An unprecedented photochemical reaction for anthracene-containing derivatives

A series of anthracene-containing derivatives have been synthesised and characterised. The photochemical behaviour of these derivatives have been investigated by 1 H NMR spectroscopy. An unprecedented photolysis reaction for anthracene-containing derivatives was observed in the case of anthracenes directly armed with a -CH 2 O-R group upon UV irradiation. The photolysis reaction process has been demonstrated to occur in three steps. Firstly, the anthracene-containing derivatives are converted into the corresponding endoperoxide intermediate upon UV irradiation in the presence of air; then, the endoperoxide intermediate is decomposed to the corresponding starting compound and 9-anthraldehyde; finally, 9-anthraldehyde is further oxidised to anthraquinone. Additionally, the photolysis reaction of anthracene-containing derivatives is significantly promoted in the presence of a thiacalix[4]arene platform

Synthesis of Diverse Indene Derivatives from 1‑Diazonaphthalen-2(1<i>H</i>)‑ones via Thermal Cascade Reactions

A sequential Wolff rearrangement of 1-diazonaphthalen-2(1<i>H</i>)-ones followed by trapping of the ketene intermediate with primary and aromatic amines or alcohols and phenols in the presence of various aldehydes generates 1<i>H</i>-indene-3-carboxamides or 1<i>H</i>-indene-3-carboxylates. This constitutes an unprecedented three-component coupling reaction that allows for the synthesis of functionalized indene derivatives under catalyst-free thermal conditions

Synthesis of Diverse Indene Derivatives from 1‑Diazonaphthalen-2(1<i>H</i>)‑ones via Thermal Cascade Reactions

A sequential Wolff rearrangement of 1-diazonaphthalen-2(1<i>H</i>)-ones followed by trapping of the ketene intermediate with primary and aromatic amines or alcohols and phenols in the presence of various aldehydes generates 1<i>H</i>-indene-3-carboxamides or 1<i>H</i>-indene-3-carboxylates. This constitutes an unprecedented three-component coupling reaction that allows for the synthesis of functionalized indene derivatives under catalyst-free thermal conditions

Gardening at School for New Good Life: Entrepreneurship for Sustainable Education in the Public Schools in Nepal

Entrepreneurship skills are isolated from school science curricula in the context of Nepal. The study explores the students\u27 engagement in the school garden for entrepreneurship resulting in sustainable education. It explicitly reconnoiters the interconnection between entrepreneurship skills through mushroom farming and the curricula of basic-level public schools. Also, the study explores the pedagogical approaches to contextualized teaching and learning for sustainable education for a new good life. A qualitative research design under the interpretivism paradigm with a purposive sampling technique was employed to select the schools and the research participants. Qualitative data were collected through eighteen in-depth interviews and nine focus group discussions and were analyzed using the Atlas-ti software. The study found that students, parents, and teachers actively engaged in mushroom farming in the school connected activities with curricula and enjoyed learning by earning. The contribution of this study chiefly lies in making a new good life through mushroom farming for economically backward parents. It is recommended that the Ministry of Education of Nepal’s government needs to formulate policies regarding entrepreneurship-based sustainable education in the context of school education in Nepal

Rational Tuning of Visual Cycle Modulator Pharmacodynamics

Modulators of the visual cycle have been developed for treatment of various retinal disorders. These agents were designed to inhibit retinoid isomerase [retinal pigment epithelium-specific 65 kDa protein (RPE65)], the rate-limiting enzyme of the visual cycle, based on the idea that attenuation of visual pigment regeneration could reduce formation of toxic retinal conjugates. Of these agents, certain ones that contain primary amine groups can also reversibly form retinaldehyde Schiff base adducts, which contributes to their retinal protective activity. Direct inhibition of RPE65 as a therapeutic strategy is complicated by adverse effects resulting from slowed chromophore regeneration, whereas effective retinal sequestration can require high drug doses with potential off-target effects. We hypothesized that the RPE65-emixustat crystal structure could help guide the design of retinaldehyde-sequestering agents with varying degrees of RPE65 inhibitory activity. We found that addition of an isopropyl group to the central phenyl ring of emixustat and related compounds resulted in agents effectively lacking in vitro retinoid isomerase inhibitory activity, whereas substitution of the terminal 6-membered ring with branched moieties capable of stronger RPE65 interaction potentiated inhibition. The isopropyl derivative series produced discernible visual cycle suppression in vivo, albeit much less potently than compounds with a high affinity for the RPE65 active site. These agents were distributed into the retina and formed Schiff base adducts with retinaldehyde. Except for one compound [3-amino-1-(3-isopropyl-5-((2,6,6-trimethylcyclohex-1-en-1-yl)methoxy)phenyl)propan-1-ol (MB-007)], these agents conferred protection against retinal phototoxicity, suggesting that both direct RPE65 inhibition and retinal sequestration are mechanisms of potential therapeutic relevance