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1.
Curr Top Med Chem ; 2024 Aug 06.
Artículo en Inglés | MEDLINE | ID: mdl-39108108

RESUMEN

Synthetic routes of chromene are an area of thrust research due to its wide application as pigments, agrochemicals, cosmetics, and an important nucleus scaffold for various pharmaco-logically active drugs. The chromene nucleus is an important moiety for the discovery of new drug candidates owing to its broad range of pharmacological actions like antitumor, anti-inflammatory, antiviral, and many others. However, traditional synthesis techniques frequently use unsafe reagents and produce hazardous waste, presenting environmental issues. The eco-friendly production of chromene derivatives utilizes sustainable raw materials, non-toxic cata-lysts, and gentle reaction conditions to reduce ecological consequences. Innovative methods like microwave irradiation, ultrasound synthesis, the use of environmentally friendly solvents, a cata-lyst-based approach with minimal environmental impact, and mechanochemistry-mediated syn-thesis are implemented. These approaches provide benefits in scalability, cost-effectiveness, and ease of purification. This review compiles and presents various recently reported green synthetic strategies of chromene and its derivatives and gives the reader a clear idea of the detailed and crit-ical aspects of various synthetic protocols described.

2.
Med Chem ; 20(5): 503-536, 2024.
Artículo en Inglés | MEDLINE | ID: mdl-38275074

RESUMEN

One of the most effective therapeutic decencies in the treatment of Type 2 Diabetes Mellitus is the inhibition of α-glucosidase enzyme, which is present at the brush border of the intestine and plays an important role in carbohydrate digestion to form mono-, di-, and polysaccharides. Acarbose, Voglibose, Miglitol, and Erniglitate have been well-known α-glucosidase inhibitors in science since 1990. However, the long synthetic route and side effects of these inhibitors forced the researchers to move their focus to innovate simple and small heterocyclic scaffolds that work as excellent α-glucosidase inhibitors. Moreover, they are also effective against the postprandial hyperglycemic condition in Type 2 Diabetes Mellitus. In this aspect, this review summarizes recent progress in the discovery and development of heterocyclic molecules that have been appraised to show outstanding inhibition of α-glucosidase to yield positive effects against diabetes.


Asunto(s)
Diabetes Mellitus Tipo 2 , Inhibidores de Glicósido Hidrolasas , Compuestos Heterocíclicos , Hipoglucemiantes , alfa-Glucosidasas , Inhibidores de Glicósido Hidrolasas/farmacología , Inhibidores de Glicósido Hidrolasas/química , Inhibidores de Glicósido Hidrolasas/síntesis química , Inhibidores de Glicósido Hidrolasas/uso terapéutico , Diabetes Mellitus Tipo 2/tratamiento farmacológico , Humanos , alfa-Glucosidasas/metabolismo , Compuestos Heterocíclicos/química , Compuestos Heterocíclicos/farmacología , Compuestos Heterocíclicos/síntesis química , Compuestos Heterocíclicos/uso terapéutico , Hipoglucemiantes/farmacología , Hipoglucemiantes/química , Hipoglucemiantes/uso terapéutico , Hipoglucemiantes/síntesis química , Animales , Estructura Molecular , Relación Estructura-Actividad
3.
J Chromatogr Sci ; 61(10): 943-952, 2023 Dec 13.
Artículo en Inglés | MEDLINE | ID: mdl-36465018

RESUMEN

A simple, specific, accurate and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the determination of lacosamide, using C18 column and a mobile phase composed of phosphate buffer (pH 4.0):acetonitrile (40:60 v/v). The retention time of lacosamide was found to be 2.7 min. Linearity was established for lacosamide in the range of 10-50 µg/mL. The percentage recovery of lacosamide was found to be in the range of 97.37-99.20%. The drug was subjected to acid, alkali, oxidation, dry heat and photolytic degradation. The degradation studies indicated condition was well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for quantitative analysis of lacosamide in bulk drug and formulation.


Asunto(s)
Lacosamida , Cromatografía Líquida de Alta Presión/métodos , Preparaciones Farmacéuticas
4.
Indian J Pharmacol ; 55(6): 367-375, 2023.
Artículo en Inglés | MEDLINE | ID: mdl-38174533

RESUMEN

OBJECTIVE: Even though oxidative and inflammatory bursts are a big part of renal reperfusion injury (RI/R), Pistia stratiotes (PS) has been used for a long time to stop these overreactions. People have said that it can drop both blood sugar and cholesterol. Hence, the goal of this study was to show how PS changed kidney reperfusion damage in both diabetic and normal rats. MATERIALS AND METHODS: In the study, 30 min of renal ischemia (RI) was followed by 1 h of recovery for each rat. Before the test, PS (100 mg/kg p. o.) was given to the animals for 7 days. Then, using the mixture from the separated kidney tissues, the antioxidant, inflammation, and histopathological effects were determined. RESULTS: When compared to RI/R, diabetic rats given PS had lower blood sugar, aspartate aminotransferase, blood urea nitrogen, and creatinine, myeloperoxidase, C-reactive protein, and tumor necrosis factor-alpha levels in their urine. CONCLUSION: PS potentially worked in hyperglycemic rats protecting them against RI/R. It is possible that PS's ability to protect the kidneys of the test rats is due to its ability to fight free radicals, lower blood sugar, and stop inflammation.


Asunto(s)
Araceae , Diabetes Mellitus Experimental , Enfermedades Renales , Daño por Reperfusión , Humanos , Ratas , Animales , Diabetes Mellitus Experimental/complicaciones , Diabetes Mellitus Experimental/tratamiento farmacológico , Glucemia/metabolismo , Riñón , Enfermedades Renales/metabolismo , Daño por Reperfusión/tratamiento farmacológico , Daño por Reperfusión/prevención & control , Inflamación/metabolismo , Inflamación/patología , Estrés Oxidativo , Creatinina/metabolismo , Creatinina/farmacología
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