Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

Benassi, Alessandra; Doria, Filippo; Pirota, Valentina

doi:10.20944/preprints202011.0029.v1

Cited by 12 publications

(7 citation statements)

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“…Five-membered heterocyclic derivatives, as pyrroles [25], imidazoles [26], triazoles [27,28], and oxadiazoles [29,30] attracted increasing attention during the last years for their interesting biological properties [31]. In this context, tetrazoles are a class of non-natural heterocyclic compounds, composed of a five-membered ring, and can be mono-or di-substituted (Fig.…”

Section: Photochemical Properties Of 25-diaryl Tetrazolesmentioning

confidence: 99%

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Lights on 2,5-diaryl tetrazoles: applications and limits of a versatile photoclick reaction

Pirota

Benassi

Doria

2022

Photochem Photobiol Sci

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Recently, photoclick chemistry emerged as a powerful tool employed in several research fields, from medicinal chemistry and biology to material sciences. The growing interest in this type of chemical process is justified by the possibility to produce complex molecular systems using mild reaction conditions. However, the elevated spatio-temporal control offered by photoclick chemistry is highly intriguing, as it expands the range of applications. In this context, the light-triggered reaction of 2,5-diaryl tetrazoles with dipolarophiles emerged for its interesting features: excellent stability of the substrates, fast reaction kinetic, and the formation of a highly fluorescent product, fundamental for sensing applications. In the last years, 2,5-diaryl tetrazoles have been extensively employed, especially for bioorthogonal ligations, to label biomolecules and nucleic acids. In this review, we summarized recent applications of this interesting photoclick reaction, with a particular focus on biological fields. Moreover, we described the main limits that affect this system and current strategies proposed to overcome these issues. The general discussion here presented could prompt further optimization of the process and pave the way for the development of new original structures and innovative applications. Graphical abstract

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Section: Photochemical Properties Of 25-diaryl Tetrazolesmentioning

confidence: 99%

“…Fig.11Recent examples of tetrazole scaffolds designed to optimize cycloaddition efficiency (24 and 25) and as innovative photoaffinity probes(26)(27)(28)(29)(30)(31) …”

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confidence: 99%

Lights on 2,5-diaryl tetrazoles: applications and limits of a versatile photoclick reaction

Pirota

Benassi

Doria

2022

Photochem Photobiol Sci

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“…[ 71 , 72 , 73 , 74 ]. Hence, oxadiazole is considered a significant heterocyclic core and becomes a major scaffold for the development of new drug candidates because of its potential to be involved in the binding interactions with different targets or receptors with suitable metabolic profile [ 75 , 76 , 77 , 78 ].…”

Section: Future Developmentmentioning

confidence: 99%

Green Synthetic Approach: An Efficient Eco-Friendly Tool for Synthesis of Biologically Active Oxadiazole Derivatives

et al. 2021

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Green synthetic protocol refers to the development of processes for the sustainable production of chemicals and materials. For the synthesis of various biologically active compounds, energy-efficient and environmentally benign processes are applied, such as microwave irradiation technology, ultrasound-mediated synthesis, photo-catalysis (ultraviolet, visible and infrared irradiation), molecular sieving, grinding and milling techniques, etc. Thesemethods are considered sustainable technology and become valuable green protocol to synthesize new drug molecules as theyprovidenumerous benefits over conventional synthetic methods.Based on this concept, oxadiazole derivatives are synthesized under microwave irradiation technique to reduce the formation of byproduct so that the product yield can be increased quantitatively in less reaction time. Hence, the synthesis of drug molecules under microwave irradiation follows a green chemistry approach that employs a set of principles to minimize or remove the utilization and production of hazardous toxic materials during the design, manufacture and application of chemical substances.This approach plays a major role in controlling environmental pollution by utilizing safer solvents, catalysts, suitable reaction conditions and thereby increases the atom economy and energy efficiency. Oxadiazole is a five-membered heterocyclic compound that possesses one oxygen and two nitrogen atoms in the ring system.Oxadiazole moiety is drawing considerable interest for the development of new drug candidates with potential therapeutic activities including antibacterial, antifungal, antiviral, anticonvulsant, anticancer, antimalarial, antitubercular, anti-asthmatic, antidepressant, antidiabetic, antioxidant, antiparkinsonian, analgesic and antiinflammatory, etc. This review focuses on different synthetic approaches of oxadiazole derivatives under microwave heating method and study of their various biological activities.

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“…For examples, some of such enzymes and membrane transporters may include carbonic anhydrases, monocarboxylate transporters, proton or bicarbonate transporters. (9)(10)(11)(12)(13)(14)(15)(16)(17)(18).…”

Section: (Manuscripts In Preparation)mentioning

confidence: 99%

Treatment of Overweight and Obesity by Suppressing Intestinal Epithelial Renewal in a Mouse Model of Obesity

Zeng¹

2021

Preprint

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Obesity and overweight pose serious risk for many diseases and clinical conditions. However currently available weight loss strategies and pharmacotherapies of obesity are not satisfactory. This study shows that treatments with pH modifiers such as acids are not only well tolerated by obese mice but also very effective in reducing bodyweight and fat mass by depleting and suppressing the proliferation of proliferating epithelial cells of the intestinal villi. Therefore other cell proliferation inhibitors that suppress intestinal epithelial renewal can also be used for pharmacotherapy of obesity and overweight.

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Groundbreaking Anticancer Activity of Highly Diversified Oxadiazole Scaffolds

Cited by 12 publications

References 100 publications

Lights on 2,5-diaryl tetrazoles: applications and limits of a versatile photoclick reaction

Lights on 2,5-diaryl tetrazoles: applications and limits of a versatile photoclick reaction

Green Synthetic Approach: An Efficient Eco-Friendly Tool for Synthesis of Biologically Active Oxadiazole Derivatives

Treatment of Overweight and Obesity by Suppressing Intestinal Epithelial Renewal in a Mouse Model of Obesity

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