Depression is a complicated neuropsychiatric condition with an incompletely understoodetiology, making the discovery of effective therapies challenging. Animal models have been crucial in improving our understanding of depression and enabling antidepressant medication development. The CUMS model has significant face validity since it induces fundamental depression symptoms in humans, such as anhedonia, behavioral despair, anxiety, cognitive impairments, and changes in sleep, food, and social behavior.
View Article and Find Full Text PDFGlipizide; an insulin secretagogue belonging to the sulfonylurea class, is a widely used antidiabetic drug for managing type 2 diabetes. However, the need for life-long administration and repeated doses poses challenges in maintaining optimal blood glucose levels. In this regard, orally active sustained-release nano-formulations can be a better alternative to traditional antidiabetic formulations.
View Article and Find Full Text PDFJ Diabetes Metab Disord
December 2023
Purpose: The present study was designed to determine the effect of levofloxacin (LVX) treatment on the blood glucose level, insulin sensitivity, anxiety level, nitrite and MDA level of STZ induced diabetic rats.
Methods: Wistar rats were used in the present study. The rats were made diabetic by the administration of single dose of STZ (45 mg/kg, i.
Mini Rev Med Chem
January 2023
Heterocyclic compounds have diverse structure, which makes them broad and economical therapeutic agents. Pyrazole is a five-membered aromatic ring that contains two nitrogen atom and is responsible for the diverse functions of heterocyclic compounds. This implies the need of reviewing the work that already has been done on the potential of pyrazole scaffolds in the field of medicinal chemistry for the synthesis of new compounds with more effective antimicrobial, antioxidant, anticancer, anti-tuberculosis, and anti-inflammatory activities.
View Article and Find Full Text PDFA rising number of researchers are interested in thiophene-based analogs as they have wide possibilities of biological potential in the largely developing chemical world of the heterocyclic moiety. It also occupies a central position in synthetic organic chemistry and is of the highest theoretical and practical importance. It became an important moiety for researchers to discover combinatorial libraries and implement the efforts in search of the lead entity.
View Article and Find Full Text PDFBackground: Traumatic brain injury (TBI) is a worldwide problem. Almost about sixtynine million people sustain TBI each year all over the world. Repetitive TBI linked with increased risk of neurodegenerative disorder such as Parkinson, Alzheimer, traumatic encephalopathy.
View Article and Find Full Text PDFMini Rev Med Chem
August 2023
Flavonoids are compounds abundantly found in nature and known as a polyphenolic group of compounds having flavancore and show the utmost abundant collection of complexes and are found in fiber-rich root vegetables, fruits, and their eatable items. Due to the presence of hydroxyl groups, flavonoids show various therapeutic activities like antioxidant, antibacterial, antiviral, and antiinflammatory. Substituent groups are responsible for the onset of biochemical actions of flavonoids, which affect the metabolism.
View Article and Find Full Text PDFImidazole is a five-membered heterocyclic moiety that possesses three carbon, two nitrogen, four hydrogen atoms, and two double bonds. It is also known as 1, 3-diazole. It contains two nitrogen atoms, in which one nitrogen bear a hydrogen atom, and the other is called pyrrole type nitrogen.
View Article and Find Full Text PDFAs we know that, Oxadiazole or furadi azole ring containing derivatives are an important class of heterocyclic compounds. A heterocyclic five-membered ring that possesses two carbons, one oxygen atom, two nitrogen atoms, and two double bonds is known as oxadiazole. They are derived from furan by the replacement of two methylene groups (= CH) with two nitrogen (-N =) atoms.
View Article and Find Full Text PDFObjectives: The aim of the present study was to develop nanotechnology-based oral formulations of glipizide to enhance the bioavailability and eliminate the frequent oral administration of the conventional dosage form. Glipizide is an antidiabetic drug with a short biological half-life and limited oral bioavailability. Novel palmitic acid-pluronic F127-palmitic acid (PA-F127) pentablock copolymer-based prolonged release glipizide nanoparticles (GNs) were prepared and screened for and studies.
View Article and Find Full Text PDFBackground: A new series of thiophene analogues was synthesized and checked for their in vitro antibacterial, antifungal, antioxidant, anticorrosion and anticancer activities.
Results: A series of ethyl-2-(substituted benzylideneamino)-4,5,6,7-tetrahydrobenzo[]thiophene-3-carboxylate derivatives were synthesized by using Gewald synthesis and their structures were confirmed by FTIR, MS and H-NMR. The synthesized compounds were further evaluated for their in vitro biological potentials i.
Thiophene and its substituted derivatives are very important class of heterocyclic compounds which shows interesting applications in the field of medicinal chemistry. It has made an indispensable anchor for medicinal chemists to produce combinatorial library and carry out exhaustive efforts in the search of lead molecules. It has been reported to possess a wide range of therapeutic properties with diverse applications in medicinal chemistry and material science, attracting great interest in industry as well as academia.
View Article and Find Full Text PDFBackground: Thiazolidinedione is a pentacyclic moiety having five membered unsaturated ring system composed with carbon, oxygen, nitrogen and sulfur molecules at 1 and 3 position of the thiazole ring and widely found throughout nature in various form. They favourably alter concentration of the hormones secreted by adipocytes, particularly adiponectin. They also increase total body fat and have mixed effects on circulating lipids.
View Article and Find Full Text PDFRecent Pat Drug Deliv Formul
July 2020
Gold nanoparticles possess unique mechanical, chemical, photo-optical and biological properties and have been an interesting field of research on life sciences. The research studies produced new nanodevices and nanotechnology-based biosensing, diagnostics therapeutics, and targeted drug delivery systems. In this review, the unique potential aspects of gold nanoparticles/ nanoformulations/ or devices related to diabetes management have been discussed together with the recent patent on the gold nanoparticles developed for diabetes management.
View Article and Find Full Text PDFChem Cent J
December 2017
Thiazolidinediones are sulfur containing pentacyclic compounds that are widely found throughout nature in various forms. Thiazolidinedione nucleus is present in numerous biological compounds, e.g.
View Article and Find Full Text PDFBackground: Pyrimidine is an aromatic heterocyclic moiety containing nitrogen atom at 1st and 3rd positions and play an important role to forms the central core for different necessity of biological active compounds, from this facts, we have designed and synthesized a new class of pyrimidin-2-ol/thiol/amine derivatives and screened for its in vitro antimicrobial activity.
Results And Discussion: The synthesized pyrimidine derivatives were confirmed by IR, H/C-NMR, Mass spectral studies and evaluated for their in vitro antimicrobial potential against Gram positive (S. aureus and B.
Background: A novel series of 5-(substituted aldehyde)-7-methyl-3-oxo--phenyl-2-((3,4,5,6-tetrahydroxytetrahydro-2-pyran-2-yl)methylene)-1,2,3,5-tetrahydroimidazo[1,2-]pyrimidine-6-carboxamide analogues (-) was synthesized using the Biginelli condensation.
Results And Discussion: The synthesized compounds were screened for their in vitro antimicrobial potential against Gram (positive and negative) bacterial and fungal strains by tube dilution technique. In the series, compound exhibited significant antimicrobial activity against and with MIC value = 1.
The unequivocal hypotheses about anticonvulsant activity of valproic acid (VPA) have always been a basic hurdle in designing next generation neurotherapeutics, particularly the anti-epileptic drugs. The present study reports about a comprehensive in-silico investigation into qualitative and quantitative binding of VPA and corresponding natural ligands of four major enzymes involved in neurotransmissions, namely-GABA transaminase (GABAt), α-keto glutarate dehydrogenase (α-KGDH), Succinate Semialdehyde dehydrogenase (SSADH) and Glutamate Decarboxylase (GAD), respectively. The molecular docking analyses revealed that VPA inhibits GABAt and α-KGDH through allosteric while SSADH through competitive mode of binding.
View Article and Find Full Text PDFBackground: A rapid and sensitive ultraviolet-visible (UV-VIS) spectroscopic method was developed for the estimation of pyrimidine derivative 6-Bromo-3-(6-(2,6-dichlorophenyl)-2-(morpolinomethylamino) pyrimidine4-yl) -2H-chromen-2-one (BT10M) in bulk form.
Results: Pyrimidine derivative was monitored at 275 nm with UV detection, and there is no interference of diluents at 275 nm. The method was found to be linear in the range of 50 to 150 μg/ml.
Background: A series of 6-(substituted aldehyde)-3,4-dihydro-1-(tetrahydro-3,4-dihydroxy-5-(hydroxymethyl) furan-2-yl)-4-phenylpyrimidine-2(1H)-one derivative (6A-6P) was synthesized from the 6-(substituted aldehyde)-4-phenylpyrimidine-2(1H)-one derivative (5A-5P) through following reaction mechanisms Claisen-Schmidt, Cyclization, and Satos fusion. The structures of the synthesized compounds were elucidated by I.R.
View Article and Find Full Text PDFCent Nerv Syst Agents Med Chem
December 2015
From last few years research work on heterocyclic compound and their derivatives has been increasing. Benzothiazole molecule has a heterocyclic structure, basic in nature with wide variety of active sites. As a small molecule, it contains electronegative atoms due to which it is feasible for other moieties to form conjugates.
View Article and Find Full Text PDFA rapid resolution high performance thin layer chromatography (HPTLC) method has been developed and validated for estimation of olmesartan medoxomil in tablet formulations. This paper describes accurate, precise, specific and reproducible method and its degradation products, related impurities for assessment of purity of bulk drug and stability of its tablet formulations. The method involve silica gel 60 F254 high performance thin layer chromatography and densitometric detection at 264 nm using toluene - acetonitrile- methanol - ethyl acetate - acetic acid (5:3.
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