4-Thiazolidinones: the advances continue….

The diversity in the biological response of 4-thiazolidinones has attracted the attention of many researchers to explore this framework for its potential. It is, therefore, of prime importance that the study of this topic and the development of new synthetic strategies should be based on the most recent knowledge, emerging from the latest research. This review is an endeavor to highlight the progress in the chemistry and biological activity of the 4-thiazolidinones, predominantly after 2006.

Mono lacunary phosphomolybdate supported on MCM-41: synthesis, characterization and solvent free aerobic oxidation of alkenes and alcohols.

A new catalyst comprising monolacunary phosphomolybdate and MCM-41 was synthesized and characterized by different physicochemical techniques. The catalytic activity was evaluated by carrying out solvent free aerobic oxidation of alkenes and alcohols. The catalyst showed 60% conversion of styrene and 28% conversion of benzyl alcohol.

Microscopic evaluation, molecular identification, antifungal susceptibility, and clinical outcomes in fusarium, Aspergillus and, dematiaceous keratitis.

Purpose: Fusarium, Aspergillus, and Dematiaceous are the most common fungal species causing keratitis in tropical countries. Herein we report a prospective study on fungal keratitis caused by these three fungal species.

Methodology: A prospective investigation was undertaken to evaluate eyes with presumed fungal keratitis.

Antiviral signaling protein MITA acts as a tumor suppressor in breast cancer by regulating NF-κB induced cell death.

Emerging evidences suggest that chronic inflammation is one of the major causes of tumorigenesis. The role of inflammation in regulation of breast cancer progression is not well established. Recently Mediator of IRF3 Activation (MITA) protein has been identified that regulates NF-κB and IFN pathways.

Molecular Characterization of Novel Serovars of Bacillus thuringiensis Isolates from India.

Novel Bacillus thuringiensis isolates GS4, GN24 and UP1 were isolated and characterized by determination of serotyping, insecticidal protein by SDS-PAGE, plasmid composition, cry gene content and insect toxicity. Serologically two isolates GS4 and UP1 were allocated to the H3abce which is a new serovar while isolate GN24 was of H3ab type. Isolate GS4 produced flat crystal inclusions while UP1 produced cuboidal crystals.

Sorption of uranium from aqueous solutions using palm-shell-based adsorbents: a kinetic and equilibrium study.

In this study adsorbents based on palm shell powder as well as modified and activated palm shell powder were studied to analyze their behavior in sorbing U(6+) by both batch and fixed column modes. Seven different two-parameter isotherm models were applied to the experimental data to predict the sorption isotherms. The ΔG(0) values from Langmuir and thermodynamic calculations indicate physisorption as the major mechanism for adsorption of uranium.

Cholic acid modified 2 kDa polyethylenimine as efficient transfection agent.

New lipopolymers were synthesized by conjugating cholic acid (ChA) to polyethylenimines (PEI; 2 and 25 kDa) and a polyallylamine (PAA; 15 kDa) via N-acylation to develop effective gene delivery systems. The extent of ChA substitution linearly varied with the feed ratio during synthesis, indicating good control over grafting ratio. While ChA did not affect binding to plasmid DNA (pDNA) for higher molecular weight (MW) polymers, ChA substitution to 2 kDa PEI significantly affected the pDNA binding.

Risk based approach for design and optimization of stomach specific delivery of rifampicin.

The research envisaged focuses on risk management approach for better recognizing the risks, ways to mitigate them and propose a control strategy for the development of rifampicin gastroretentive tablets. Risk assessment using failure mode and effects analysis (FMEA) was done to depict the effects of specific failure modes related to respective formulation/process variable. A Box-Behnken design was used to investigate the effect of amount of sodium bicarbonate (X1), pore former HPMC (X2) and glyceryl behenate (X3) on percent drug release at 1st hour (Q1), 4th hour (Q4), 8th hour (Q8) and floating lag time (min).

Application of multiple regression analysis in optimization of anastrozole-loaded PLGA nanoparticles.

The present investigation deals with development of anastrozole-loaded PLGA nanoparticles (NPs) as an alternate to conventional cancer therapy. The NPs were prepared by nanoprecipitation method and optimized using multiple regression analysis. Independent variables included drug:polymer ratio (X1), polymer concentration in organic phase (X2) and surfactant concentration in aqueous phase (X3) while dependent variables were percentage drug entrapment (PDE) and particle size (PS).

Keggin type mono Ni(II)-substituted phosphomolybdate: a sustainable, homogeneous and reusable catalyst for Suzuki-Miyaura cross-coupling.

Keggin type mono Ni(II)-substituted phosphomolybdate was synthesized and characterized by various physico-chemical techniques and used as a catalyst for Suzuki-Miyaura cross-coupling. The influence of different reaction parameters was studied, to get the maximum yield. The novelty of the present work lies in obtaining >97% yield of biphenyl in 14 h under mild reaction conditions.

Surface immobilization of carbon nanotubes by beta-cyclodextrins and their inclusion ability.

The surface immobilization of beta-cyclodextrins on the surface of multiwalled carbon nanotubes (MWNTs) in an aqueous medium was achieved by covalent-binding of diamino-functionalized beta-cyclodextrin with carboxylic acid-functionalized MWNTs via amide linkages using a water-soluble condensation agent at room temperature. The obtained product denoted as beta-cyclodextrin-modified MWNTs was highly dispersible in an aqueous medium. The covalent surface functionalization of MWNTs by beta-cyclodextrin was characterized by FTIR, TGA, EDS and TEM.

Design and synthesis of 6,7-dimethoxyquinazoline analogs as multi-targeted ligands for α1- and AII-receptors antagonism.

Multiple-targeted ligands can have certain advantages for the management of hypertension which has multiple controls. Molecules with dual bioactivities are available in literature for treating metabolic disorders like diabetes, hypertension and hypercholesterolemia. After scrutinizing the SAR of prazosin-type α1-blockers and AII-antagonists it was planned to develop dual α1- and AII-antagonists.

The expression of adhesin EF-Tu in response to mucin and its role in Lactobacillus adhesion and competitive inhibition of enteropathogens to mucin.

Aims: To analyse the expression of EF-Tu in Lactobacillus strains with response to mucin exposure and its role in interfering with adhesion of enteropathogens to mucin.

Methods And Results: The Lactobacillus strains were analysed for their ability to adhere to immobilized mucin in microtiter plates. Lactobacillus delbrueckii M and Lactobacillus plantarum CS24.

A Small Molecule Swertisin from Enicostemma littorale Differentiates NIH3T3 Cells into Islet-Like Clusters and Restores Normoglycemia upon Transplantation in Diabetic Balb/c Mice.

Aim. Stem cell therapy is one of the upcoming therapies for the treatment of diabetes. Discovery of potent differentiating agents is a prerequisite for increasing islet mass.

Development of solid lipid nanoparticles based controlled release system for topical delivery of terbinafine hydrochloride.

The study describes the development and evaluation of solid lipid nanoparticles (SLNs) of terbinafine hydrochloride (TH) for sustained release and skin targeting. TH-loaded SLNs were prepared by solvent-injection technique and optimized using 3(3) full-factorial design. Effect of drug:lipid ratio, surfactant concentration and volume of organic solvent were studied on % entrapment efficiency (%EE) and particle size (PS).

Anthropometric indices and dietary intake: prospective determinants of geriatric cognitive impairment?

Objective: To assess the magnitude of elderly (aged 60-85 years) persons with cognitive impairment and its relation with their dietary and anthropometric status.

Design: Cross-sectional study. The cognitive status of the subjects was screened using the Mini Mental Score Examination (MMSE).

Basal expression of pluripotency-associated genes can contribute to stemness property and differentiation potential.

Pluripotency and stemness is believed to be associated with high Oct-3/4, Nanog, and Sox-2 (ONS) expression. Similar to embryonic stem cells (ESCs), high ONS expression eventually became the measure of pluripotency in any cell. The threshold expression of ONS genes that underscores pluripotency, stemness, and differentiation potential is still unclear.

Nitrogen containing privileged structures and their solid phase combinatorial synthesis.

The existence of preferred molecular scaffolds that possess inherent biological activity, called privileged structures, is now well recognized. Such privileged structures not only provide enhanced drug-like properties but also give new hits for developing leads. The synthesis of combinatorial libraries, especially with the insertion of privileged substructures into heterocyclic moieties containing nitrogen, provides for a greater probability of the discovery of novel lead compounds using chemical transformation.

Novel 2-aminobenzamides as potential orally active antithrombotic agents.

In an effort to develop potent antithrombotic agents, a series of novel 2-aminobenzamide derivatives were synthesized and screened for their in vivo antithrombotic activity. Among the 23 compounds tested, compound (8g) showed the most promising antithrombotic activity, which was comparable with clinically used aspirin or warfarin, but at variance with these standard drugs, 8g did not exhibit the increased bleeding time, suggesting its potential as a novel antithrombotic agent.

Design and development of multiple emulsion for enhancement of oral bioavailability of acyclovir.

The objective of this investigation was to design and develop water-in-oil-in-water type multiple emulsions (w/o/w emulsions) entrapping acyclovir for improving its oral bioavailability. Multiple emulsions (MEs) were prepared and optimized using Span-80 and Span-83 as lipophilic surfactant and Brij-35 as hydrophilic surfactant. The physio-chemical properties of the w/o/w emulsions - particle size, viscosity, phase separation (centrifugation test) and entrapment efficiency were measured and evaluated along with macroscopic and microscopic observations to confirm multiple nature, homogeneity and globule size.

Coriandrum sativum L. seed extract mitigates lipotoxicity in RAW 264.7 cells and prevents atherogenic changes in rats.

This study was designed to assess the efficacy of Coriandrum sativum L. (CS) in preventing in vitro low density lipoprotein (LDL) oxidation mediated macrophage modification. Further, an in vivo study was also conducted to confirm upon the efficacy of CS seed extract in alleviating pathophysiological alterations of high cholesterol diet induced atherosclerosis in rats.

Recent patents and advances on anti - tuberculosis drug delivery and formulations.

Tuberculosis has remained, unambiguously, a significant health care problem since long times, particularly in developing countries. The endeavoring battle against multi drug resistant TB, multiple dosing, their prominent side effects and bioavailability hiccups related to fixed dose combinations has undeniably become a Herculean task indicating rigorous research requirement in anti TB drug therapy. In view of the fact that patenting a drug molecule, a drug delivery system or a formulation has been very fruitful for the growth and sustainment of pharmaceutical industry, a meticulous review of recent developments, providing a balanced view on merits/demerits, will facilitate researchers to update themselves, thereby focusing their research in more relevant areas to furnish desired quality traits.

Novel methods and strategies in the discovery of TACE inhibitors.

Introduction: Tumor necrosis factor-α (TNF-α) is a key player in inflammation and joint damage in rheumatoid arthritis (RA). One treatment approach to exclude TNF-α from the biological system is by inhibiting tumor necrosis factor-alpha converting enzyme (TACE), the enzyme responsible for the production of its active form. To date, a number of TACE inhibitors have been reported in the literature from various strategies and methods.

Falcipain inhibitors as potential therapeutics for resistant strains of malaria: a patent review.

Introduction: There is an urgent need to discover new antimalarial drugs due to emergence of resistance in the parasite to the existing drugs. Malarial cysteine proteases falcipin-2 (FP-2) and falcipain-3 (FP-3) are attractive targets for antimalarial chemotherapy. The structures and functions of FP-2/3, their binding domains and their interactions with small- and macro-molecules are well studied.