Effect of dialkyl- [2-(1-oxa-3,4,9-triaza-fluoren-2-yl-methoxy)ethyl] amines on biogenic amines: new potential antidepressants.

A thorough survey of the literature has revealed that indole derivatives have shown various central nervous system activities. This study aims to evaluate the antidepressant activity of the newly synthesized dialkyl- [2-(1-oxa-3,4,9-triaza-fluoren-2-yl-methoxy)ethyl] amines and their effect on biogenic amines. In this study, the synthesized compounds were assessed by in-vivo antidepressant models, by forced swim test and tail suspension test in mice and effect of synthesized compounds on biogenic amines in brain in a chronic unpredictable stress model. The test compounds have demonstrated significant (P < 0.05) reduced immobility duration in mice when compared with the control group animals. The reduced immobility displayed by mice indicates potential antidepressant activity. In this study, chronic unpredictable stress led to decreased monoamine levels in the cortex and hippocampus regions of the brain. With chronic administration of the investigated compounds there is an increased in monoamines in the brain, in the chronic unpredictable stress model. Decreased levels of monoamines induced by the chronic unpredictable stress induced model of depression, were normalized by treatment with the test compounds, which indicates potential antidepressant activity.

Synthesis of N4 donor macrocyclic Schiff base ligands and their Ru (II), Pd (II), Pt (II) metal complexes for biological studies and catalytic oxidation of didanosine in pharmaceuticals.

A series of tetraaza (N(4) donor) macrocyclic ligands (L(1)-L(4)) were derived from the condensation of o-phthalaldehyde (OPA) with some substituted aromatic amines/azide, and subsequently used to synthesize the metal complexes of Ru(II), Pd(II) and Pt(II). The structures of macrocyclic ligands and their metal complexes were characterized by elemental analyses, IR, (1)H &(13)C NMR, mass and electronic spectroscopy, thermal, magnetic and conductance measurements. Both the ligands and their complexes were screened for their antibacterial activities against Gram positive and Gram negative bacteria by MIC method. Besides, these macrocyclic complexes were investigated as catalysts in the oxidation of pharmaceutical drug didanosine. The oxidized products were further treated with sulphanilic acid to develop the colored products to determine by spectrophotometrically. The current oxidation method is an environmentally friendly, simple to set-up, requires short reaction time, produces high yields and does not require co-oxidant.

Iodine-catalyzed condensation of isatin with indoles: a facile synthesis of di(indolyl)indolin-2-ones and evaluation of their cytotoxicity.

Isatin reacts smoothly with indoles in the presence of a catalytic amount of molecular iodine under mild conditions to afford a novel class of di(indolyl)indolin-2-one derivatives in good yields. These molecules are found to possess a promising cytotoxicity against cancer cells only but not on normal cells.

Iodine-catalyzed conjugate addition of indoles onto en-1,4-dione: a novel synthesis of 3-(1-(1H-indol-3-yl)-2-oxo-2-phenylethyl)indolin-2-ones as antibacterial and antifungal agents.

Indole and its derivatives undergo smooth conjugate addition onto en-1,4-dione derived from isatin and acetophenone, in the presence of a catalytic amount of molecular iodine in acetonitrile under mild conditions to afford a novel class of 3-(1-(1H-indol-3-yl)-2-oxo-2-phenylethyl)indolin-2-one derivatives in good yields with high degree of 1,4-selectivity. Some of these compounds are found to exhibit modest antibacterial and antifungal properties.

Effect of pomegranate pretreatment on the oral bioavailability of buspirone in male albino rabbits.

UNLABELLED: BACK GROUND AND THE PURPOSE OF STUDY: Many drug substances and variety of naturally occurring dietary or herbal components are capable of interaction with the CYP enzyme system. The aim of the study was to investigate the effect of pomegranate juice pretreatment on the bioavailability of buspirone in rabbits. METHODS: White New Zealand rabbits weighing 2.1±0.13 Kg were selected for study. The bioavailability of buspirone after pre-treatment with pomegranate juice (10 ml Kg(-1) for seven days) was compared with an oral solution of 10 mg kg(-1) of buspirone in distilled water. Animals were allowed free access to food and water, until night prior to dosing and were fasted for 10 hrs. In the first phase oral solution (10 mg kg(-1)) was administered through feeding tube followed by rinsing with 10 ml of water. In the second phase, the group was pretreated with pomegranate juice for 7 days and study was conducted after 15 days of washout period. RESULTS AND CONCLUSION: The results showed that there was a significant (p<0.05) difference in the bioavailability of buspirone after pre-treatment with pomegranate juice.This increase in bioavailability might be due to inhibition of CYP3A4. Further studies are required to prove this mechanism in humans.

Synthesis and anti-inflammatory activity of 2-substituted-((N, N-disubstituted)-1, 3-benzoxazole)-5-carboxamides.

A series of 2-substituted-((N, N-disubstituted)-1, 3-benzoxazole)-5-carboxamides derivatives were synthesized by the reaction of 2-substituted-5-carbomethoxy benzoxazole with different secondary amines. The newly synthesized compounds were characterized on the basis of spectral (FT-IR, 1H NMR, MS) & elemental analysis. All these compounds were screened for anti-inflammatory activity using carrageenan induced rat paw edema method. All of these compounds exhibited significant activity. Among the tested compounds Ve, Vg, Vf and Va were considered to have potent anti-inflammatory activity and was comparable with standard.

Binuclear cobalt(II), nickel(II), copper(II) and palladium(II) complexes of a new Schiff-base as ligand: synthesis, structural characterization, and antibacterial activity.

A binucleating new Schiff-base ligand with a phenylene spacer, afforded by the condensation of glycyl-glycine and o-phthalaldehyde has been served as an octadentate N4O4 ligand in designing some binuclear complexes of cobalt(II), nickel(II), copper(II), and palladium(II). The binding manner of the ligand to the metal and the composition and geometry of the metal complexes were examined by elemental analysis, conductivity measurements, magnetic moments, IR, ¹H, ¹³C NMR, ESR and electronic spectroscopies, and TGA measurements. There are two different coordination/chelation environments present around two metal centers of each binuclear complex. The composition of the complexes in the coordination sphere was found to be [M2(L)(H(2)O)4] (where M=Co(II) and Ni(II)) and [M2(L)] (where M=Cu(II) and Pd(II)). In the case of Cu(II) complexes, ESR spectra provided further information to confirm the binuclear structure and the presence of magnetic interactions. All the above metal complexes have shown moderate to good antibacterial activity against Gram-positive and Gram-negative bacteria.

Substituted tertiary phosphine Ru(II) organometallics: catalytic utility on the hydrolysis of etofibrate in pharmaceuticals.

Some new organometallics of ruthenium(II) of the type [RuCl2(COD)(CO)L] (1a-f) and [RuCl2(COD)L2] (2a-f) (where L is substituted tertiary phosphines), have been synthesized by using precursors [RuCl2(COD)(CO)(CH3CN)] (1) and [RuCl2(COD)(CH3CN)2] (2) with the substituted tertiary phosphine ligands in 1:1 and 1:2 molar ratio. The organometallics (2a-f) have been further reacted with carbonmonoxide to produce compounds of the type [RuCl2(CO)L2] (3a-f). These compounds were characterized by elemental analysis, IR, NMR (1H, 13C and 31P), mass and electronic spectral data. The catalytic activity of all these organometallics were studied and found that they are efficient catalysts for hydrolysis of etofibrate. The hydrolyzed product was separated by column chromatography and the percent yields are found in the range of 98.6-99.1%.

A short, stereoselective, and common approach for the synthesis of 4,5-disubstituted delta-lactones simplactone B and its C-5 analogue.

A short, stereoselective, and a common approach for the synthesis of 4,5-disubstituted delta-lactones simplactone B and its analogue using Evans protocol is described.

Design, synthesis and cytotoxic studies on the simplified oxy analog of eleutherobin.

A straight forward entry into nine membered B ring of eleutherobin as oxy analog and its cyctotoxic properties on HBL cell lines is described. Molecular modeling studies were carried out to ascertain the binding of the model compound to the active site of beta-tubulin.

Synthesis of new 2-substituted-[1,3,4]-oxadiazino-[6,5-b]-indoles with H1-antihistaminic, antimuscarinic and antimicrobial activity [corrected].

New 2-substituted-[1,3,4]-oxadiazino-[5,6-b]-indoles have been prepared and tested for their antibacterial, antifungal, H1-antihistaminic and antimuscarinic activities. Among them, compounds 5b, 5d, 5k exhibited higher H1-antihistaminic activity than pheniramine maleate. Compounds 5c, 5d showed higher antibacterial activity than ampicillin against Staphylococcus aureus and E. coli, respectively.