[Show abstract][Hide abstract] ABSTRACT: The methanolic extract of the Citrus sinensis peel was screened for antidiarrhoeal activity using animal models against castor oil induced diarrhoea. The parameters evaluated are small intestine secretion by enteropooling assay, rate of defecation and small intestine transit. The methanolic extract showed significant activity (p<0.05) against castor oil induced diarrhoea and interluminal accumulation of fluid. It also reduced gastrointestinal motility after charcoal meal administration in albino mice. The results indicates that the action of Citrus sinensis peel extract (CSPE) could be through a combination of inhibition of elevated prostaglandin biosynthesis and reduced propulsive movement of the small intestine.
[Show abstract][Hide abstract] ABSTRACT: Hypercholesterolemia, or high cholesterol, occurs when there is too much cholesterol in the body. Cholesterol is a soft, waxy, fat-like substance that is a natural component of all the cells of the body. Molecular docking is used to predict the binding orientation of small molecule drug candidates to their protein targets in order to in turn predict the affinity and activity of the small molecule. Hence docking plays an important role in the rational design of drugs. The present study is deals with the molecular docking of derivatives of 2α-hydroxyursolic acid which is the active component of the plant Banaba leaves (Lagerstroemia speciosa L. Pers, Lythraceae) against HMG CoA reducatse involved in cholesterol biosynthesis using AutoDock software. The protein file of HMG CoA reductase [PDB ID: 1DQ8] was taken from the protein data bank. The lead moiety 2α-hydroxyursolic acid has shown best ligand binding energy -5.32kcal/mol. All the derivatives have shown best ligand binding energy between–2.82 kcal/mol to -12.52kcal/mol. Out of the nine derivatives 1I show best ligand binding energy as -12.52 kcal/mol.
Full-text · Article · Jul 2011 · International Journal of PharmTech Research
[Show abstract][Hide abstract] ABSTRACT: A simple and general method has been developed for the synthesis of various 3,4-dihydro quinazolinone derivatives by the treatment of an aldehydes with excess equivalent of urea in ethanol affords Arylideno-bis-ureas 1 which on condensation with p-amino benzoic acid in acidic medium cyclised to 4-aryl-6-hydroxy-2-oxo-3,4-dihydroquinazolines 2. Reaction of 2 with benzoylchloride in 10% NaOH results in 1-benzoyl 4-aryl-6-hydroxy-2-oxo-3,4-dihydroquinazolin-2(H)-one 3. The structures of the compounds were characterized by elemental analysis, IR, 1H-NMR and 13C-NMR spectra. Compounds 3 have been evaluated for their analgesic and antibacterial activity.
[Show abstract][Hide abstract] ABSTRACT: A series of substituted pyridinyl 1, 3, 4 oxadiazole derivatives were synthesized from Schiff bases of
nicotinic acid derivatives through chlorination followed by reaction with hydrazine hydrate and with the use
various aldehydes. The synthesized compounds were characterized by elemental analysis,H NMR and Mass
Spectra. All the compounds were screened for in vitro antioxidant activity by DPPH and Nitric oxide scavenging assay. Compounds substituted with electron donating groups like methoxy and hydroxyl showed higher antioxidant activity.
Full-text · Article · Oct 2010 · Research Journal of Pharmaceutical, Biological and Chemical Sciences
[Show abstract][Hide abstract] ABSTRACT: Some novel Mannich base isatin derivatives were synthesized by reacting 1-(5-methyl-2-oxoindolin-3-ylidene)-4-(substitutedpyridin-2-yl)thiosemicarbazide with formaldehyde and several secondary amines. Their chemical structure was elucidated by means of spectral (FT-IR, (1)H- and (13)C-NMR and mass) analysis. Investigation of anti-inflammatory activity of synthesized compounds was done by carrageenan induced paw oedema method using diclofenac sodium as standard drug and analgesic activity was done by acetic acid induced writhing method. The synthesized compounds showed significant anti-inflammatory and analgesic activity.
[Show abstract][Hide abstract] ABSTRACT: Some novel mannich base isatin derivatives were synthe-sized by reacting 1-(5-chloro-2-oxoindolin-3-ylidene)-4-(pyridine-2-yl)thiosemicarbazide with formaldehyde and several secondary amines. Their chemical structures were elucidated by means of spectral (FT-IR, 1 H NMR and mass) analysis. Investigation of in vitro antibacterial and antifungal activity of synthesized compounds was done by disc diffusion method against B. subtilis, S. aureus, E. coli, P. aeruginosa, C. albicans and A. niger. All the synthesized compounds were screened for anticonvulsant activity by MES method using phenytoin as standard drug. All the compound exhibited moderate to good antibacterial and antifungal activity. All the compounds of the series exhibited significant anticonvulsant activity at 100 mg/kg dose level.
[Show abstract][Hide abstract] ABSTRACT: A series of 1-(5-substituted-2-oxoindolin-3-ylidene)-4-(substituted-pyridin-2-yl)thio semicarbazide derivatives were synthesized by the reaction of 4-(substituted-pyridin-2-yl) thiosemicarbazide and 5-halogenated isatin derivatives. The newly synthesized compounds were characterized on the basis of spectral (FT-IR, 1 H, 13 C NMR and mass) analysis. Investigation of in vitro anti-bacterial and anti-fungal activity of synthesized compounds was done by disc diffusion method against B. subtilis, S. aureus, E. coli, P. aeruginosa, C. albicans, and A. niger. All the compounds exhibited moderate to good anti-bacterial and anti-fungal activity.