New Histamine-Related Five-Membered N-Heterocycle Derivatives as Carbonic Anhydrase I Activators

A series of histamine (HST)-related compounds were synthesized and tested for their activating properties on five physiologically relevant human Carbonic Anhydrase (hCA) isoforms (I, II, Va, VII and XIII). The imidazole ring of HST was replaced with different 5-membered heterocycles and the length of the aliphatic chain was varied. For the most interesting compounds some modifications on the terminal amino group were also performed. The most sensitive isoform to activation was hCA I (KA values in the low micromolar range), but surprisingly none of the new compounds displayed activity on hCA II. Some derivatives (1, 3a and 22) displayed an interesting selectivity for activating hCA I over hCA II, Va, VII and XIII.

Comprehensive Review on Synthetic Approaches and Biological Activities of 1,3,4-Oxadiazole

Among the large variety of nitrogen and oxygen heterocycles, 1,3,4-oxadiazole, the scaffold, has attracted considerable attention owing to its ability to showing an extensive range of pharmacological actions. Therefore, significant efforts of organic chemists have been directed towards the construction of new drug candidates containing 1,3,4-oxadiazole subunits connected to a known pharmaceutical or a potential pharmacophore. This digest highlights recent publications on the various synthesis techniques of 1,3,4-oxadiazole and related compounds over the previous ten years (2011–2021). The purpose of this review is to learn about several ways for synthesizing oxadiazole. These heterocyclics are formed mainly by the cyclization reactions of various reactants under diverse circumstances. According to the literature investigations, they were given a high priority for their pharmacological significance, such as anticonvulsant, anticancer, antioxidant, anti-inflammatory, antibacterial, antidiabetic, etc.

Characterization of opposing responses to phenol by Bacillus subtilis chemoreceptors

Bacillus subtilis employs ten chemoreceptors to move in response to chemicals in its environment. While the sensing mechanisms have been determined for many attractants, little is known about the sensing mechanisms for repellents. In this work, we investigated phenol chemotaxis in B. subtilis . Phenol is an attractant at low, micromolar concentrations, and a repellent at high, millimolar concentrations. McpA was found to be the principal chemoreceptor governing the repellent response to phenol and other related aromatic compounds. In addition, the chemoreceptors McpC and HemAT were found to govern the attractant response to phenol and related compounds. Using chemoreceptor chimeras, McpA was found to sense phenol using its signaling domain rather than its sensing domain. These observations were substantiated in vitro, where direct binding of phenol to the signaling domain of McpA was observed using saturation-transfer difference nuclear magnetic resonance. These results further advance our understanding of B. subtilis chemotaxis and further demonstrate that the signaling domain of B. subtilis chemoreceptors can directly sense chemoeffectors. IMPORTANCE Bacterial chemotaxis is commonly thought to employ a sensing mechanism involving the extracellular sensing domain of chemoreceptors. Some ligands, however, appear to be sensed by the signaling domain. Phenolic compounds, commonly found in soil and root exudates, provide environmental cues for soil microbes like Bacillus subtilis . We show that phenol is sensed both as an attractant and a repellent. While the mechanism for sensing phenol as an attractant is still unknown, we found that phenol is sensed as a repellent by the signaling domain of the chemoreceptor McpA. This study furthers our understanding of the unconventional sensing mechanisms employed by the B. subtilis chemotaxis pathway.

Effectiveness of Curcumin on Outcomes of Hospitalized COVID-19 Patients: A Systematic Review of Clinical Trials

Despite the ongoing vaccination efforts, there is still an urgent need for safe and effective treatments to help curb the debilitating effects of COVID-19 disease. This systematic review aimed to investigate the efficacy of supplemental curcumin treatment on clinical outcomes and inflammation-related biomarker profiles in COVID-19 patients. We searched PubMed, Scopus, Web of Science, EMBASE, ProQuest, and Ovid databases up to 30 June 2021 to find studies that assessed the effects of curcumin-related compounds in mild to severe COVID-19 patients. Six studies were identified which showed that curcumin supplementation led to a significant decrease in common symptoms, duration of hospitalization and deaths. In addition, all of these studies showed that the intervention led to amelioration of cytokine storm effects thought to be a driving force in severe COVID-19 cases. This was seen as a significant (p < 0.05) decrease in proinflammatory cytokines such as IL1β and IL6, with a concomitant significant (p < 0.05) increase in anti-inflammatory cytokines, including IL-10, IL-35 and TGF-α. Taken together, these findings suggested that curcumin exerts its beneficial effects through at least partial restoration of pro-inflammatory/anti-inflammatory balance. In conclusion, curcumin supplementation may offer an efficacious and safe option for improving COVID-19 disease outcomes. We highlight the point that future clinical studies of COVID-19 disease should employ larger cohorts of patients in different clinical settings with standardized preparations of curcumin-related compounds.

Synthesis, crystal structure and Hirshfeld surface analysis of 2-(perfluorophenyl)acetamide in comparison with some related compounds

The molecular and crystal structures of the title compound, C8H4F5NO, were examined by single-crystal X-ray diffraction and Hirshfeld surface analysis. The title compound was synthesized by a new method at the interface of aqueous solutions of LiOH and pentafluorophenylacetonitrile. In the crystal, hydrogen bonds and π–halogen interactions connect the molecules into double layers. Analysis of the Hirshfeld surface showed that the most important contributions to the crystal packing are made by F...F (30.4%), C...F/F...C (22.9%), O...H/H...O (14.9%), H...F/F...H (14.0%) and H...H (10.2%) contacts. The Hirshfeld surfaces of analogues of the title compound were compared and the effect of perfluorination on the crystal packing was shown.

Synthesis of Fluorenes and Their Related Compounds from Biaryls and Meldrum’s Acid Derivatives

A new synthetic method for preparing fluorenes from amino group-containing biaryls and Meldrum’s acid derivatives was developed. The reaction proceeded without a catalyst and loss of functional groups. The corresponding...

Biological activity and its related compounds of Red Jasmine rice extracts linked to normal fibroblast viability for cosmetic product

Red jasmine rice is recognized as a healthy food with high phenolic compounds. These compounds present antibacterial and anti-free radical properties. Moreover, colored rice exhibits a biological activity against anticancer. Objectives of this study are 1) exploring a biological screening and cell viability of 70% ethanol and aqueous extracts of red jasmine rice, 2) investigating cytotoxicity to fibroblast NIH3T3 (IC80) that is one hundred cells were found cell viability 80 cells. Red jasmine rice extracts were dried and transformed into a powder using the freeze-drying method. The extracts were treated with fibroblast NIH3T3 for MTT. The highest of IC50 of red jasmine rice extract to scavenge the DPPH and ABTS radicals was found in ethanol extract (53.20±7.37 and 64.17±5.76, respectively). The experiment showed that the ethanol and aqueous extract of red rice did not show cytotoxicity to fibroblast NIH3T3 (IC80). The extracts of red rice show the biological screening of anti-oxidation with total phenolic compounds and flavonoid contents. Moreover, it does not modify the physical properties of the cream formula. It can be concluded that the red rice extract is highly promising for the value addition.

Recent updates on Synthetic Strategies and Biological Potential of 1,3,4-oxadiazole: Review

Among the large variety of nitrogen and oxygen-containing heterocycles, 1,3,4-oxadiazole, the scaffold, has attracted considerable attention owing to its ability to show an extensive range of pharmacological actions. According to literature investigations, prepared 1,3,4-oxadiazole and its derivative are pharmacologically significant and consist of a variety of activities, such as anticonvulsant, anticancer, antioxidant, anti-inflammatory, antibacterial, antidiabetic, etc. These heterocyclics are formed mainly by the cyclization reactions of various reactants under diverse reaction circumstances. Therefore, significant efforts of organic chemists have been directed towards the synthesis of new drug candidates containing 1,3,4-oxadiazole subunits connected to an established potential pharmacophore to improve the efficacy and potency. This article aims to highlight recent publications on the various synthesis techniques of 1,3,4-oxadiazole and related compounds over the previous ten years (2011–2021). The purpose of this review is to help researchers by summarizing several synthetic strategies for synthesizing oxadiazole.