Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and receptors in live organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarins compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, anti-diabetics, anti-inflammatory, antibacterial, antifungal and anti-neurodegerative agents. Additionally, it also includes applications of coumarins as fluorescent sensors for biological systems. Thus, this work aims to contribute to the development of new rational research projects for the treatment and diagnosis of pathologies using coumarin derivatives.
Coumarin-β-ketoesters were used to synthesize new blue-fluorescent compounds exhibiting ICT. The Knoevenagel intermediate suggests that our Biginelli reaction passing by this mechanistic way is unlikely.
Emissive 7-OH-coumarins were synthesized by a microwave-assisted protocol and spectral changes were induced after conformational changes in low polarity media.
Coumarins are natural products characterized as 2H-chromen-2-one, according to IUPAC nomenclature, largely distributed in plants, as well as, in species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert non-covalent interactions with many enzymes an receptors in living organisms lead the coumarins to exhibit a wide range of biological activities and applications. Then, this manuscript provides an overview of the use of coumarin compounds in medicinal chemistry in treating many diseases. Important examples of the last years have been selected concerning the activities of coumarins as anticoagulant, anticancer, antioxidant, antiviral, antidiabetics, anti-inflammatory, antibacterial, antifungal, and anti-neurodegenerative agents. Thus, this work aims at contributing to the development of new rational research projects searching for new treatments and bioactive compounds for many pathologies using coumarin derivatives.
A synthetic procedure for obtaining the fluorescent coumarin umbelliferone (7-hydroxycoumarin) and its spectral parameters were fully developed aiming at an undergraduate organic chemistry laboratory class. Umbelliferone is traditionally prepared via Pechmann condensation using malic acid, resorcinol and sulfuric acid as catalyst. The use of domestic microwave oven and the absence of solvent allow our methodology to be simple, fast and easy applied in obtaining umbelliferone at organic chemistry laboratory being greener than classical techniques of synthesis. In this class the student will learn how to measure the potency of a microwave oven, the applicability of this kind of irradiation in the organic synthesis of fluorescent compounds and how to determine the pKa of an organic compound through an UV/VIS spectrometric analysis. These experiments were designed to be suitable for a second and third year undergraduate curriculum.
A doença de Alzheimer (DA) é atualmente uma das demências mais estudadas devido ao aumento de casos com o passar dos anos. Os inibidores de acetilcolinesterase (AChE) tem sido amplamente estudados com o intuito de obtermos novos candidatos a fármacos no combate a DA. Neste sentido novos derivados do produto natural 6-gingerol foram planejdos e analisados frente a inibição da enzima acetilcolinesterase in silico e sua previsão sobre o modelo de Absorção, Distribuição, Metabolismo, Eliminação e Toxicidade (ADMET). Usando ferramentas de modelagem molecular para minimizar as estruturas do compostos estudados e então verificar as interações destes derivados em comparação com o padrão donepezila, devido sua semelhança estrutural, com a enzima AChE. Os resultados mostraram que dois compostos apresentam as melhores interações in silico e as melhores propriedades ADMET para um bom fármaco que pode atuar no Sistema Nervoso Central.
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