Posted by admin on Jan 31, 2021 in |
The present research work involves the use of exclusively and commercially available indole-3-carbaldehyde as a starting material to synthesize novel pyrimidine analogues. The synthesis of series of indole and pyrimidine containing N-substituted-4-(1H-indol-3-yl)-6-methyl-2-oxo-1, 2, 3, 4-tetrahydro-pyrimidine-5-carbohydrazide U(1-10) has been done by using principle of Biginelli condensation reaction.Indole-3-carbaldehyde was prepared by formylation of indole (Vilsmeier Haack reaction) using dimethylformamide and phosphorus oxychloride (1). The intermediate indole dihydropyrimidines was synthesized from a mixture of indole-3-carbaldehyde, urea and ethyl acetoacetate in the presence of zinc chloride as acid catalyst (2). The intermediate compound then refluxed with hydrazine hydrate by the addition of catalytic amount of conc. sulphuric acid, led to formation of parent compound 4-(1H-indol-3-yl)-6-methyl-2-oxo-1, 2, 3, 4-tetrahydropyrimidine-5-carbohydrazide(3). The parent compound 3 was used for synthesis of N’-substituted-4-(1H-indol-3-yl)-6-methyl-2-oxo- 1, 2, 3, 4-tetrahydropyrimidine-5-carbohydrazide and substituted aldehydes U (1-10), and/or Schiff bases of N’-substituted-4-(1H-indol- 3- yl)- 6- methyl- 2- oxo- 1, 2, 3, 4-tetrahydropyrimidine-5-carbohydrazide. Elemental analysis, FT-IR, 1H-NMR, and Mass spectral data supports the structures of synthesized compounds. The selected synthesized compounds were screened for...
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Posted by admin on Jan 31, 2021 in |
Dengue is a fatal disease connected to the environment that spreads rapidly. As there is currently no effective vaccine against dengue and no exact treatment for the disease, controlling and preventing dengue fever outbreaks are essential steps for keeping people healthy. Dengue viruses are a member of the Flaviviridae family, mosquito-borne, and causative agents for dengue fever. Bioactive compounds obtained from natural products, including medicinal plants, are a potentially good target to control infections. Thus the current study was designed to find potential phytochemical inhibitors against the Dengue virus NS2B/NS3 protease, which can inhibit the viral replication and control the dengue vector Aedes aegypti. Larvicidal, functional group analysis (FTIR), and molecular docking studies results revealed that the bioactive compounds from the medicinal plant flower extract Cassia auriculata showed high inhibitory activity against the dengue protease enzyme NS2B-NS3 and Aedes aegypti vector. Out of fifteen compounds identified from GCMS, five compounds showed high inhibitory activity against the protease 2FOM in the docking analysis. The main antiviral approach of plant compounds...
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Posted by admin on Jan 31, 2021 in |
Hydroxychloroquine, widely used to treat certain autoimmune diseases and inflammatory conditions, has been repositioned as a new lead against the COVID-19 pandemic. Preliminary studies have suggested that hydroxychloroquine inhibits the entry of the SARS-CoV2 virus mediated by the ACE2 receptor and is a particularly interesting anti-inflammatory and immunomodulatory action in the cytokine storm during COVID-19 infection. Furthermore, cardiovascular effects have been reported in hypertensive patients. These last are thought to result from the inhibition of cyclooxygenase 2. Our results reveal for the first time in atomic detail how hydroxychloroquine, one of the most controversial drugs, has an affinity for a new molecular target (COX2) with a docking score: -7.6 (kcal/mol) and a root mean square deviation (RMSD = 2.542). Hydroxychloroquine binds to cyclo-oxygenase 2 via two hydrogen bonds (H-GLY136 and H-GLY45) and four hydrophobic bonds: Cl -CYS36, 0 -CYS36, 0 -CYS47 and 0 -PRO154). This mechanism has never been elucidated. Hydroxychloroquine proved to be promiscuous. Its structure, which differs from that of non-steroidal anti-inflammatory drugs , tends to show...
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Posted by admin on Jan 31, 2021 in |
Dengue is the most rapidly spreading mosquito-borne viral disease in the world. Patients with dengue fever are treated symptomatically. There is no specific allopathic treatment for dengue fever. Traditional medicinal plants have been reported to be useful in the treatment of dengue fever. The development of new anti-dengue products from bioactive compounds is necessary to find an effective treatment for dengue. The present work aims at formulation development and evaluation of herbal IR tablets with faster disintegration and good mechanical strength for the treatment of Dengue. Tablets are stable solid dosage forms and are favorable for formulation derived from herbal extracts. The Carica papaya Linn and Boswellia serrata having anti-thrombocytopenic effect, anti-viral and antipyretic effect were used for the development of the nutraceutical tablet. Simple direct compression method was used for the formulation of an immediate release tablet. The effect of various superdisintegrant and diluents was explored. The compressed formulations were evaluated on various pre-compression and post-compression parameters. The tablets were coated with hydroxyl propyl methylcellulose (HPMC) 5 cps...
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Posted by admin on Jan 31, 2021 in |
Background: Sesuvium portulacastrum L. and Excoecaria agallocha (L.) are two important medicinal plants inhabited in mangrove regions. Early researches focused on antimicrobial activity of leaves of concerned plants with various solvents among which ethanol, chloroform, and methanol were the best Objective: In the present study the extracts of two therapeutic plants were researched to measure the activity against 2 Gram-positive bacteria, 2 Gram-negative bacteria and 3 fungal strains. Materials and Methods: Hexane, Ethyl acetate, and Methanol were utilized for extraction. Bacterial Strains Staphylococcus aureus, Streptococcus pyogenes, Escherichia coli, Pseudomonas aeruginosa, and fungal strains Aspergillus niger, Aspergillus flavus, Aspergillus fumigatus were used to test the antimicrobial activity. Results: The activity increased in dose dependent manner thus hexane concentrate of Sesuvium portulacastrum display most noteworthy action against P.aeruginosa and E. coliand Aspergillus flavus demonstrated maximum. Excoecaria agallocha show the highest zone against S. aureus, and P. aeruginosa demonstrated the least movement. Hexane was demonstrated best dissolvable for Sesuvium portulacastrum and Excoecaria agallocha. Ethyl acetate was finest for the fungal activity of...
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