Synthesis of 1,2,3-triazole tethered bifunctional hybrids by click chemistry and their cytotoxic studies

In view of the drug resistance with most of the currently used anticancer drugs, molecular hybrids of pyrazolyl chalcones and p-nitro benzyl functionalities tethered by triazole ring have been synthesised and evaluated for cytotoxic studies against three human cancer cell lines (THP, COLO-205, A-549). The results of the preliminary investigation exhibited marked dependence of the cytotoxic activity on the electronic factors. Placement of naphthyl (JGPT-11) and trimethoxy phenyl ring (JGPT-6) as ring A proved to be extremely beneficial in enhancing the cytotoxic potential. Thus we herein report the synthesis and cytotoxic studies of a new class of molecular hybrids. Detailed investigation on the biological mechanistic insights of JGPT-11 and 6 is under progress.     

Aprepitant’s Prophylactic Efficacy in Decreasing Postoperative Nausea and Vomiting in Morbidly Obese Patients Undergoing Bariatric Surgery

Background

Postoperative nausea and vomiting is a major cause of patient dissatisfaction towards surgery. For bariatric surgery, increased vomiting/retching is detrimental to surgical anastomosis. The present study evaluated the efficacy of aprepitant (neurokinin-1 inhibitor) as a prophylactic antiemetic in morbidly obese patients for laparoscopic bariatric surgery.

Methods

After institutional review board approval, 125 morbidly obese patients were recruited into this double-blind placebo-controlled trial. On random division, the patients received a tablet of aprepitant (80 mg) in group A, or a similar-appearing placebo in group P, an hour prior to surgery. All patients received intravenous ondansetron (4 mg) intraoperatively. Postoperatively, the patients were evaluated for nausea and vomiting by a blinded evaluator at 30 min, 1, 2, 6, 24, 48, and 72 h.

Results

Both groups were evenly distributed for age, body mass index, type, and length of surgery. Cumulative incidence of vomiting at 72 h was significantly lower in group A (3 %) compared to group P (15 %; p?=?0.021). Odds ratio for vomiting in group P compared to group A was 5.47 times. On Kaplan–Meier plot, time to first vomiting was also significantly delayed in group A (p?=?0.019). A higher number of patients showed complete absence of nausea or vomiting in group A compared to group P (42.18 vs. 36.67 %). On the other hand, nausea scores were unaffected by aprepitant, and no significant difference between groups was found at any of the measured time points.

Conclusions

In morbidly obese patients undergoing laparoscopic bariatric surgery, addition of aprepitant to ondansetron can significantly delay vomiting episodes simultaneously lowering the incidence of postoperative vomiting.     

A Systematic Review on Cannabis Hyperemesis Syndrome and Its Management Options

IntroductionSeveral forms of cannabinoids are currently being used to manage nausea and vomiting (N/V). Emerging cases of refractory N/V associated with chronic cannabis use among adults and older patients have been reported named cannabis hyperemesis syndrome (CHS). CHS is a condition that leads to repeated and severe N/V in long-term users of cannabinoids.ObjectiveThe aim of this study was to outline current treatments for the management of CHS.MethodsA systematic review was conducted using PubMed, Ovid MEDLINE, Cochrane Central, EMBASE, and Google Scholar. Databases were used to search for articles on CHS published from January 2009 to June 2021, yielding 225 results of which 17 were deemed relevant and underwent review by 2 separate reviewers.ResultsThe duration of cannabis administration ranged between 6 months to 11 years may precipitate symptoms of CHS. The Rome IV diagnostic criteria of CHS require cannabinoid use and persistence of N/V symptoms for at least the past 6 months. Cannabis cessation is noted to be the most successful management, but other treatments also demonstrated symptom relief; these include hot water hydrotherapy, topical capsaicin cream, haloperidol, droperidol, benzodiazepines, propranolol, and aprepitant administration.ConclusionMore research on CHS is needed to enhance knowledge translation, education, and create awareness in the medical community on the side effects of cannabinoids and to propose the best treatment options.     

Nutritional and Functional Properties of Defatted,Debittered and Off-Flavour Free High Protein Guar (Cyamopsis tetragonoloba) Meal Flour

Proceedings of the National Academy of Sciences, India Section B: Biological Sciences - A process for the preparation of defatted, debittered and off-flavour free guar meal flour (GMF) with high...     

A facile and new approach to synthesize 2-amino-4-(4-amoinophenyl)-1<Emphasis Type="Italic">H</Emphasis>-1,3-diazol-1-yl-alkylaminomethanethiones

An “intellectual connection” approach to design a facile and new synthesis of suitably substituted 2-aminoimidazole-based precursors of expected antiasthmatic agents through a benzidine type of rearrangement of 2-phenylazoimidazole and subsequent coupling of the product thus obtained with alkylisothiocyanates involving a degenerative operation, thereby improving the time frame of the overall synthetic sequence, is reported. The alkylisothiocyanates required in this synthetic sequence are prepared using a best combination of reported methods. The compounds reported here can be used to produce derivatives of other biological agents.