Design, synthesis and biological evaluation of benzoxazolinone-containing 1,3,4-thiadiazoles as TNF-α inhibitors

A library of nineteen benzoxazolinone-based 1,3,4-thiadiazoles has been synthesized and screened for their anti-inflammatory activity. The compound 1f exhibited a potent anti-inflammatory activity with an inhibition of 65.83% and 32.50% after 3 h and 5 h respectively. It also exhibited a significant in vitro (p < 0.01), TNF- α inhibitory activity with 51.44 % inhibition. The compound 1f showed hydrogen bonding with GLN 61 and interactions with TYR 119, TYR 151 and GLY 121. The histopathology report showed that none of the compounds caused gastric ulceration. The results from the in vivo &amp; in vitro antiinflammatory activity along with In Silico studies exhibit that benzoxazolinone-based 1,3,4-thiadiazoles may be used in the future development of anti-inflammatory drugs

Two new pentacyclic triterpenoid glycosides from the bark of <i>Terminalia arjuna</i>

2905-2908Two new pentacyclic triterpenoid glycosides isolated from the bark of Terminalia arjuna, have been characterized as olean-3α,22β-diol-12-en-28-oic acid-3-O-β--glucopyranosyl (1→4)-β- -glucopyranoside 1 and olean-3β,6β,22α-triol-12-en-28-oic acid-3-O-β- -glucopyranosyl (1→4)- β- -glucopyranoside 2 on the basis of spectral data analyses and chemical studies

QUANTITATIVE DETERMINATION OF PLATINUM AND PALLADIUM IN DONEPEZIL HYDROCHLORIDE USING INDUCTIVELY COUPLED PLASMA – OPTICAL EMISSION SPECTROSCOPY

Objective: To develop a precise, accurate, sensitive and selective analytical method using inductively coupled plasma – optical emission spectroscopy (ICP-OES) for the determination of platinum and palladium in Donepezil hydrochloride raw material, a reversible acetyl cholinesterase inhibitor.Methods: The method developed and validated uses dry ashing for the extraction of platinum and palladium from Donepezil hydrochloride. Ash thus obtained was leached into an acidic solution followed by analysis of platinum and palladium using ICP-OES at wavelength 306.471 nm and 340.458 nm respectively. The method was studied for the various validation parameters including precision, accuracy, linearity, etc. for both the elements.Results: The method was found to be linear in the wide working range of 0.2 µg/ml to16 µg/ml with a correlation coefficient of 0.9998 for platinum and 0.1µg/ml to 8µg/ml with a correlation coefficient of 0.9999 for palladium. The recoveries of platinum and palladium from the spiked samples of Donepezil hydrochloride at three different spiking levels were found to be in the range of 86.87 – 98.59% for both platinum and palladium. The limit of detection was found as 0.1 µg/ml and 0.05 µg/ml for platinum and palladium respectively while the limit of quantitation was found to be 0.2 µg/ml and 0.1 µg/ml for platinum and palladium.Conclusion: The results of the validation studies indicate that the proposed method can be used for the simultaneous determination of platinum and palladium in Donepezil hydrochloride to ensure the quality and purity of Donepezil hydrochloride as a raw material for formulating the pharmaceutical formulations.Â

Two new terpenes from the lichen Parmelia perlata

173-176The lichen Parmelia perlata has yielded a new lanost-2-en type triterpene, named parmelanostene and a new labdane type diterpenoid, named permelabdone, identified on the basis of spectroscopic studies as 29, 30-nordimethyl-lanost-2-en 1 and 2'-methoxyphenyl-19-[4α, 8β, 10β-trimethyl-9-(13-methyl butyl)-decahydronapthalen-4-yl]-20-methoxybenzoate 2, respectively which were also found to have antibacterial potential against S. aureus and E. coli bacterial strains

Two new phytoconstituents from Rumex maritimus

619-622A new polyhydroxy ketone derivative and a terpene glycoside have been isolated from the seeds of Rumex maritimus. Their structures have been established as 3,7,11,15-tetramethyl-n-octadac-13-en-3,4,6,7,8,11-hexol-12-one 1 and 8 β-hydroxy-14β -methyl-7-oxopodocarp-5-en-13-(19⍺-hydroxy-19,22,22-trimethylheptyl)-22-O-(β-D-glucopyranosyl)-(41) β-D-glucopyranoside 2, respectively, on the basis of chemical and spectral data analysis