Background: Regardless of the availability of all novel and earlier treatments, seizure control is notoriously complicated. In the hopes of discovering the latest and ultimate therapy, medicinal chemists will keep on to hunt for new antiepileptic compounds with high specificity and low CNS toxicity. The biological effects of benzodiazepine compounds have been examined. Benzene and a diazepine ring are fused together to form the chemical structure. Diverse combinations of moieties attached to the innermost structure in positions 1, 2, 5, and 7 the pharmacological qualities, effect potency, and pharmacokinetic conditions are all influenced by the various side groups. Method: This paper describes the synthesis of several 1H-benzo[b][1,5]diazepin-2(3H)-one derivatives. The substituents at N1 are benzoyl, 5-substituted-1,3,4-thiadiazoles-2-yl-aminoacetyl. Condensation of orthophenylene diamine with ethyl acetoacetate gave 7-substituted-4-methyl-1H-benzo[b][1,5]diazepin-2(3H)-ones, which were then linked to benzoyl chloride and chloroacetyl chloride to yield N1-benzoyl and N1-chloroacetyl derivatives. N1- chloroacetyl derivatives were further linked with 5-substituted-1,3,4-thiadiazoles amines using microwave irradiation. Result: IR, 1H-NMR, and mass spectroscopy were used to authenticate the synthesized compounds. The PTZ produced convulsions method was used to test the compounds for anticonvulsant activity. Compounds 4a and 4c gave 80% protection at 0.4 mg/kg, whereas Compounds 2a and 2c offered 80% protection at 20 and 30 mg/kg, respectively, when compared to the Control. Conclusion: When compared to a control, the experimental synthesis and pharmacological assessment of the 1,5-benzodiazepin-2-one moiety replaced with 1,3,4-thiadiazole yields a potentially active anticonvulsant drug.
Quantum dots (QDs) are semiconducting nanoparticles having different optical and electrical properties when compared to larger particles. They exhibit photoluminescence when irradiated with ultraviolet light, which is due to the transition of an excited electron from the valence band to the conductance band followed by the return of the exciting electron back into the valence band. The size and material of QDs can affect their optical and other properties too. The QDs possess special attributes like high brightness, protection from photobleaching, photostability, color tunability, low toxicity, low production cost, a multiplexing limit, and a high surfaceto-volume proportion, which make them a promising tool for biomedical applications. Here, in this study, we summarize the utilization of QDs in different applications including bioimaging, diagnostics, immunostaining, single-cell analysis, drug delivery, and protein detection. Moreover, we discuss the advantages and challenges of using QDs in biomedical applications when compared with other conventional tools.
Herein, the synthesis of 3-(3-(substituted benzylidine)amino)phenyl-2-phenylquinazolin-4(3H)-ones from 3-aminophenyl-2-phenyl-quinazolin-4(3H)-ones is reported. The chemical structures of the synthesized compounds were confirmed by FT-IR, 1H NMR and 13C NMR studies. All compounds were evaluated for their anticonvulsant activity against maximal electroshock seizure method. The LD50 value was found to be 550 mg/Kg and the duration of tonic phase was reduced upto 1.1 s and that of stupor phase was reduced upto 70 s. The structure activity relationship of the compounds revealed that Schiff bases viz. 3-(3-benzylidineamino)phenyl-2-phenylquinazolin-4(3H)-one, 3-(3-(3- chlorobenzylidine)amino)phenyl-2-phenylquinazolin-4(3H)-one, 3-(3-(3- nitrobenzylidine)amino)phenyl-2-phenylquinazolin-4(3H)-one by significantly shorten the tonic and stupor phases of convulsions compared to controls, thus thereby these compounds demonstrated strong anticonvulsant potential.
According to the World Health Organization, the majority of people with epilepsy who live in developing countries do not have access to high-quality treatment. Modern anticonvulsants are in high demand since the unwanted effects of those compounds already in use make therapy difficult. The synthesis of derivatives of 5,5-disubstituted-N3-[(2-aryl thiazolidine-4-one-3-yl)amino]hydantoins has been reported. The position N3 of the hydantoin nucleus was substituted with 4-thiazolidinone moiety containing aryl substituent at 2nd position with the goal of achieving the enhanced anticonvulsant effect. Compounds 5c, 5d, 5l, 5r showed significant activity among the evaluated compounds compared to control at dose of 45 mg/kg. The analysis of structural features revealed that the substitution of p-hydroxy phenyl and cinnamyl substituted at 2nd position of thiazolidinone ring in 5,5-diphenyl-2,4- imidazolidinedione and p-chloro phenyl, p-methoxy phenyl substituted at 2nd position of thiazolidinone ring in (5,5-dialkyl)/(5-alkyl-5-substitutedphenyl)-2,4-imidazolidinedione skeleton enhanced the anticonvulsant potentiality of the synthesized compounds.
A sensitive and accurate high performance liquid chromatography method utilizing ultraviolet/visible light detection (HPLC-UV) for the quantification of Ribociclib in Spiked Human Plasma by HPLC-UV was developed and validated. Ribociclib (RCB) and the internal standard (IS), Trifluridine, were first extracted from plasma samples by a simple Protein Precipitation extraction using Acetonitrile. Plasma concentration of RCB and internal standard were then analyzed by applying reversed phase chromatography using Orochem orosil C18 (4.6 mm × 250 mm, 5 μ) and elution with a isocratic mobile phase consisting of 10 mM phosphate buffer – Acetonitrile (60:40, v/v) adjusted to pH 3.0 at a flow rate of 1.0 ml/min. Detection of RCB and the IS was subsequently done at a wavelength of 260 nm. The limit of quantification was 10 ng/ml. The calibration curve was linear (R2>0.998) over the concentration range of 10-1000 ng/ml. For human plasma, the accuracy and precision were within ±15% and ≤15%, respectively, for all concentrations, except for the lower limit of quantification, where they were within ≤20%.
Analytical methodologies are critical throughout the medicine development process, including marketing and post-marketing studies. The advancement of bio-analytical techniques has resulted in a dynamic field with many exciting potentials for further advancement in the future. Bio-analysis is commonly utilised in the pharmaceutical drug development of drug's and its metabolites' quantitative levels. The goal is to undertake pharmacokinetic and pharmacodynamic studies, as well as kinetics, toxicokinetics, bioequivalence, and exposure studies. Bioanalytical research employs a variety of bioanalytical techniques, including new instrumental techniques, separation techniques, and ligand-Indused test. This study emphasizes the importance of bio-analytical techniques and hyphenated devices in evaluating drug bio-analysis and the role of several current bio-analytical techniques such as LC-Mass, HPLC-PDA, UPLC-Mass spectroscopy, HPTLC, LC-Tandem, AAS, ICP-Mass.etc., and their recent modernization in drug analytical and bio-analysis investigations
Introduction: Hepato-renal toxicity is a devastating, non-communicable disease. Because of a lack of information on low-cost management to combat the disease, this study postulates the ameliorative effect of selected phytoconstituents against toxicity. Aim and Objective: The current study reveals an active phytoconstituent, α- Pinene, that has the ability to combat the degenerative effects of CCl4. Methodology: Carbon tetrachloride (CCl4) is an organic xenobiotic molecule as well as the most potent hepatotoxic agent used (1200 mg/kg body weight; i.p.) to induce hepato-renal toxicity in experimental rats. To determine in vivo hepato-renal toxicity, three different doses (0.05 ml/kg body weight, 0.1 ml/kg body weight, and 0.15 ml/kg body weight; intraperitoneally) were chosen. Vitamin C at the dose of 250 mg/kg/p.o. was used as a standard, due to its maximum ameliorative activity against oxidative damage in CCl4-induced hepato-renal toxicity in rats. For 7 days, the animals were pre-treated with α-pinene and Vitamin C. CCl4 was charged only on the 7th day. Result and Conclusion: The related biochemical tests were studied. CCl4 intoxication reduces mitochondrial membrane potential in liver and kidney cells, which accelerates excessive intracellular ROS production, but α-pinene pretreatment successfully restores it in both liver and kidney cells. Pretreatment with α-pinene and vitamin C for 7 days increased intracellular ameliorative capability in hepatic and renal cells significantly (p 0.01). In conclusion, α-pinene is capable of restoring antioxidant status by quenching intracellular ROS. As a result, α-pinene has the potential to provide hepatoprotective and nephroprotective effects against CCl4-induced toxicity in rats.
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