Discovery of isoalloxazine derivatives as a new class of potential anti-Alzheimer agents and their synthesis.

This article describes discovery of a novel and new class of cholinesterase inhibitors as potential therapeutics for Alzheimer's disease. A series of novel isoalloxazine derivatives were synthesized and biologically evaluated for their potential inhibitory outcome for both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). These compounds exhibited high activity against both the enzymes AChE as well as BuChE.

Blue excitable green emitting Ce(3+) doped CaS phosphor for w-LEDs.

CaS:Ce(3+) is an efficient green-emitting (535 nm) phosphor, excitable with blue light (450-470 nm) and was synthesized via a solid-state reaction method by heating under a reducing atmosphere. The luminescent properties, photoluminescent (PL) excitation and emission of the phosphor were analyzed by spectrofluorophotometry. The excitation and emission peaks of the CaS:Ce(3+) phosphor lay in the visible region, which made them relevant for light-emitting diode (LED) application for the generation of white light.

Crystal structure of [1-(3-chloro-phen-yl)-5-hy-droxy-3-methyl-1H-pyrazol-4-yl](p-tol-yl)methanone.

In the title compound C18H15ClN2O2, the dihedral angles between the central pyrazole ring and the pendant chloro-benzene and p-tolyl rings are 17.68 (10) and 51.26 (12)°, respectively.

Steric considerations on improving the diastereomeric ratio of (+)- and (-)-neomenthyl phenyl sulfoxides using bulky-headed oxidant hexadecyltrimethylammonium periodate and assignment of their configuration.

The bulky-headed oxidant hexadecyltrimethylammonium periodate affords the diastereomeric pairs, (Ss)-(+)/(Rs)-(+) and (Ss)-(-)/(Rs)-(-)-neomenthyl phenyl sulfoxides in stereochemically pure states with improved diastereomeric excess (48% diastereomeric excess [de]) as compared to its nonbulky counterpart, sodium metaperiodate (28% de) from respective (+)/(-)-neomenthyl phenyl sulfides. Steric effects involving the head group volume of hexadecyltrimethylammonium periodate is found to play a role in improving the diastereomeric ratio of the products. The two diastereomers can be readily separated by column chromatography.

Synthesis and Biological Studies of a Novel CB1 Antagonist.

This paper describes the synthesis, early process development, salt selection strategies and pre clinical evaluation of novel, potent and selective CB1 antagonist, 8-Chloro-1-(2,4-dichloro-phenyl)-4,5-dihydro-1H-6-oxa-1,2-diaza-benzo[e]azulene-3-carboxylic acid piperidin-1-ylamide 1. The CB1 antagonism of compound 1 is also confirmed by reversal of CB1 agonist-induced hypothermia in Swiss albino mice. The process for the preparation of the compound 1 as a crystalline solid is also described.

Role of 5-HT2 receptors in diabetes: Swertiamarin seco-iridoid glycoside might be a possible 5-HT2 receptor modulator.

In the present review, we are focusing on modulators of 5-HT2 receptors, swertiamarin and their role in diabetes. These drugs possess both central and peripheral actions in various animal models of depression, diabetes and obesity. Swertiamarin and 5-HT2 antagonist are reported antidepressant, hypolipidemic and beneficial in peripheral vasculopathy.

Adsorption of chromium from aqueous solutions using crosslinked chitosan-diethylenetriaminepentaacetic acid.

Chitosan (CH) and its derivatives have been the focus of attention for researchers as potential adsorbents for heavy metal removal. The adsorption potential of chitosan cross-linked with diethylenetriaminepentaacetic acid (CD) for Cr6+ was investigated. CD was characterized by FTIR, XRD, TGA, XPS and ESR techniques.

Chitosan, nanoclay and chitosan-nanoclay composite as adsorbents for Rhodamine-6G and the resulting optical properties.

The objective of this study was to investigate the use of chitosan-clay nanocomposite (CC) as an adsorbent for Rhodamine 6G (Rh-6G). The effects of adsorbent dose, contact time, and concentration on the adsorption process were systematically studied. Isotherm models were applied to the experimental equilibrium data obtained from spectrophotometric measurements of dye adsorption.

Characterization of an adhesive molecule from Bacillus megaterium ADE-0-1.

An adhesive exopolysaccharide (EPS), from a biofilm forming marine strain ADE-0-1, identified as Bacillus megaterium using conventional microbiological test and 16S rDNA analysis, contained 75% carbohydrate, 17% uronic acid and 0.00125% pyruvate on dry weight basis as per colorimetric determinations and found anionic in nature by ion exchange chromatography. Paper chromatographic and HPLC analysis of EPS hydrolysate indicated presence of arabinose, glucose, mannose, galacturonic acid and glucuronic acid.

Antioxidant activities and phenolics profiling of different parts of Carica papaya by LCMS-MS.

This article deals with the comparison of the antioxidant activity of aqueous extracts of various parts of Carica papaya L. The evaluation of total phenolic content and total flavonoid content revealed high antioxidant potential of the seeds and fruits. The free radical-scavenging potential of the aqueous extracts indicated the seeds to have better DPPH-scavenging activity than fruits.

Crystal structure of (4Z)-1-(3,4-di-chloro-phen-yl)-4-[hy-droxy(4-methyl-phen-yl)methyl-idene]-3-methyl-4,5-di-hydro-1H-pyrazol-5-one.

The title compound, C18H14Cl2N2O2, crystallizes with two mol-ecules, A and B, in the asymmetric unit. In mol-ecule A, the dihedral angles between the central pyrazole ring and pendant di-chloro-benzene and p-tolyl rings are 2.18 (16) and 46.

TNF-α regulates miRNA targeting mitochondrial complex-I and induces cell death in dopaminergic cells.

Parkinson's disease (PD) is a complex neurological disorder of the elderly population and majorly shows the selective loss of dopaminergic (DAergic) neurons in the substantia nigra pars compacta (SNpc) region of the brain. The mechanisms leading to increased cell death of DAergic neurons are not well understood. Tumor necrosis factor-alpha (TNF-α), a pro-inflammatory cytokine is elevated in blood, CSF and striatum region of the brain in PD patients.

C-terminal domain of CagX is responsible for its interaction with CagT protein of Helicobacter pylori type IV secretion system.

Helicobacter pylori are the well known human pathogen associated with gastric cancer and peptic ulcer. Pathogenesis is mainly due to the presence of 40 kb cagPAI (cag Pathogenicity Island) region that encodes the type IV secretion system (TFSS) consisting of a cytoplasmic part, a middle part/core complex (spans from inner membrane to outer membrane), and an outer membrane associated part. CagX and CagT are two important proteins of TFSS that have homology with virB9 and virB7 of Agrobacterium tumefaciens TFSS.

Design and synthesis of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents.

Type 2 diabetes (T2D) is a lifestyle disease affecting millions of people worldwide. Various therapies are available for the management of T2D and dipeptidyl peptidase-IV (DPP-IV) inhibition has emerged as a promising therapy for the treatment of type 2 diabetes (T2D). Here we report design, synthesis and in vitro efficacy of sulfonamide derivatives of pyrrolidine and piperidine as anti-diabetic agents.

Receptor-targeted drug delivery: current perspective and challenges.

Receptor-targeted drug delivery has been extensively explored for active targeting. However, the scarce clinical applications of such delivery systems highlight the implicit hurdles in development of such systems. These hurdles begin with lack of knowledge of differential expression of receptors, their accessibility and identification of newer receptors.

Potential of Piperazinylalkylester Prodrugs of 6-Methoxy-2-Naphthylacetic Acid (6-MNA) for Percutaneous Drug Delivery.

Piperazinylalkyl ester prodrugs (4a-5d) of 6-methoxy-2-naphthylacetic acid (6-MNA) (1) were synthesized and evaluated in vitro for the purpose of percutaneous drug delivery. These ionizable prodrugs exhibited varying aqueous solubilities and lipophilicities depending on the pH of the medium. The prodrugs (4a-5c) showed higher aqueous solubility and similar lipophilicity at pH 5.

Crystal structure of (Z)-1-(3,4-dichlorophenyl)-3-methyl-4-[(naphthalen-1-yl-amino)(p-tolyl)methylidene]-1H-pyrazol-5(4H)-one.

The title Schiff base compound, C28H21Cl2N3O, was synthesized by the condensation of 1-(3,4-di-chloro-phen-yl)-3-methyl-4-(4-methyl-benzo-yl)-1H-pyrazol-5(4H)-one with 1-aminona-phthalene. The p-tolyl ring is normal to the pyrazole ring, with a dihedral angle of 88.02 (14)°, and inclined to the naphthalene ring system by 78.

Expanding the spectrum of mutations in Indian patients with Tay-Sachs disease.

Tay-Sachs disease is an autosomal recessive neurodegenerative disorder occurring due to impaired activity of β-hexosaminidase-A (EC 3.2.1.

Luminescence study and dosimetry approach of Ce on an α-Sr2 P2 O7 phosphor synthesized by a high-temperature combustion method.

We report synthesis of a cerium-activated strontium pyrophosphate (Sr2 P2 O7 ) phosphor using a high-temperature combustion method. Samples were characterized by X-ray diffraction (XRD), Fourier transform infrared spectroscopy (FT-IR), photoluminescence (PL) and thermoluminescence (TL). The XRD pattern reveals that Sr2 P2 O7 has an α-phase with crystallization in the orthorhombic space group of Pnam.

Simultaneous HPTLC analysis of ursolic acid, betulinic acid, stigmasterol and lupeol for the identification of four medicinal plants commonly available in the Indian market as Shankhpushpi.

In this study, we investigated a new, simple, sensitive, selective and precise high-performance thin-layer chromatography (HPTLC) fingerprint and quantitative estimation method for the analysis of ursolic acid, betulinic acid, stigmasterol and lupeol in Shankhpushpi botanicals. Linear ascending development was carried out in a twin trough glass chamber saturated with petroleum ether-ethyl acetate-toluene (7:2:1, v/v/v). The plate was dried, sprayed with anisaldehyde reagent and analyzed by CAMAG TLC scanner III at 580 nm.

Modulation of steroidogenic pathway in rat granulosa cells with subclinical Cd exposure and insulin resistance: an impact on female fertility.

Changes in lifestyle lead to insulin resistance (IR) in females ultimately predisposing them towards infertility. In addition, cadmium (Cd), an environmental endocrine disruptor, is reported for detrimental effects on granulosa cells, thus leading to ovarian dysfunction. A combination of these factors, lifestyle and environment, seems to play a role in etiology of idiopathic infertility that accounts for 50% amongst the total infertility cases.