Enhanced safety and efficacy profile of CD40 antibody upon encapsulation in pHe-triggered membrane-adhesive nanoliposomes.

Aim: To develop pH (pHe)-triggered membrane adhesive nanoliposome (pHTANL) of CD40a to enhance anti-tumor activity in pancreatic cancer while reducing systemic toxicity.

Materials And Methods: A small library of nanoliposomes (NL) with various lipid compositions were synthesized to prepare pH (pHe)-triggered membrane adhesive nanoliposome (pHTANL). Physical and functional characterization of pHTANL-CD40a was performed via dynamic light scattering (DLS), Transmission Electron Microscopy (TEM), confocal microscopy, and flow cytometry.

Phyto-metabolomic investigation of biologically active fraction of leaf.

(Wight & Arn.) Benth., leaves are used traditionally in variety of diseases.

A staphylococcal capsule-producing enzyme that unfolds via multiple intermediates predominantly exists as the trimers at low concentrations.

CapG, an enzyme expressed by , catalyzes an epimerization reaction to synthesize -acetyl-L-fucosamine, a constituent of capsule involved in pathogenesis. This protein has two domains, exists as the homohexamers in the solution, and usually produces products at hundred-nanomolar concentrations. To determine the folding-unfolding mechanism and the oligomeric form of CapG, particularly at low concentrations, we have investigated a recombinant CapG (rCapG) using different probes.

Advancements and challenges in tuberculosis drug discovery: A comprehensive overview.

Tuberculosis continues to pose a health challenge causing the loss of millions of lives despite the existence of multiple drugs, for treatment. The emergence of drug-resistant strains has made the situation more complex making it increasingly difficult to fight against this disease. This review outlines the challenges associated with TB drug discovery, the nature of Mycobacterium tuberculosis shedding light on the mechanisms that lead to treatment failure and antibiotic resistance.

Design, synthesis, and biological evaluation of pyrazole-ciprofloxacin hybrids as antibacterial and antibiofilm agents against .

In our continued efforts to tackle antibiotic resistance, a new series of pyrazole-ciprofloxacin hybrids were designed, synthesized, and evaluated for their antibacterial activity against (), (), and (). Most of the compounds exhibited good to excellent activities against , and six compounds (7a, 7b, 7d, 7g, 7k, and 7p) exhibited higher or comparable activity (MIC = 0.125-0.

Effect of two-fold single-atom substitutions (S, Se; C, N) in band gap engineered donor-acceptor conjugated microporous polymers on the efficient aerobic photooxidation of aryl sulfides.

Substitution of a single atom in a photoactive system is capable of vastly altering its optoelectronic properties leading to the generation of an efficient photocatalyst. In this study, we explore the impact of two-fold single-atom substitutions on the optoelectronic properties and photocatalytic performance of donor-acceptor type conjugated microporous polymers (D-A CMPs). For this, three isostructural triphenylamine (TPA)-based D-A CMPs were synthesized namely PTPA-BT, PTPA-BS, and PTPA-PS containing 2,1,3-benzothiadiazole, 2,1,3-benzoselenadiazole and [1,2,5]selenadiazolo[3,4-]pyridine as the acceptor moieties, respectively.

Sulfoximine Aided Ru(II)-Catalyzed Asymmetric Double C(sp)-H Hydroarylations of Olefins.

Presented here is a sulfoximine-directed Ru(II)-catalyzed asymmetric intramolecular double C(sp)-H hydroarylation of olefins. This process provides a diastereoselective and enantiospecific synthetic route to highly substituted tetrahydrobenzodifurans. Notably, the reaction accommodates labile functional groups and is scalable to gram quantities.

Visible Light-Induced Radical Cascade Functionalization of Quinoxalin-2(1)-ones: Three-Component 1,2-Di(hetero)arylation Approach with Styrenes and Thianthrenium Salts.

The additive-free visible light-induced three-component 1,2-di(hetero)arylation of styrenes was developed using quinoxalin-2(1)-ones and thianthrenium salts. The purple visible light excitable quinoxalin-2(1)-ones were utilized for the single-electron transfer to aryl thianthrenium salts, where the generated aryl radical species underwent the addition cascade to styrenes and quinoxalin-2(1)-ones. The direct aryl radical addition to quinoxalin-2(1)-ones also led to the formation of a side product, C3-aryl quinoxalin-2(1)-ones, capable of a photoredox process to help the formation of 1,2-di(hetero)arylation products.

Post-Functionalization of Fluorinated Dibenzosulfone-Based Conjugated Polymer for Smart 'Turn-off' Sensing of Cu Ions.

Post-functionalization of conjugated polymeric backbone with various N-containing heterocycles through nucleophilic aromatic substitution reaction (SAr) demonstrates crucial tailoring of their photophysical properties. This study explores an approach of post-polymerization modification of a fluorinated dibenzosulfone-based conjugated polymer aiming to incorporate functional groups having coordinating sites to bind metal ions. The resulting polymers, namely BDT-DBTS-IM, BDT-DBTS-TR, and BDT-DBTS-PY revealed successful substitution reactions with imidazole, triazole, and pyridine respectively, and showed significant changes in their absorption and emission properties.

2-Aryl-Benzoimidazoles as Type II NADH Dehydrogenase Inhibitors of .

The nonproton pumping type II NADH dehydrogenase in is essential for meeting the energy needs in terms of ATP under normal aerobic and stressful hypoxic environmental states. Type II NADH dehydrogenase conduits electrons into the electron transport chain in , which results in ATP synthesis. Therefore, the inhibition of NDH-2 ensures the abolishment of the entire ATP synthesis machinery.

Visible Light-Mediated Co(II) Catalyzed Synthesis of Epoxy Ketones by Oxidative Coupling of Alkenes and Aldehydes in Water.

A one-step, two-component visible light-mediated CoCl·6HO-catalyzed oxidative acylation of alkenes by aldehydes to synthesize -epoxy ketone has been achieved in water at room temperature. The photocatalytic activity of Co(II) presented a remarkable achievement for synthesis of -epoxy ketones from aldehydes and olefins, with a wide substrate compatibility including aromatic, heteroaromatic and aliphatic aldehydes, styrenes with both electron-donating and withdrawing groups, α-substituted styrenes, stilbene, acrylates, and even the challenging unactivated aliphatic alkenes. Mechanistic studies including radical trapping experiments, intermediate detection by GCMS, Hammett analysis, and DFT studies unveil the nature of the photocatalytic pathway.

Heterogenization of Homogeneous Donor-Acceptor Conjugated Polymers for Efficient Photooxidation: An Approach Toward Sustainable and Recyclable Photocatalysis.

Recovery of homogeneous photocatalysts from reaction mixture is challenging, affecting the cost-effectiveness, and masks their advantages, including 4-8 fold higher catalytic activity than corresponding heterogeneous counterparts. Incorporation of long alkyl chains within the rigid π-conjugated backbone of conjugated polymers can augment their solubility in particular organic solvents; accordingly, they can function as homogeneous photocatalysts. Consequently, these polymers facilitate the recovery of catalysts through the reverse dissolution process, thus creating a well-suited platform to meet certain advantages of both homo- and heterogeneous photocatalysts.

Staphylococcus aureus major cell division protein FtsZ assembly is inhibited by silibinin, a natural flavonolignan that also blocked bacterial growth and biofilm formation.

The bacterial cell division protein FtsZ has been considered a potential therapeutic target due to its rapid treadmilling that induces cellular wall construction in bacteria. The current study discovered a novel antimicrobial compound, silibinin, a natural flavonolignan and its impact on the recombinant S. aureus FtsZ (SaFtsZ).

Development and Evaluation of Bis-benzothiazoles as a New Class of Benzothiazoles Targeting DprE1 as Antitubercular Agents.

Benzothiazole-bearing compounds have emerged as potential noncovalent DprE1 (decaprenylphosphoryl-β-d-ribose-2'-epimerase) inhibitors active against . Based on structure-based virtual screening (PDB ID: 4KW5), a focused library of thirty-one skeletally diverse benzothiazole amides was prepared, and the compounds were assessed for their antitubercular activity against H37Ra. Most potent compounds and were further evaluated against the H37Rv strain by the microdilution assay method.

Burden of drug-resistant tuberculosis by the GeneXpert MTB/RIF assay and its clinico-epidemiological aspects at a tertiary care hospital in West Bengal.

Multidrug -resistant tuberculosis (MDRTB) is a serious threat to mankind. India has the highest number of MDRTB cases, although majority remain undiagnosed due to inadequate diagnostic infrastructure, leading to increased community transmission and mortality. This one-year observational retrospective study highlighted the effectiveness of the National Tuberculosis Elimination Program (NTEP) for prompt detection of drug-resistant TB by GeneXpert MTB/RIF assay and revealed its associated clinico-epidemiological factors.

Chiral Sulfoximine Mediated Cobalt-Catalyzed Atropselective C-H Annulation of Ynamides.

An achiral Cp*Co(III)-catalyzed enantioselective C-H activation/annulation of chiral sulfoximine-enabled thioamides with ynamides is presented herein. This method successfully synthesizes axially chiral five-membered 2-amidoindenones with good enantiocontrol. Interestingly, the annulation with chiral oxazolidone-containing ynamides could provide a separable mixture of diastereomers (up to ~10 : 1 dr).

Moisture-resistant radical anions of quinoxalin-2(1)-ones in aerial dioxygen activation.

This study demonstrates the successful formation of a radical anion intermediate in a moist atmosphere, facilitating chemical reactions by activating aerial dioxygen through a single electron transfer (SET) mechanism. Derived from deprotonating quinoxaline-2(1)-one with KOBu, it shows potential in oxygenation chemistry. Validation comes from radical scavenging and EPR experiments.

Antitubercular activity of 2-mercaptobenzothiazole derivatives targeting type II NADH dehydrogenase.

() type II NADH dehydrogenase (NDH-2) transports electrons into the mycobacterial respiratory pathway at the cost of reduction of NADH to NAD and is an attractive drug target. Herein, we have synthesised a series of 2-mercaptobenzothiazoles (C1-C14) and evaluated their anti-tubercular potential as NDH-2 inhibitors. The synthesised compounds C1-C14 were evaluated for MIC and ATP depletion against H37Ra, , and H37Rv mc 6230.

Immunomodulatory and immune-toxicological role of nanoparticles: Potential therapeutic applications.

Nowadays, Nanoparticle-based immunotherapeutic research has invoked global interest due to their unique properties. The immune system is a shielding structure that defends living things from external threats. Before the use of any materials in drug design, it is essential to study the immunological response to avoid triggering undesirable immune responses in the body.

Cobalt(II)-Catalyzed Synthesis of γ-Diketones from Aryl Alkenes and Its Utilization in the Synthesis of Various Heterocyclic Compounds.

An earth-abundant Co(II) salt-catalyzed mild and affordable synthetic route has been developed for the synthesis of industrially relevant 1,4-dicarbonyl compounds (or γ-diketones) oxidative coupling between aryl alkenes and ketones (both cyclic and acyclic) using TBHP and DBU as the oxidant and base, respectively. 1,4-Dicarbonyl compounds are known to be synthesized using expensive metal catalysts, dual catalysts, or low-cost metal complexes combined with an additive or ligand template, which further needs to be synthesized. Herein, we report the synthesis of 1,4-dicarbonyl compounds using cobalt(II) acetate as a catalyst without any expensive co-catalyst or ligand templates.

Te and Er doped ZrO nanoparticles with enhanced photocatalytic, antibacterial activity and dielectric properties: A next generation of multifunctional material.

Amid rising water contamination from industrial sources, tackling toxic dyes and pathogens is critical. Photocatalysis offers a cost-effective and eco-friendly solution to this pressing challenges. Herein, we synthesized Te and Er doped ZrO photocatalysts through hydrothermal method and investigated their efficacy in degrading Congo red (CR) and pathogens under visible light.

Ferroelectric polymorphic phenomena in the layered antiferromagnet Cu(OH).

Ferroic orders and their associated structural phase transitions are paramount in the understanding of a multitude of unconventional condensed matter phenomena. On this note, our investigation focuses on the polymorphic ferroelectric (FE) phase transitions of Copper(II) hydroxide, Cu(OH), considering an antiferromagnetic ground state. By employing the first-principles studies and group theory analysis, we have provided a systematic theoretical investigation of vibrational properties in the hypotheticalhigh-symmetry phase to unveil the symmetry-allowed ferroic phases.

Sonochemically synthesized black phosphorus nanoparticles: a promising candidate for piezocatalytic antibacterial activity with enhanced dielectric properties.

The drawbacks inherent to traditional antibacterial therapies, coupled with the escalating prevalence of multi-drug resistant (MDR) microorganisms, have prompted the imperative need for novel antibacterial strategies. Accordingly, the emerging field of piezocatalysis in semiconductors harnesses mechanical stress to drive chemical reactions by utilizing piezo-generated free charge carriers, presenting a promising technology. To the best of our knowledge, this study is the first to provide a comprehensive overview of the eradication of pathogenic bacteria using few-layer black phosphorus (SCBP) piezo catalyst under mechanical stimuli, along with the exploration of temperature dependent dielectric properties.

Does novelty influence the foraging decisions of a scavenger?

Acquiring knowledge about the environment is crucial for survival. Animals, often driven by their exploratory tendencies, gather valuable information regarding food resources, shelter, mating partners, . However, neophobia, or avoiding novel environmental stimuli, can constrain their exploratory behaviour.

Exploring rhodanine linked enamine-carbohydrazide derivatives as mycobacterial carbonic anhydrase inhibitors: Design, synthesis, biological evaluation, and molecular docking studies.

With the rise of multidrug-resistant tuberculosis, the imperative for an alternative and superior treatment regimen, incorporating novel mechanisms of action, has become crucial. In pursuit of this goal, we have developed and synthesized a new series of rhodanine-linked enamine-carbohydrazide derivatives, exploring their potential as inhibitors of mycobacterial carbonic anhydrase. The findings reveal their efficacy, displaying notable selectivity toward the mycobacterial carbonic anhydrase 2 (mtCA 2) enzyme.