SO2Me hydrogen-bonding pharmacophores were replaced by a dipolar azido bioisosteric substituent, exhibited good oral antiinflammatory and analgesic activities. Expand
Design and synthesis of 4,5-diphenyl-4-isoxazolines: novel inhibitors of cyclooxygenase-2 with analgesic and antiinflammatory activity.
2,3-dimethyl-5-(4-methylsulfonylphenyl)-4-phenyl-4-isoxazoline (13j) exhibited excellent analgesic and AI activities, and it was a potent and selective COX-2 inhibitor, and a molecular modeling (docking study) for 13j showed that the S atom of the MeSO2 substituent is positioned about 6.46 A inside the entrance to the COx-2 secondary pocket. Expand
Synthesis and Antifungal Activities of Myristic Acid Analogs
Myristic acid analogs that are putative inhibitors of N‐myristoyl‐transferase were tested in vitro for activity against yeasts and filamentous fungi and exhibited potent activity against C. albicans, Cryptococcus neoformans and Aspergillus niger. Expand
A mild and efficient methodology for the synthesis of 5-halogeno uracil nucleosides that occurs via a 5-halogeno-6-azido-5,6-dihydro intermediate
A mild and efficient methodology for the synthesis of 5-halogeno (iodo, bromo, or chloro) uracil nucleosides has been developed. 5-Halo-2′-deoxyuridines 4a–c (84–95%), 5-halouridines 7a–c (45–95%),Expand
Bioavailability and pharmacokinetic parameters for 5-ethyl-2'-deoxyuridine.
Although the biotransformation of EDU was similar in mice and rats, cleavage of the EDU glycoside bond was less extensive in mice than in rats, which indicates that EDU undergoes degradation by phosphorylases present in the gastrointestinal tract and/or by presystemic metabolism. Expand
Electrophysiological characterization of a recombinant human Na+‐coupled nucleoside transporter (hCNT1) produced in Xenopus oocytes
Human concentrative nucleoside transporter 1 (hCNT1) mediates active transport of nucleosides and anticancer and antiviral nucleoside drugs across cell membranes by coupling influx to the movement ofExpand
Synthesis and biological evaluation of 1,3-diphenylprop-2-en-1-ones possessing a methanesulfonamido or an azido pharmacophore as cyclooxygenase-1/-2 inhibitors.
The structure-activity data acquired indicate that the propenone moiety constitutes a suitable scaffold to design new acyclic 1,3-diphenylprop-2-en-1-ones with selective COX-1 orCOX-2 inhibitory activity. Expand
Radiopharmaceuticals to monitor gene transfer.
An overview of gene transfer therapy and imaging based on radiolabelled nucleoside substrates for herpes simplex type-1 thymidine kinase, with emphasis on IVFRU, a stable, potent and selective HSV-1 TK substrate developed in the laboratories. Expand
Cytotoxicity and cellular uptake of pyrimidine nucleosides for imaging herpes simplex type-1 thymidine kinase (HSV-1 TK) expression in mammalian cells.
These nucleosides are unpredictably cytotoxic to the various cell lines studied, and this unpredictability extends across the HSV-1 TK expression characteristic; their uptake by cells engineered to express HSV the virus is also dependent on the molecular construction of the gene cassette carrying the viral TK gene. Expand