Rofecoxib Analogues Possessing a Nitric Oxide Donor Sulfohydroxamic Acid (SO2NHOH) Cyclooxygenase-2 Pharmacophore: Synthesis, Molecular Modeling, and Biological Evaluation as Anti-inflammatory Agents

ChemMedChem ◽  
2011 ◽  
Vol 7 (1) ◽  
pp. 62-67 ◽  
Author(s):  
Atul Bhardwaj ◽  
Zhangjian Huang ◽  
Jatinder Kaur ◽  
Edward E. Knaus
Keyword(s):  
Nitric Oxide ◽  
Molecular Modeling ◽  
Biological Evaluation ◽  
Cyclooxygenase 2 ◽  
Nitric Oxide Donor ◽  
Anti Inflammatory

scholarly journals The synthesis, characterization and biological evaluation of a new nitric oxide donor agent

2014 ◽  
Vol 79 (4) ◽  
pp. 389-400 ◽  
Author(s):  
Lenuta Profire ◽  
Maria Apotrosoaei ◽  
Anca Oprea ◽  
Mihai Brebu ◽  
Florentina Lupascu ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Weight Loss ◽  
Biological Properties ◽  
Biological Evaluation ◽  
Nitric Oxide Donor ◽  
Biological Assays ◽  
Ft Ir ◽  
Anti Inflammatory ◽  
Tg And Dtg ◽  
Inflammatory Effect

The synthesis of a new xanthine nitric oxide donor (TSP-81) has been discussed. The designed compound includes two structural moieties - theophylline (1,3-dimethylxanthine) and acetaminophen (4-hydroxyacetanilide) linked by the nitric oxide donor alkyl chain as a spacer. The compound has been characterized by microanalysis (CHN), 1H-NMR, 13C-NMR, FT-IR, UV-vis, TG and DTG. The thermal behaviour showed that TSP-81 melts with decomposition, in four steps, the most important ones being the 2nd one (the registered weight loss being 17.6 %) and the 3rd one (with a registered weight loss of 30.4 %). The toxicity degree, the anti-inflammatory effect and the ability of releasing nitric oxide of the TSP-81 have also been evaluated. The biological assays established that TSP-81 exhibits enhanced biological properties such as lower toxicity and higher anti-inflammatory effect in reference with theophylline and acetaminophen, the drugs used as parents molecules. The TSP-81 is approximately 2 times more active than theophylline and 4 times more active than acetaminophen in reducing cotton pellet-granuloma formation. Furthermore, the release of nitric oxide (NO) appears to have an important contribution to enhancing the anti-inflammatory effect.

Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents

2018 ◽  
Vol 77 ◽  
pp. 38-46 ◽  
Author(s):  
Adnan A. Bekhit ◽  
Ahmed M. Farghaly ◽  
Ragab M. Shafik ◽  
Mona M.A. Elsemary ◽  
Alaa El-Din A. Bekhit ◽  
...  
Keyword(s):  
Molecular Modeling ◽  
Antimicrobial Agents ◽  
Biological Evaluation ◽  
Anti Inflammatory

scholarly journals The cytoprotective effect of a nitric oxide donor drug on gastric mucous membrane of rats treated with ketoprofen, a non-steroidal anti-inflammatory drug

2006 ◽  
Vol 43 (3) ◽  
pp. 233-237 ◽  
Author(s):  
Afonso Luiz Villa ◽  
Ceneviva Reginaldo ◽  
Fernanda Viaro ◽  
Fernando Ramalho ◽  
Antonio Dorival Campos ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Isosorbide Dinitrate ◽  
Saline Solution ◽  
Isotonic Saline ◽  
Nitric Oxide Donor ◽  
Group Iii ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Gastric Mucous ◽  
Lesion Index

BACKGROUND: Non-steroidal anti-inflammatory drugs are considered today a very important group of medication, with a wide variety of therapeutic use, in different areas of modern medicine. Despite their beneficial effects on the patient, these drugs show a high incidence of side effects, mainly in the gastrointestinal tract. The physiopathological mechanisms of non-steroidal anti-inflammatory drugs induced lesions and the gastric mucosa defense mechanism became an important source for medical research, especially those which try to evaluate the role of nitric oxide as a cytoprotective agent. AIM: To define a possible cytoprotective effect of a nitric oxide donor, isosorbide dinitrate, on the gastric mucous of rats submitted to non-steroidal anti-inflammatory drugs ketoprofen treatment. METHODS: Adult male Wistar rats, previously submitted to starvation for 24 hours and divided in three groups: group I (standard): animals that received isotonic saline solution intragastric by gavage and intravenous. Group II (control-ketoprofen): animals that received isotonic saline solution intragastric by gavage and ketoprofen intravenous. Group III (nitrate/ketoprofen): animals that received 2mM solution of isosorbide dinitrate intragastric by gavage and ketoprofen intravenous. Later on, these animals were sacrificed and had their stomach removed and submitted to macroscopical, microscopical and biochemical studies. The evaluated parameters were: a) gastric lesion index; b) gastric mucous layer thickness; c) gastric tissue nitrate/nitrite (NOx) concentration and d) gastric tissue malondialdehyde concentration. RESULTS: a) Gastric lesion index evaluation showed a smaller statistically significant incidence on the animals of group III; b) group III showed a thicker mucous layer, which also was statistically significant, when compared to group II; c) the variation on tissue nitrate/nitrite concentration was similar in all three groups, without statistical significance when compared to each other. CONCLUSION: Isosorbide dinitrate has a cytoprotective activity on the gastric mucosa of rats submitted to ketoprofen action.

Structure-Based Design, Synthesis, and Biological Evaluation of Indomethacin Derivatives as Cyclooxygenase-2 Inhibiting Nitric Oxide Donors§

2007 ◽  
Vol 50 (25) ◽  
pp. 6367-6382 ◽  
Author(s):  
Shiow-Jyi Wey ◽  
Michael E. Augustyniak ◽  
Edward D. Cochran ◽  
James L. Ellis ◽  
Xinqin Fang ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Biological Evaluation ◽  
Cyclooxygenase 2 ◽  
Nitric Oxide Donors ◽  
Design Synthesis ◽  
Synthesis And Biological Evaluation

A novel indazolo-triazolo-benzotriazepine exerts anti-inflammatory effects by inhibition of cyclooxygenase-2 activity and nitric oxide synthase-2 expression

2003 ◽  
Vol 368 (1) ◽  
pp. 26-32 ◽  
Author(s):  
Patricia Fern�ndez ◽  
M. Isabel Guill�n ◽  
Amalia Ubeda ◽  
Pablo L�pez-Cremades ◽  
Enrique Aller ◽  
...  
Keyword(s):  
Nitric Oxide ◽  
Nitric Oxide Synthase ◽  
Cyclooxygenase 2 ◽  
Anti Inflammatory ◽  
Nitric Oxide Synthase 2 ◽  
Oxide Synthase
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