CdS Nanorod-Driven Photocatalytic Reforming of Pyridine-Functional Glycopolymers for H Evolution.

Photoreforming of biomass presents a promising approach for sustainable H production by utilizing renewable solar energy under ambient conditions. However, its application is often limited by the poor solubility of biomass-derived substrates. Herein, this challenge is addressed by synthesizing hydrophilic, electron-rich pyridine-based glycopolymers via reversible addition-fragmentation chain transfer polymerization, followed by deacetylation of glucose- and maltose-based segments.

Correction: Esterase-induced release of a theranostic prodrug in lysosomes for improved therapeutic efficacy and lower systemic toxicity.

[This corrects the article DOI: 10.1039/D5SC03783B.].

Comprehensive biological evaluation of Rheinal as a potent antimicrobial, alone and in combination with gentamicin and minocycline targeting MDR S. aureus in vitro and in vivo.

Antimicrobial resistance is recognized as a threat to healthcare systems worldwide and consequently, discovery and development of new antimicrobials is a top priority. Natural products and their derivatives have historically been an excellent source of antimicrobials. In this context, anti-bacterial activity of synthesized natural product derivative, Rheinal, was assessed against a panel of Gram-positive and Gram-negative bacterial pathogens where it exhibited potent bactericidal activity against S.

Alkaline pretreatment wastewater from lignocellulosic biomass: challenges and emerging management strategies.

Alkaline pretreatment is the most widely employed chemical process for lignocellulosic biomass, particularly at an industrial scale. However, this method generates a significant volume of complex wastewater, which contains recalcitrant organic molecules, high concentrations of biopolymers, and hazardous chemicals. These waste streams have been largely overlooked, with conventional disposal methods, such as incineration in recovery boilers, posing serious environmental and resource inefficiency concerns.

Design, synthesis, and docking studies of novel cinnamaldehyde-chalcone derivatives with anti-cancer potential and acute oral toxicity profiling.

Cinnamaldehyde is a natural compound known for its antimicrobial and anticancer properties. Fourteen novel cinnamaldehyde-chalcone analogues (5a-5n) were synthesized and evaluated for anti-cancer, anti-bacterial, and anti-fungal activities. Among these, bromoethane chalcone 5n exhibited significant cytotoxicity against DU145 (IC50: 8.

Total Synthesis of Rohitukine and Dysoline and Their Anticancer Analogues Flavopiridol and IIIM-290.

Rohitukine is a naturally occurring piperidine alkaloid that has led to the discovery of several potent CDK9/T1 inhibitors, including flavopiridol and IIIM-290. (-)-(3,4)-1-Methyl-4-(2,4,6-trimethoxyphenyl)-piperidin-3-ol serves as a crucial chiral intermediate in the synthesis of rohitukine and its analogues. In this paper, we describe the asymmetric synthesis of the chiral alcohol through the diastereoselective reduction of (+)-()-1-methyl-4-(2,4,6-trimethoxyphenyl)-piperidin-3-one in >90% yield and ≥99.

Divergent coupling of -alkynylnaphthols and -quinone monoketals through a Michael addition/intramolecular annulation cascade to access benzofuryl β-naphthols.

A CFOH-catalysed tandem cyclization of -alkynylnaphthols and -quinone monoketals is disclosed. The CFOH catalyst activates alkynylnaphthol to generate an all-carbon tetrasubstituted VQM by nucleophilic addition to quinone monoketal (Michael addition). Furthermore, the CFOH catalyst triggers -quinone monoketal to generate an electrophilic oxocarbenium cation to be captured by -alkynylnaphthol regiospecifically, resulting in the formation of an all-carbon tetrasubstituted VQM, followed by an intramolecular cyclization to afford a series of 1-(3-arylbenzofuran-2-yl)naphthalen-2-ols.

Tailored magnetic transitions and magnetocaloric properties towards room temperature in LaBiSrMnO ( = 0.05-0.25) manganites.

A series of Bi-doped manganites, , LaBiSrMnO ( = 0.05, 0.1, 0.

Lipid Nanoparticles for the Delivery of mRNA.

The development of lipid-based nanoparticles (LNPs) has significantly advanced the field of drug delivery, particularly for nucleic acids, such as mRNA being clinically used in the vaccines against COVID-19. This chapter explores the structural composition and functional properties of LNPs, including key components, such as ionizable cationic lipids, neutral/helper phospholipids, cholesterol, and lipid-anchored polyethylene glycol (PEG) constructs. The discussion includes the role of these components in improving the stability, biocompatibility, and delivery efficiency of LNPs.

Total Syntheses of β-Carboline-Based Natural Alkaloids Including Secofascaplysin A, Strychnocarpine, Rutaecarpine and Euxylophoricine A Using NHC-Catalyzed Imine Umpolung‒Oxidation.

Despite N-heterocyclic carbene (NHC) organocatalysis proceeding through umpolung reactivity mode, which has been widely explored using aldehydes, the conspicuous use of imines is still an underdeveloped area. Oxidation of imines to amides using organocatalysis is an attractive topic. Herein, we have demonstrated the application of NHC-catalyzed oxidation of a cyclic imine to the corresponding cyclic amide, proceeding through imine umpolung, as a key step in the total syntheses of biologically active natural β-carboline alkaloids of marine/plant origin, including secofascaplysin A, strychnocarpine, rutaecarpine, euxylophoricine A and also an mGluR1 antagonist.

Copper-Mediated -Selective C(sp)-H Functionalization of Carboxylic Acid Derivatives with N(sp)-H Sulfonimidamides: A Mild and General Strategy for C-N Bond Formation.

Herein, we report the copper (Cu)-mediated selective C-H bond functionalization of easily accessible N(sp)-aryl derivatives of hexavalent, diazaanalogs of sulfones such as sulfonimidamides (SIAs) with carboxylic acid derivatives decorated with oxazolidine. The -C-H bonds of aryl amides underwent a smooth reaction with the N(sp)-H bonds of a variety of sulfonimidamides (SIAs). The reaction offers a broad array of C-N(sp) bond derivatives with good functional group tolerance in good yields under mild reaction conditions in an selective manner.

Diastereoselective Synthesis of CF-Dihydrobenzo[]phenanthridones via Radical-Promoted Annulation of CF-Alkenyl Quinolones with Aldehydes.

A diastereoselective, radical-promoted annulation of CF-alkenyl quinolones with aldehydes has been achieved, providing efficient access to trifluoromethyl carbinol-functionalized dihydrobenzo[]phenanthridinones. Acyl radicals, generated in situ from the aldehydes in the presence of di--butyl peroxide (DTBP), promote this annulation. The reaction proceeds under metal-free conditions and exhibits excellent functional group tolerance.

Esterase-induced release of a theranostic prodrug in lysosomes for improved therapeutic efficacy and lower systemic toxicity.

5-Fluorouracil (5-FU) is the third most used chemotherapeutic agent. Despite being a frontline drug, it inhibits thymidylate synthase in malignant and non-malignant cells, which adds to its severe systemic toxicity. To address this, a new physiologically benign theranostic prodrug of 5-FU, named PD, has been developed by covalently linking 5-FU with a fluorophore and a lysosome-targeting morpholine moiety through an ester functionality.

Iron Single-Atom Catalyzed N-Alkylation of Amines with Alcohols via Solvent-Free Borrowing Hydrogen Strategy.

Industrial hydrogenation is a pivotal process in chemical synthesis. However, it has significant drawbacks, including high cost, safety risks associated with the use of molecular hydrogen gas, and substantial energy demands due to the need for elevated temperatures and pressures to achieve satisfactory yields. The borrowing hydrogen synthesis, which enables the transfer of hydrogen between molecules, offers a promising approach for green, one-pot synthesis of industrially important chemicals and intermediates.

Glucocorticoid receptor-targeted liposomal delivery of wnt/β-catenin pathway inhibitor selectively induces efficient colorectal tumor regression.

Wnt/β-catenin signaling pathway is a highly conserved developmental pathway. This pathway is also involved in colorectal cancer and thus its selective targeting to cancer cells, albeit the risk involved, can serve as a promising therapeutic approach. Glucocorticoid receptor (GR) is a nuclear hormone receptor present in both cancer and non-cancer cells.

Identification of malaria vulnerable zones in North East Region of India: Spatiotemporal assessment through geographical information system and self-organizing maps.

Malaria continues to pose a significant public health challenge in India, particularly in the North East Region (NER), which presents a multifaceted epidemiological landscape. Malaria control and prevention programs demonstrate greater efficiency and cost-effectiveness when they target hotspot regions. This study is aimed to explore spatiotemporal clusters of malaria incidence at the district level across NER of India.

Targeting steroid hormone receptors for anti-cancer therapy.

Steroid Hormone Receptors (SHRs) when bound to its ligand can act as transcription factors, which are responsible for transcription of important genes via hormone responsive element in our genome. Many studies have revealed the molecular mechanisms involved with SHRs. Cancer specific aberrant expression pattern of SHR and variation in their mechanism created an opportunity to specifically target SHRs for developing highly effective anti-cancer therapeutics.

Role of Repressive Histone Lysine Demethylases and Methylases in Susceptibility to Depression Using a Novel Progressive Social Defeat Stress Mouse Model.

Major depressive disorder (MDD) results from repeated and constant exposure to stress over prolonged periods. The highly variable response to stress and the low heritability suggests that MDD has a strong epigenetic basis. Studies show global dysregulation of histone modifications in both susceptible and resilient animals after chronic stress suggesting involvement of epigenetics in stress response in the brain.

Stroke Modeling and Assessment in Mice Using Internal Carotid Artery Occlusion.

The internal carotid artery occlusion (ICAO) model in mice replicates a clinically relevant subtype of stroke (mild to moderate ischemic stroke). The ICAO model represents a significant advancement in preclinical stroke research, providing a more accurate representation of human strokes caused by internal carotid artery occlusion. This model has facilitated novel insights into epigenetic modifications following stroke, specifically the dynamics of histone lysine methylation and demethylation, which are crucial in ischemia-induced brain damage and recovery.

Modeling vicarious social defeat stress in rodents for investigating emotional stress-induced depression.

Vicarious trauma, a form of emotional stress experienced by observing the suffering of others has gained prominence as a major contributor to depression and other stress-related disorders. Traditional animal models of depression such as Chronic Social Defeat Stress (CSDS) focus on physical stressors but fail to replicate the psychological dimensions of vicarious trauma. The Vicarious Social Defeat Stress (VSDS) model fills this gap by inducing emotional stress without physical injury.

Quantitative estimation of squalene levels in acute respiratory distress syndrome (ARDS) and treated lung tissues by gas chromatography-mass spectrometry.

Squalene (SQ), a naturally occurring triterpenoid, is a key precursor in steroid biosynthesis, particularly cholesterol. Its role in lung surfactant contributes to the enhancement of pulmonary function. This study aimed to quantify squalene levels in lung tissues affected by acute respiratory distress syndrome (ARDS) and in hydroalcoholic pre-treated extract (HAEGS).

Reagent-Controlled One-Pot Assembly of Divergent Indolopyrido-Quinazolinones via Uninterrupted C-Propargylation/N-Annulation.

Herein, a novel synthesis of different indolopyrido-quinazolinones by the reaction of easily accessible 2-indolyl quinazolinone with propargylic alcohols has been developed. This [4 + 2] annulation proceeds through sequential acid-catalyzed C-propargylation and base-promoted -annulation by forming C-C and C-N bonds in a one-pot operation. Interestingly, the reagent-controlled regiodivergent annulations were observed leading to diversely fused N1-C2 or C2-N3 indolopyrido-quinazolinones.

Regioselective Rh(III)-Catalyzed Spiro-Cyclization and -C(sp)-H-Annulations of Secondary Aromatic Amide with Maleimide: Construction of Spiropyrrolidinetriones and Dibenzoazocinetriones.

A facile Rh(III)-catalyzed spiro-cyclization and -(proximal) aromatic C-H activation reaction of amides with maleimides has been established via a weakly coordinating amide carbonyl acting as the directing group. This protocol features high competence, functional group tolerance, and wide-ranging substrate scope and, by slight adjustments of the reaction conditions, affords either a variety of spiropyrrolidinetrione or substituted 8-membered unsaturated lactams known as azocines in moderate yields. Additionally, the reaction is highly regioselective, furnishing mono--spiro and mono--8-membered annulated products.

Synthesis and biological evaluation of N-acyl diaryl pyrimidines (NDAPYs) as novel reverse transcriptase inhibitors.

Diaryl pyrimidines (DAPYs) are privileged structures for Non-Nucleosidic Reverse Transcriptase Inhibitors (NNRTIs), and they are considered as one of the fundamental scaffolds of existing anti-HIV agents. In this study, we designed novel molecules by the addition of a N-acyl group to the C4-position of Rilpivirine/Etravirine basic scaffold, a well-known class of DAPYs, in order to provide more interactions with K103 and E138 in Reverse Transcriptase. This was leading, as expected, to better in vitro RT inhibition, and the compounds 12c (56 %) and 12 k (49 %) demonstrated three-fold higher potency than Doravirine (17 %).

Rh(III)-Catalyzed Dual C─H Annulation of Isoquinolones and 1,6-Diynes: Access to Naphtho-Fused Polycyclic Derivatives.

Transition metal-catalyzed annulations of unsaturated systems through dual C─H activation represent a straightforward tool to access multi cyclic scaffolds. We disclose herein, a Rh(III)-catalyzed weakly coordinating inherent functional group assisted dual C─H annulation of isoquinolones with 1,6-diynes. Some necessary control experiments were conducted to untangle the reaction mechanism.