Synthesis and Anticancer Evaluation of Disubstituted Benzimidazoles via One-Pot Telescopic Grinding Approach.

Benzimidazole compounds are known for their broad spectrum therapeutic potentials. A small library of benzimidazole derivatives were designed and synthesized via a one-pot telescopic grinding approach. The ability of these molecules as proposed anticancer agents were evaluated by their potential to bind to two important cancer pathway protein targets, human estrogen receptors and cyclin dependant kinases, 3ERT and 5FGK respectively.

Efficacy and safety of curcumin in maintaining remission during disease-modifying antirheumatic drug withdrawal in rheumatoid arthritis at 52 weeks: a phase III double-blind, randomized placebo-controlled trial.

Curcumin has anti-inflammatory properties but current evidence is limited to advocate its use in rheumatoid arthritis (RA). We explored whether curcumin could maintain remission in patients with RA while tapering conventional synthetic Disease-Modifying Antirheumatic Drugs (csDMARD). In this patient-and investigator-blinded trial, adults with RA in sustained remission for more than six months were randomized to oral curcumin (1 g) with piperine (5 mg) twice daily or matching placebo.

Correlates of breakthrough Omicron (B.1.1.529) infections in a prospective cohort of vaccinated patients with rheumatic diseases.

Background: Data on the effectiveness of SARS-CoV-2 vaccines and the durability of protection against the prevalent Omicron variant are scarce, especially in patients with autoimmune rheumatic diseases (AIRDs). Hence, we prospectively studied Omicron breakthrough infections in patients with AIRDs and attempted to isolate associated risk factors.

Methods: Patients with AIRDs who had completed primary vaccination with either AZD1222 or BBV152 vaccines were included and prospectively followed up from January 2022 onwards for the development of breakthrough Omicron infections.

Analyzing gender differentials in dietary diversity across urban and peri-urban areas of Hyderabad, India.

Background: India's recent increase in urbanization alongside with feminization of rural agriculture could increase the existing gender disparities in dietary diversity. With many rural men migrating to urban areas, women have increased domestic burdens as well as productive burdens such as making informed crop production decisions so household members consume a diverse diet. Given the rapid and recent onset of this phenomenon, there is a need to explore gender differentials in diet diversity across urban and rural areas to assess if certain populations are being disproportionately impacted by this trend.

COVID-19 Impact on Household Food Security in Urban and Peri-Urban Areas of Hyderabad, India.

This paper investigates the impact of the COVID-19 pandemic on food security and on coping-strategies in urban and peri-urban areas of the Hyderabad, India. Household survey data were collected before (October 2018) and during (January 2021) the onset of the pandemic. Results from logistic regression with the standarized Food Insecurity Expecience Scale (FIES) as dependent variable reveal that close to 40% of the households surveyed experienced a deterioration in food security status during the pandemic.

Diabetic macular edema treatment guidelines in India: All India Ophthalmological Society Diabetic Retinopathy Task Force and Vitreoretinal Society of India consensus statement.

Diabetic macular edema (DME) is a common cause of moderate visual impairment among people with diabetes. Due to the rising number of people with diabetes in India, the absolute numbers of people with DME are significant. There are several treatment options for DME, and the choice of treatment is based on the availability of retinal specialists and infrastructure for the delivery of treatment.

Understanding nutritional outcomes through gendered analysis of time-use patterns in semi-arid India.

The objective of this paper is to understand individual nutritional outcomes through an examination of gendered time use patterns. The analysis of the data from eight villages in the Semi-Arid Tropics (SAT), India confirm previous conclusions about the gendered influence of agricultural interventions, especially time demands on the rural poor. Agricultural interventions in the harsh, drought-prone environment of the SAT tend to increase the time burden on women.

One-Pot, Telescopic Approach for the Chemoselective Synthesis of Substituted Benzo[]pyrido/pyrazino/pyridazino[1,2-][1,2,4]thiadiazine dioxides and Their Significance in Biological Systems †.

The one-pot telescopic approach has been developed for the chemoselective synthesis of substituted benzo[]pyrido/pyrazino/pyridazino[1,2-][1,2,4]thiadiazine dioxides using readily available 2-aminopyridines/pyrazines/pyridazine and 2-chloro benzene sulfonyl chloride. This one-pot procedure involves the chemoselective sulfonylation of 2-aminopyridines/pyrazines/pyridazine with 2-chloro benzene sulfonyl chloride followed by a Cu(I)-catalyzed Ullmann-type C-N coupling reaction to obtain benzo[]pyrido/pyrazino/pyridazino[1,2-][1,2,4]thiadiazine dioxides with broad substrate scope and high functional group tolerance. The synthetic sequence merges well with the nucleophilic attack on the 2-amino group of pyridines/pyrazines/pyridazines on the 2-chloro benzene sulfonyl chloride, followed by Cu(I)-catalyzed ipso chloro displacement to C-N bond formation resulting in a more modular and straightforward approach.

Rapid Construction of an Imidazo[4,5-]pyridine Skeleton from 2-Chloro-3-nitropyridine via Tandem Reaction in HO-IPA Medium.

A highly efficient, clean, and simple procedure for the synthesis of a privilege imidazo[4,5-]pyridine scaffold from 2-chloro-3-nitropyridine in combination with environmentally benign HO-IPA as a green solvent is presented. The scope of the novel method has been demonstrated through the tandem sequence of SAr reaction with substituted primary amines followed by the in situ nitro group reduction and subsequent heteroannulation with substituted aromatic aldehydes to obtain functionalized imidazo[4,5-]pyridines with only one chromatographic purification step. The synthesis pathway appears to be green, simple, and superior compared with other already reported procedures, with the high abundance of reagents and great ability in expanding the structural diversity.

Taming C-terminal peptides of Staphylococcus aureus leukotoxin M for B-cell response: Implication in improved subclinical bovine mastitis diagnosis and protective efficacy in vitro.

Leukotoxin M/F'-PV (LukM/F'-PV) produced by bovine mastitis causing Staphylococcus aureus structurally comprises three domains, the β-sandwich, rim and stem domain. The rim and stem domains interacting with target cell membrane lipid rafts contributes to the virulent trait of the toxin. In the present study, two facts were hypothesized that neutralization of these domains will ebb LukM/F'-PV leukotoxicity.

Diversity in the antibacterial potential of probiotic cultures Bacillus licheniformis MCC2514 and Bacillus licheniformis MCC2512.

The aim of the present study was to investigate the characteristic diversity and stability of antimicrobial compounds produced by two probiotic strains of Bacillus licheniformis (MCC2514 and MCC2512). Antimicrobial compounds from the two strains notably varied, related to stability and potency. The inhibitory spectrum of B.

Postpartum Acute Pulmonary Oedema with Sub clinical Rheumatic Heart Disease.

Acute dyspnea with pulmonary oedema in postpartum is uncommon but life-threatening event. Contributing factors for pulmonary oedema include, administration of tocolytics, underlying cardiac disease, iatrogenic fluid overload and preeclampsia acounting 0.08% of pregnancies.

Corosolic acid content and SSR markers in Lagerstroemia speciosa (L.) Pers.: a comparative analysis among populations across the Southern Western Ghats of India.

Lagerstroemia speciosa commonly known as 'Banaba' is native of south-east Asia which exhibits both horticultural and therapeutic value. The anti-diabetic and anti-obese property of the tree is attributed to corosolic acid (CRA)-a pentacyclic triterpene seen predominantly in the mature leaves. Although there are studies on either chemical or genetic variation in L.

Immunogenicity of Staphylococcus aureus LukM/F'-PV recombinant subunits: validation of diagnostic potential and evaluation of protective efficacy in vitro.

Leukotoxin M/F'-Panton Valentine (LukM/F'-PV), a beta pore-forming toxin secreted by Staphylococcus aureus, is a major virulence factor involved in the pathogenesis of bovine mastitis. The present study was aimed to determine immunogenicity of two recombinant subunits of LukM/F'-PV, rLukM (MW 38 kDa) and rLukF (MW 39 kDa), develop and validate an indirect enzyme linked immunosorbent assay (ELISA) using polyclonal antibodies raised in rabbits, and evaluate applicability of the assay to diagnose clinical and subclinical bovine mastitis. Additionally, in vitro assays were conducted to determine abilities of antibodies to neutralize cytotoxicity of the native leukotoxin.

Anaesthetic management of a neonate with right sided congenital diaphragmatic hernia.

Neonates who are born with CDH suffer from sub-stantial morbidity and mortality. Modalities of treatment are said to influence outcome, apart from pre-natal and post-natal factors. Reports from developed countries have described improved survival with High Frequency Oscillatory Ventilation (HFOV), Extra Corporeal Membrane Oxygenation (ECMO) and inhaled Nitric Oxide (NO).

Molecular Characterization and Toxicity Confirmation of LukM/F'-PV Producing Staphylococcus aureus Isolated from Bovine Mastitis Samples in Mysore, India.

The widespread status of subclinical condition of bovine mastitis is often associated with the production of leukotoxin M/F'-PV producing Staphylococcus aureus. The present study aims for the profiling of such leukotoxin producers through conventional and molecular methods in parallel to their leukotoxicity. The incidence of this particular pathogen was assessed in mastitis infected Holstein-Friesian cattle, where eight isolates of staphylococci were found to be present in 20 % of collected samples.

Efficient phyto-synthesis and structural characterization of rutile TiO2 nanoparticles using Annona squamosa peel extract.

In the present study, the biosynthesis of rutile TiO(2) nanoparticles (TiO(2) NPs) was achieved by a novel, biodegradable and convenient procedure using fruit peel Annona squamosa aqueous extract. This is the first report on the new, simple, rapid, eco-friendly and cheaper methods for the synthesis of rutile TiO(2) NPs at lower temperature using agricultural waste. Rutile TiO(2) NPs were characterized by UV, XRD, SEM, TEM and EDS studies.

In vitro safety evaluation and anticlastogenic effect of BacoMind on human lymphocytes.

Objective: BacoMind (BM) is a standardized extract of Bacopa monnieri, which belongs to the family Scrophulariaceae and is a creeping annual plant found throughout the Indian subcontinent. It has been used by Ayurvedic medicinal practitioners in India for almost 3000 years and is classified as a medharasayana, a substance which improves memory and intellect. With the widespread traditional use as well as scientific validation of Bacopa monnieri for nootropic activity, a bioactive-rich unique phytochemical composition-BacoMind was developed from B.

Screening of selected Indian medicinal plants for acetylcholinesterase inhibitory activity.

Seventy-six plant extracts including methanolic and successive water extracts from 37 Indian medicinal plants were investigated for acetylcholinesterase (AChE) inhibitory activity (in vitro). Results indicated that methanolic extracts to be more active than water extracts. The potent AChE inhibiting methanolic plant extracts included Withania somnifera (root), Semecarpus anacardium (stem bark), Embelia ribes (Root), Tinospora cordifolia (stem), Ficus religiosa (stem bark) and Nardostachys jatamansi (rhizome).

Trypsin inhibitory activity of Lawsonia inermis.

The ethanolic extract of Lawsonia inermis leaves and lawsone tested for trypsin inhibitory activity showed an IC(50) value of 64.87 and 48.6 microg/ml, respectively.

Brine shrimp lethality bioassay of selected Indian medicinal plants.

Ethanolic extracts of six Indian medicinal plants, piperine, guggulsterone E and guggulsterone Z were tested for cytotoxicity using brine shrimp lethality test. Piper longum showed most potent cytotoxic activity. Piperine, guggulsterone E and guggulsterone Z showed potent activity with LC(50) 2.

alpha-Glucosidase inhibitory activity of Mangifera indica bark.

The ethanolic extracts of Lawsonia inermis leaves, Holarrhena antidysenterica bark, Swertia chirata whole plant and Mangifera indica bark were tested (in-vitro) for alpha-glucosidase inhibitory activity. M. indica extract was found to be the most potent, with an IC(50) value of 314 microg/ml.

Anthelmintic activity of essential oil of Ocimum sanctum and eugenol.

The essential oil of Ocimum sanctum and eugenol, tested in vitro, showed potent anthelmintic activity in the Caenorhabditis elegans model. Eugenol exhibited an ED(50) of 62.1 microg/ml.

Anthelmintic activity of Butea monosperma.

The methanol extract of Butea monosperma seeds, tested in vitro, showed significant anthelmintic activity.

Effect of certain plant extracts on alpha-amylase activity.

Ethanolic extracts of Punica granatum, Mangifera indica, Boerhaavia diffusa, Embelia ribes, Phyllanthus maderaspatensis, and Withania somnifera, were tested for their effect on alpha-amylase activity (in vitro). P. granatum and M.