An Insight into the Synthesis and SAR of 2,4-Thiazolidinediones (2,4-TZD) as Multifunctional Scaffold: A Review.

2,4-Thiazolidinedione (2,4-TZD) is a versatile pharmacophore, a privileged scaffold, and a remarkable sulphur-containing heterocyclic compound with diverse pharmacological activities. The multifarious biological activities, due to different mechanisms of action, low cost, and easy availability of 2,4-TZD impressed medicinal chemists to integrate this moiety to develop various lead compounds with diverse therapeutic actions. This resulted in the swift development in the last decade for generating different new potential molecules bearing 2,4-TZD.

Virtual reality among the elderly: a usefulness and acceptance study from Taiwan.

Background: Virtual reality (VR) has several applications in the medical domain and also generates a secure environment to carry out activities. Evaluation of the effectiveness of VR among older populations revealed positive effects of VR as a tool to reduce risks of falls and also improve the social and emotional well-being of older adults. The decline in physical and mental health, the loss of functional capabilities, and a weakening of social ties represent obstacles towards active aging among older adults and indicate a need for support.

Phytochemical Composition, Antioxidant, and Antimicrobial Attributes of Different Solvent Extracts from Buch.-Ham. ex. D. Don Leaves.

: Plant diversity is a basic source of food and medicine for local Himalayan communities. The current study was designed to assess the effect of different solvents (methanol, ethyl acetate, and water) on the phenolic profile, and the corresponding biological activity was studied. : Antioxidant activity was investigated using 2,2-diphenyl-1-picrylhydrazyl (DPPH) and 2,2″-azino-bis(3-ethylbenzothiazoline-6-sulphonic) acid (ABTS) assay, while the antimicrobial activity was evaluated by disk diffusion method using various bacterial and fungal strains.

Direct Conversion of Carboxylic Acids to Various Nitrogen-Containing Compounds in the One-Pot Exploiting Curtius Rearrangement.

Herein we report, a single-pot multistep conversion of inactivated carboxylic acids to various N-containing compounds using a common synthetic methodology. The developed methodology rendered the use of carboxylic acids as a direct surrogate of primary amines, for the synthesis of primary ureas, secondary/tertiary ureas, /-carbamates, benzoyl ureas, amides, and formyls, exploiting the Curtius reaction. This approach has a potential to provide a diversified library of N-containing compounds, starting from a single carboxylic acid, based on the selection of the nucleophile.

Resveratrol loaded functionalized nanostructured lipid carriers for breast cancer targeting: Systematic development, characterization and pharmacokinetic evaluation.

Resveratrol (RSV) has shown to possess anti-cancer potential in various studies; however, its poor water solubility, extensive first-pass metabolism, and photostability issues have limited its clinical application. Therefore, the aim of the current investigation was to formulate and optimize a nanostructured lipid carriers (NLCs) based parenteral formulation of RSV for its effective delivery to breast cancer cells. NLCs loaded with RSV (RSV-NLCs) were formulated by the modified solvent injection technique and were systematically optimized using a three level-three factor Box-Behnken design.

Lacidipine attenuates reserpine-induced depression-like behavior and oxido-nitrosative stress in mice.

Depression is a serious medical illness displaying high lifetime prevalence, early-age onset that adversely affects socio-economic status. The bidirectional association between oxidative stress and calcium-signaling adversely affects the monoaminergic neuron functions that instigate the pathogenesis of depression. The present study investigates the effect of lacidipine (LCD), L-type Ca-channel blocker, on reserpine-induced depression in mice.

Buch.-Ham. ex D. Don: A Natural Source for Health Promotion and Disease Prevention.

(Myricaceae) is a popular medicinal plant most commonly found in the sub-tropical Himalayas. It is widely used in folk medicine to treat several ailments such as asthma, cough, chronic bronchitis, ulcers, inflammation, anemia, fever, diarrhea, and ear, nose, and throat disorders. Due to its multidimensional pharmacological and therapeutic effects, it is well recognized in the ayurvedic pharmacopeia.

Novel p-Functionalized Chromen-4-on-3-yl Chalcones Bearing Astonishing Boronic Acid Moiety as MDM2 Inhibitor: Synthesis, Cytotoxic Evaluation and Simulation Studies.

Background: Novel 4-[3-(6/7/8-Substituted 4-Oxo-4H-chromen-3-yl)acryloyl]phenylboronic acid derivatives (5a-h) as well as other 6/7/8-substituted-3-(3-oxo-3-(4-substitutedphenyl) prop-1-enyl)-4H-chromen-4-one derivatives (3a-u) have been designed as p53-MDM2 pathway inhibitors and reported to possess significant cytotoxic properties against several cancer cell lines.

Objectives: The current project aims to frame the structure-anticancer activity relationship of chromen-4-on-3-yl chalcones (3a-u/5a-h). In addition, docking studies were performed on these chromeno-chalcones in order to have an insight into their interaction possibilities with MDM2 protein.

An Update on the Use of Alginate in Additive Biofabrication Techniques.

Background: Solid free forming (SFF) technique also called additive manufacturing process is immensely popular for biofabrication owing to its high accuracy, precision and reproducibility.

Method: SFF techniques like stereolithography, selective laser sintering, fused deposition modeling, extrusion printing, and inkjet printing create three dimension (3D) structures by layer by layer processing of the material. To achieve desirable results, selection of the appropriate technique is an important aspect and it is based on the nature of biomaterial or bioink to be processed.

Development and evaluation of isradipine via rutin-loaded coated solid-lipid nanoparticles.

The objective was to develop a stable and non-compliance coated solid-lipid nanoparticles (coated SLN) using polymer (Eudragit L100) and lipoid (glycerol monostearate: soya lecithin) for partial dose reduction of isradipine [ISR; 2.5 mg by combination of bioenhancing agent (rutin; Ru) in equivalent ratio]. The physicochemical characterizations were performed by FT-IR and DSC of elected model drug (ISR), drug mixer with Ru/polymer and coated SLN with Ru (ONbp); the resulted distinctive peaks demonstrated that no chemical interaction and incompatibility found between them.

Chloro and bromo-pyrazole curcumin Knoevenagel condensates augmented anticancer activity against human cervical cancer cells: design, synthesis, docking and cytotoxicity analysis.

With an endeavor to develop novel curcumin analogs as potential anti-cancer agents, we designed and synthesized a series of Knoevenagel condensates by clubbing pyrazole carbaldehydes at the active methylene carbon atom of the curcumin backbone. Molecular docking studies were carried out to target the proposed derivatives on human kinase β (IKKβ), a potential anti-cancer target. The chloro derivative displayed five hydrogen bond interactions with a docking score of -11.

Design, Development and In vitro/Ex vivo Evaluation of Mucoadhesive Buccal Film of Benzydamine Hydrochloride for the Effective Treatment of Aphthous Stomatitis.

Background: During the recent two decades, the development of mucoadhesive drug delivery system has been gained tremendous importance to cure many recurrent diseases of the oral cavity. The drug delivery through the buccal route is quite challenging due to limited absorption area, movements of the target region and regular flow of saliva lead to the sub-therapeutic drug level in the buccal region.

Objective: The aim is to develop unidirectional release mucoadhesive buccal film for the mucosal delivery of Benzydamine Hydrochloride (WO2016126217Al, EP0812193B1) and evaluate the effects of a different grade of HPMC polymer (US5980942A) with the presumption to prolong the residence time and therapeutic effectiveness at the target site.

Cefixime-associated acute generalized exanthematous pustulosis: Rare cases in India.

Background: Cefixime is a widely used third-generation cephalosporin schedule H1 drug, which is prescribed for the treatment of otitis media, respiratory tract infections, and uncomplicated urinary tract infections and is effective against infections caused by and species in India. The National Coordination Centre (NCC)-Pharmacovigilance Programme of India (PvPI), Indian Pharmacopoeia Commission (IPC), has received rare individual case safety reports (ICSRs) for acute generalized exanthematous pustulosis (AGEP) associated with the use of cefixime.

Materials And Methods: IPC, NCC-PvPI also acts as a national collaborating center for pharmacovigilance activities under the aegis of Ministry of Health and Family Welfare, Government of India; moreover, it is a member country in global pharmacovigilance system, World Health Organization-Uppsala Monitoring Centre, Sweden.

Role of adenylyl cyclase activator in controlling experimental diabetic nephropathy in rats.

The present study aimed to investigate the role of adenylyl cyclase activator in preventing diabetic nephropathy in rats. Renal function parameters, renal hypertrophy, lipid profile, markers of oxidative stress and free radical scavenging activities were assessed. Histopathology was performed to confirm Streptozotocin induced renal morphological changes in diabetic rats.

A facile synthesis of Cs loaded TiO nanotube photoelectrode for the removal of 4-chloroguaiacol.

In this study, novel Cesium (Cs) doped TiO nanotubes photoelectrode (Cs/TiONTs) were synthesized by simple electrochemical anodization method and characterized by several physicochemical techniques. In particular, the photocatalytic (PC), electrocatalytic (EC) and photoelectrocatalytic (PEC) activity of newly synthesized Cs/TiONTs electrodes was investigated using 4-Chloroguaiacol (4-CG). The effect of operating parameters like Cs concentration, electrolyte concentration, external current and pH on degradation efficacy was examined.

Performance and emission characteristics of CNG-fueled compression ignition engine with Ricinus communis methyl ester as pilot fuel.

Surge in petroleum prices, its drying sources and degradation in air quality focused interest on renewable energy sources as substitute for existing fuels for internal combustion engines. This study highlights the combustion, performance, and emission characteristics of diesel engines fueled with compressed natural gas (CNG) as primary fuel and castor (Ricinus communis) oil methyl ester (COME) as pilot fuel. COME was produced from non-edible grade Ricinus communis oil.

N-pyridin-2-yl benzamide analogues as allosteric activators of glucokinase: Design, synthesis, in vitro, in silico and in vivo evaluation.

Glucokinase (GK) is the key enzyme controlling levels of blood glucose under normal physiological range, and GK activators are emerging class of drug candidates with promising hypoglycaemic activity. The current study was planned to design, synthesize and evaluate novel N-pyridin-2-yl benzamide analogues as allosteric activators of GK. A novel series of N-pyridin-2-yl benzamide analogues were synthesized starting from 3-nitrobenzoic acid and evaluated in vitro for GK activation followed by in silico studies to predict the binding interactions of the designed molecules with GK protein.

Nanotechnological Carriers for Treatment of Acne.

Background: Acne is a multifactorial skin disease associated with pilosebaceous unit and caused by bacteria Propionibacterium acnes and Acne vulgaris. Near about 95% people throughout the world suffer from acne at some point in their life span. This disease is more prominent in adults compared to neonates and prepubescent children.

Emerging and Alternative Therapies For Parkinson Disease: An Updated Review.

Parkinson's disease (PD) is standout amongst the most common neurodegenerative malady with unpredictable dynamic pathology. At present, accessible traditional choices for PD have certain impediments of their own, and subsequently persistent consistence and fulfillment are low. Current contemporary treatment options just give symptomatic alleviation constrained control to anticipate malady progression, bringing about poor patient consistence and fulfilment.

Augmentation of hepatoprotective potential of Aegle marmelos in combination with piperine in carbon tetrachloride model in wistar rats.

The current study investigated hepatoprotective and antioxidant effects of Aegle marmelos leaves extract. The major constituent present in the extract i.e.

Transethosomes of Econazole Nitrate for Transdermal Delivery: Development, In-vitro Characterization, and Ex-vivo Assessment.

Background: Transdermal drug delivery is an attractive approach for both local and systemic therapeutics of various diseases. Transdermal drug delivery systems show various advantages like reduction of local irritation, prevention of first-pass hepatic metabolism, and bioavailability enhancement of bioactive molecules over conventional drug delivery systems.

Objective: The main objective of the present research work was to develop and characterize (in-vitro and ex-vivo) econazole nitrate loaded transethosomes and their comparison with marketed cream of econazole nitrate [Ecoderm, Brown and Burk Pharmaceutical (Pvt.

Recent Updates on Glucokinase Activators and Glucokinase Regulatory Protein Disrupters for the Treatment of Type 2 Diabetes Mellitus.

Introduction: The impairment of glucose metabolism leads to hyperglycemia and type-2 diabetes mellitus. Glucokinase enzyme is the key regulator of glucose homeostasis that catalyzes the conversion of glucose to glucose-6-phosphate in liver and pancreatic cells. In hepatocytes, GK controls the glucose uptake and glycogen synthesis.

Nano-colloidal carrier polymeric coating for oral delivery of isradipine.

Our research objective was to develop, characterize, and optimize stable form of nano-colloidal carrier with Eudragit-coated solid lipid nanobioparticles (SLNbp) for oral delivery of isradipine (ISR). To achieve, a three factors, i.e.

Advanced Drug Delivery Systems for Transdermal Delivery of Non-Steroidal Anti-Inflammatory Drugs: A Review.

Background: Transdermal route of delivery of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs) has several advantages over other routes like reduced adverse effects, less systemic absorption, and avoidance of first-pass effect and degradation in the gastrointestinal tract (GIT). Transdermal route is also beneficial for drugs having a narrow therapeutic index. The skin acts as the primary barrier for transdermal delivery of various therapeutic molecules.

Exploring Therapeutic Potential of Nanocarrier Systems Against Breast Cancer.

Background: Breast cancer is the most widely occurring non-cutaneous cancer in women. Treatment options available for breast cancer are limited and there are a number of toxicity concerns associated with them. Therefore, nanocarrier based approaches have been explored for breast cancer treatment.