scholarly journals Development, Characterization and Pharmacological Investigation of Umbelliferone Conjugates of NSAIDs

2021 ◽  
Vol 30 (1) ◽  
pp. 240-248
Author(s):  
NIJA B ◽  
Arun Rasheed ◽  
A Kottaimuthu
Keyword(s):  
Mefenamic Acid ◽  
Protective Action ◽  
Chemical Characterization ◽  
Parent Drug ◽  
Brain Targeting ◽  
The Central Nervous System ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Ester Prodrug ◽  
Ester Prodrugs

The present investigation developed the ester prodrugs of Non-steroidal anti inflammatory drugs (NSAIDs), Mefenamic acid and Flurbiprofen by conjugating with the natural antioxidant, 4-methyl umbelliferone that resulted the formation of Mefenamic acid-umbelliferone ester prodrug and Flurbiprofen-umbelliferone ester prodrug .The principal objective this study is the synthesis of the ester prodrugs of NSAIDs with the enhanced therapeutic activity and minimized side effects. Prodrugs were synthesized by coupling method using N,N’- dicyclohexylcarbodiimide/4-dimethylaminopyrimidine, subjected to  physical, chemical characterization, spectral characterization (IR, 1H NMR, 13C NMR and Mass spectra),hydrolysis-kinetic study and pharmacological evaluation such as anti-inflammatory, ulcerogenecity as well as the effect of the NSAIDs in the central nervous system against degenerative mechanisms. The current study revealed that the umbelliferone conjugates of NSAIDs which upon administration would release the parent drug as a result of enzymatic or non-enzymatic hydrolysis in the desired site with enhanced anti inflammatory activity and reduction in the gastro intestinal toxicity. Also the synthesized pordrugs showed enhanced brain targeting efficiency with protective action against the degenerative processes.

Multidrug salt forms of norfloxacin with non-steroidal anti-inflammatory drugs: solubility and membrane permeability studies

CrystEngComm ◽  
2018 ◽  
Vol 20 (41) ◽  
pp. 6420-6429 ◽  
Author(s):  
Biswajit Bhattacharya ◽  
Amit Mondal ◽  
Saundray Raj Soni ◽  
Susobhan Das ◽  
Surojit Bhunia ◽  
...  
Keyword(s):  
Membrane Permeability ◽  
Mefenamic Acid ◽  
Dissolution Properties ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Permeability Studies ◽  
Salt Forms

Dissolution properties and membrane permeability studies were conducted for four newly prepared multidrug salts of norfloxacin with four NSAIDs, diclofenac, diflunisal, mefenamic acid and indomethacin.

scholarly journals Anti-Inflammatory and Gastroprotective Evaluation of Prodrugs of Piroxicam

Ulcers ◽  
2014 ◽  
Vol 2014 ◽  
pp. 1-4 ◽  
Author(s):  
Vivekkumar K. Redasani ◽  
Amol B. Shinde ◽  
Sanjay J. Surana
Keyword(s):  
Cinnamic Acid ◽  
Parent Drug ◽  
Inflammatory Activity ◽  
Hydroxyl Group ◽  
Ulcer Index ◽  
Cinnamic Acid Derivative ◽  
Rat Paw Edema ◽  
Anti Inflammatory ◽  
Rat Paw ◽  
Ester Prodrug

Therapeutically potential prodrugs of piroxicam were synthesized by effective masking of enolic hydroxyl group through generation of ester congeners. The reaction facilitated using N,N′-dicyclohexylcarbodiimide coupled with acetic acid, benzoic acid, p-toluic acid, m-toluic acid, and cinnamic acid. Synthesized prodrugs were characterized for confirmation of the said structures. The modification of piroxicam showed better anti-inflammatory activity as evoked by all prodrugs. Interestingly, compound 3e, cinnamic acid ester prodrug, depicted 75 percent inhibition of rat paw edema as compared to 56 percent for parent piroxicam at 6 h of study. The present work proves the applicability not only with increased anti-inflammatory activity, but also with marked attenuation in ulcerogenicity. Novel prodrug 3e, cinnamic acid derivative, was found to be the least ulcerogenic having ulcer index of 0.67 as compared to parent drug piroxicam with 2.67.

Non-steroidal anti-inflammatory drugs and their effect on the nervous system: neurotoxicity, types, mechanism of occurrence

2021 ◽  
pp. 459-464
Author(s):  
Elmira Erfanovna Alimova ◽  
Elena Evgenievna Al-Rabadi
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Hearing Loss ◽  
Side Effects ◽  
World Health ◽  
The World ◽  
The Central Nervous System ◽  
Inflammatory Drugs ◽  
Anti Inflammatory ◽  
Health Organization

Currently, according to the World Health Organization, about 20% of the world's population takes non-steroidal anti-inflammatory drugs (NSAIDs). NSAIDs are lipophilic substances that easily penetrate the blood-brain barrier and can cause side effects from the central nervous system. Neurotoxicity (headache, dizziness, insomnia, depression, depersonalization, psychosis, and tremor occur during the treatment with indomethacin; visual impairment, drowsiness - during the treatment with meloxicam; hearing loss - when taking salicylates) ranks second after gastrotoxicity. The article describes the mechanisms of neurotoxicity that occur when taking NSAIDs.

Manganese-mefenamic acid complexes exhibit high lipoxygenase inhibitory activity

2014 ◽  
Vol 43 (28) ◽  
pp. 10930-10939 ◽  
Author(s):  
Jie Feng ◽  
Xin Du ◽  
Hui Liu ◽  
Xin Sui ◽  
Chen Zhang ◽  
...  
Keyword(s):  
Metal Ions ◽  
Metal Complexes ◽  
Mefenamic Acid ◽  
Inhibitory Activity ◽  
Inflammatory Drugs ◽  
Anti Inflammatory

The coordination of non-steroidal anti-inflammatory drugs (NSAIDs) to metal ions could improve the pharmaceutical efficacy of NSAIDs due to the unique characteristics of metal complexes.

Sign in / Sign up

Export Citation Format

Share Document