QSAR Investigation on 3,5-diaryl-4,5-dihydro-1H-pyrazole-1-carbothioamides as EGFR Kinase Inhibitors
In order to establish a quantitative relationship between epidermal growth factor receptor (EGFR) kinase inhibitory activity and physicochemical / structural properties, a quantitative structure activity relationship (QSAR) study was performed on a series of 3,5-diaryl-4,5-dihydro-1H-pyrazole-1-carbothioamides. Using multiple linear regression (MLR) analysis, many statistical regression equations were developed. Model 2...
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Study on Synthesis and Appraisal of Some 2,5-Disubstituted-1,3,4-Thiadiazoles as Diuretic Agents
Acetazolamide and Methazolamide are diuretic 1,3,4-thiadiazole compounds that are well-known. As a result, certain novel 2,5-disubstituted-1,3,4-thiadiazoles were synthesised and diuretic efficacy was tested. The diuretic action of a handful of the compounds, including IVa1, IVb2, and IVc2, was comparable to that of the conventional medication acetazolamide. The Osiris property...
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Study on 1, 3, 4-Oxadiazole Derivatives as an Antibacterial and Antifungal Agents
A new series of 1, 3, 4-oxadiazoles (3a-j) was synthesised in this study by reacting INH (1) with substituted aromatic acids (2) in the presence of POCl3. IR, 1H NMR, and mass spectrum data were used to identify the novel compounds. In-vitro antibacterial and antifungal properties were tested on...
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Determining the Effect of 1, 3, 5-trimethyl-2, 6-diphenyl Piperidin-4-one Oxime on the Electrochemical Behaviour of Mild Steel in HCl Medium
The corrosion inhibitory capacity of a synthetic heterocyclic molecule, namely 1, 3, 5-trimethyl-2, 6-diphenyl piperidin-4-one oxime, was evaluated using weight loss experiments, electrochemical methods, and SEM examinations in 1M hydrochloric acid (HCl) media against mild steel (MS) (TPO). The weight loss studies were conducted at three different temperatures for...
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Study on Synthesis and Characterization of New 8- Trifluloromethyl Quinazolin-2,4-(3H)-Dione Nucleosides
The synthesis of 8-trifluloromethyl quinazolin-2,4-(1H,3H)-dione 2, which was ribosylated by coupling with 1-O-acetyl-2,3,5-tri-O-benzoyl—D-ribofuranose 4 via the silylation method, yielded mixture and -anomeric benzoylated nucleoside derivatives 5 and 6, respectively. As part of our ongoing interest in the synthesis of new nucleosides with expected biological activity, quinazolin-2,4-(3H)-dione nucleosides containing trifluloromethyl...
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Isolation, Characterizations of Bioactive Principles from Melia dubia Leaf and Its In-silico and In-vitro Urolithiatic Activity
Many medicinal plants contain a wide range of bioactive compounds at various levels. The primary goal of this research is to identify and separate antioxidants from different extracts of Melia dubia leaves. Soxhlet extraction was used with solvents such as hexane, chloroform, ethyl acetate, methanol, water, and 70% ethanol....
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5-[Substituted]-1, 3, 4-thiadiazol-2-amines: Synthesis, Spectral Characterization, and Evaluation of their DNA Interactions
One of the most important aspects of the manufacture of medicinal drugs is the synthesis of novel thiadiazoles. Current medicinal chemistry research has focused on the properties of new compounds with possible novel structural features and biological applications. In this context, the synthesis and characterization of 5-[substituted]-1, 3, 4-thiadiazol-2-amines...
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Recent Study on Synthesis of Novel Series of Quinolino [3,2-f][1,2,4] triazolo [3,4-b][1,3,4] Thiadiazepines Derivatives Incorporated with 3-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl) Moiety as Potent Antimicrobial Agent
A Quinolino novel series[3,2-f] [1,2,4] The [3,4-b] Triazolo [1,3,4] The Thiadiazepine (7a-i) derivatives incorporated with 3-(5–i) (benzofuran-2-yl) -1-phenyl-1H-3-yl pyrazol) Moiety was synthesised by a 5-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)) one-point cyclo-condensation reaction. -4-amino-4H-1,2,4-triazole-3-thiol (4) in the presence of K2CO3 in DMF with 2-chloro-quinoline-3-carbaldehyde derivatives (6a-i). Characterization of 3-(5-(benzofuran-2-yl)-1-phenyl-1H-pyrazol-3-yl)-substituted quinolino [3,2-f] newly synthesised compounds...
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Synthesis and Structural Features of Indanone, Tetralone and Naphthone Derivatives: Selective Fluorination and Condensation Products
The present study seeks to investigate the synthesis and structural characteristics of derivatives of Indanone, Tetralone and Naphthone. Via Claisen condensations, arylhydrazine condensations, BakerVenkataraman rearrangements, Claisen-Schmidt reactions, selective fluorinations and trifluoroacetylations in yields ranging from 22-92 percent, indanone, tetralone and naphthone derivatives and fused-ring heterocycles were prepared. Regiochemistry and...
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Synthesis of Azido Derivatives of Mucobromic Acid: Critical Study
Mucobromic acid is a highly reactive multicentered molecule. It was converted to its corresponding but unstable diazido derivative by reaction with two equivalents of sodium azide. The resultant 3,4- diazido-5-hydroxyfuran-2(5H)-one was obtained in moderate yield (42%) but decomposed readily even at low temperatures. Its more stable analogue 3,4-diazido-5-methoxyfuran-2(5H)-one was...
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