Design, Synthesis, and Antibacterial Activities of Multi-Functional C-Functionalized 1,4-Naphthoquinonyl Organoseleniums.

A practical and efficient reaction for C-selenylation of 1,4-naphthoquinones has been explored. This coupling reaction of two redox structural motifs, such as 2-bromo-1,4-naphthoquinone with diaryldiselenide/ebselen has been achieved by using sodium borohydride reducing agent at room temperature. Using this approach, several 2-selenylated-1,4-naphthoquinones were obtained in moderate to good yields and thoroughly characterized by multinuclear (H, C, and Se) NMR, cyclic voltammetry, and mass spectrometry.

Development of naphthalimide hydrazide derivatives as potent antibacterial agents against carbapenem-resistant .

In this work, a novel series of naphthalimide hydrazide derivatives were designed, synthesized and evaluated against a bacterial pathogen panel. Most of the compounds were found to exhibit potent antibacterial activity against carbapenem-resistant BAA 1605, with MIC ranging from 0.5 to 16 μg mL.

Corannulene Amino Acid-Derived Water-Soluble Amphiphilic Buckybowls as Broad-Spectrum Membrane Targeting Antibacterial Agents.

To date, the use of corannulene has been restricted in the area of material science, but its application in biomedical research has yet to be established due to its nonsolubility in an aqueous environment and synthetic infeasibility. Herein, we detail the development of a new family of highly curved π-conjugated corannulene-containing unnatural α-amino acid (CAA) derivatives to overcome this challenge. These CAAs have been extended as novel constituents for the synthesis of corannulene-containing water-soluble cationic peptides (CCPs), which display inhibitory activity against broad-spectrum pathogenic bacteria along with drug-resistant bacteria via a membrane-damaging mechanism.

Facile one-pot synthesis of N-pyridinylaminonaphthol derivatives and their antibacterial evaluation against multidrug-resistant Staphylococcus aureus.

The escalating severity of the menace posed by bacterial resistance has rendered the existing antibiotics less effective, thus necessitating the discovery of new antibacterial agents. The current study reports the exploration of substituted N-pyridinylaminonaphthols produced by a straightforward, one-pot multicomponent reaction process as antibacterial agents. The synthesized derivatives were assessed in vitro for their antibacterial properties against a panel of bacterial pathogens.

Synthesis and biological evaluation of new naphthalimide-thiourea derivatives as potent antimicrobial agents active against multidrug-resistant and .

The emergence of antibiotic resistance to and , particularly MRSA, VRSA, and drug-resistant tuberculosis, poses a serious threat to human health. Towards discovering new antibacterial agents, we designed and synthesized a series of new naphthalimide-thiourea derivatives and evaluated them against a panel of bacterial strains consisting of , , , , and various mycobacterial pathogens. Compounds 4a, 4l, 4m, 4n, 4q, 9f, 9l, 13a, 13d, 13e, 17a, 17b, 17c, 17d, and 17e demonstrated potent antibacterial activity against with MIC 0.

Pyridine-2,6-Dicarboxamide Proligands and their Cu(II)/Zn(II) Complexes Targeting Staphylococcus Aureus for the Attenuation of In Vivo Dental Biofilm.

In the pursuit to combat stubborn bacterial infections, particularly those stemming from gram-positive bacteria, this study is an attempt to craft a precision-driven platform characterized by unparalleled selectivity, specificity, and synergistic antimicrobial mechanisms. Leveraging remarkable potential of metalloantibiotics in antimicrobial applications, herein, this work rationally designs, synthesizes, and characterizes a new library of Pyridine-2,6-dicarboxamide ligands and their corresponding transition metal Cu(II)/Zn(II) complexes. The lead compound L demonstrates robust antibacterial properties against Staphylococcus aureus (Minimum Inhibitory Concentration (MIC) = 2-16 µg mL), methicillin and vancomycin-resistant S.

Assessment of Safe Drinking Water Handling Practices in Households of Northern India: A Cross-Sectional Study.

Background Waterborne diseases are the most common form of infectious disease, spreading from contaminated water, especially in a developed country. These diseases are a major concern for the environment and public health. The living conditions in developing countries like India affect the water-handling practices, which make the population vulnerable to waterborne diseases.

Antimicrobial peptide mimetic minimalistic approach leads to very short peptide amphiphiles-gold nanostructures for potent antibacterial activity.

Strategically controlling concentrations of lipid-conjugated L-tryptophan (vsPA) guides the self-assembly of nanostructures, transitioning from nanorods to fibres and culminating in spherical shapes. The resulting Peptide-Au hybrids, exhibiting size-controlled 1D, 2D, and 3D nanostructures, show potential in antibacterial applications. Their high biocompatibility, favourable surface area-to-volume ratio, and plasmonic properties contribute to their effectiveness against clinically relevant bacteria.

Barriers of household toilet utilization among toilet owners in a rural area of Northern India: An analytical cross-sectional study.

Background: Open defecation continues to prevail among toilet owners despite effective implementation of the Swachh Bharat Mission (Gramin). We conducted this study to determine toilet utilization rates and learn about the barriers to toilet use in the rural areas. By understanding the barriers, physicians can provide targeted education and become better equipped to manage their patients' conditions and advocate for their demands.

Estimation of Access to Safe Drinking Water to Households in Etawah District: A Cross-Sectional Study.

Context: Unsafe drinking water causes diarrheal disease and environmental enteropathy. The quality of water is determined by its physical, chemical, and biological characteristics. Water sources have a significant impact on household members' health, particularly children.

One-pot synthesis of thioethers from indoles and -quinone methides using thiourea as a sulfur source.

Thiourea is an inexpensive and user friendly sulfur reagent that acts as a sulfur source. A simple and efficient protocol has been developed to access thioethers by reacting indoles with -quinone methides using thiourea as the sulfur source. In our experiments, the reaction apparently proceeded through an -(3-indolyl)isothiuronium iodide intermediate and subsequent generation of indolethiol that attacked the 1,6 position of -quinone methides to give desired thioethers in good to excellent yields.

Discovery of benzoxazole-thiazolidinone hybrids as promising antibacterial agents against and species.

Antibiotic resistance is rapidly exacerbating the unceasing rise in nosocomial infections caused by drug-resistant bacterial pathogens such as methicillin-resistant (MRSA), carbapenem-resistant (CRE) and vancomycin-resistant (VRE). Therefore, there is a dire need for new therapeutic agents that can mitigate the unbridled emergence of drug-resistant pathogens. In the present study, several benzoxazole-thiazolidinone hybrids (BT hybrids) were synthesized and evaluated for their antibacterial activity against the ESKAP pathogen panel.

Pyrrole-thiazolidinone hybrids as a new structural class of broad-spectrum anti-infectives.

A series of pyrrole-thiazolidinone hybrids was designed, synthesized and evaluated for activities against ESKAP bacteria panel and mycobacterial pathogens. From the series, compound 9d showed prominent activity against S. aureus (MIC = 0.

Mechanochemical Studies on Coupling of Hydrazines and Hydrazine Amides with Phenolic and Furanyl Aldehydes-Hydrazones with Antileishmanial and Antibacterial Activities.

Hydrazone compounds represent an important area of research that includes, among others, synthetic approaches and biological studies. A series of 17 hydrazones have been synthesized by mechanochemical means. The fragments chosen were phenolic and furanyl aldehydes coupled with 12 heterocyclic hydrazines or hydrazinamides.

Synthesis of tryptanthrin appended dispiropyrrolidine oxindoles and their antibacterial evaluation.

The synthesis of sixteen tryptanthrin appended dispiropyrrolidine oxindoles, employing [3 + 2] cycloaddition of tryptanthrin-derived azomethine ylides with isatilidenes, and their detailed antibacterial evaluation is described. The antibacterial activities of the compounds were evaluated against ESKAPE pathogens and clinically relevant drug-resistant MRSA/VRSA strains, from which the bromo-substituted dispiropyrrolidine oxindole 5b (MIC = 0.125 μg mL) was found to be a potent molecule against ATCC 29213 with a good selectivity index.

β-Turn editing in Gramicidin S: Activity impact on replacing proline α-carbon with stereodynamic nitrogen.

Gramicidin S, natural antimicrobial peptide is used commercially in medicinal lozenges for sore throat and Gram-negative and Gram-positive bacterial infections. However, its clinical potential is limited to topical applications because of its high red blood cells (RBC) cytotoxicity. Given the importance of developing potential antibiotics and inspired by the cyclic structure and druggable features of Gramicidin S, we edited proline α-carbon with stereodynamic nitrogen to examine the direct impact on biological activity and cytotoxicity with respect to prolyl counterpart.

Targeting multidrug resistant Staphylococcus aureus with cationic chlorpromazine-peptide conjugates.

Antimicrobial resistance is a serious public health risk. Its severity is fueled on an unprecedented scale, necessitating the demand for novel antimicrobial scaffolds aimed at novel targets. Herein, we present cationic chlorpromazine peptide conjugates that are rationally intended to targetmultidrug-resistant (MDR) bacteria.

Water-soluble copper pyrithione complexes with cytotoxic and antibacterial activity.

Copper Pyrithione, [Cu(PyS)] has shown excellent biological activity against cancer cells and bacterial cells, however, it has extremely low aqueous solubility, limiting its applicability. Herein, we report a series of PEG-substituted pyrithione copper(II) complexes with significantly increased aqueous solubility. While long PEG chains lead to a decrease in bioactivity, the addition of short PEG chains leads to improved aqueous solubility with retention of activity.

Silver-Nanoparticle-Embedded Short Amphiphilic Peptide Nanostructures and Their Plausible Application to Reduce Bacterial Infections.

The microbiota-gut-brain axis (GBA) plays a critical role in the development of neurodegenerative diseases. Dysbiosis of the intestinal microbiome causes a significant alteration in the gut microbiota of Alzheimer's disease (AD) patients, followed by neuroinflammatory processes. Thus, AD beginning in the gut is closely related to an imbalance in gut microbiota, and hence a multidomain approach to reduce this imbalance by exerting positive effects on the gut microbiota is needed.

Design and synthesis of novel halogen rich salicylanilides as potential antileishmanial agents.

The available therapeutic treatment for leishmaniasis is inadequate and toxic due to side effects, expensive and emergence of drug resistance. Affordable and safe antileishmanial agents are urgently needed and toward this objective, we synthesized a series of 32 novel halogen rich salicylanilides including niclosamide and oxyclozanide and investigated their antileishmanial activity against amastigotes of Leishmania donovani. In vitro data showed fifteen compounds inhibited intracellular amastigotes with an IC of below 5 μM and selectivity index above 10.

Hospital-Based Retrospective Cross-sectional Study to Analyse the Causes of Maternal Deaths at a Tertiary Health Care Facility.

Context: Maternal mortality is considered a key health indicator of Maternal and Child Health. Considering the fact that complications are preventable and most of them are modifiable, the study has been planned to analyse maternal deaths in order to suggest recommendations for preventing it. There are various delays according to the three-delay model at primary and secondary level; therefore, interventions are needed at those levels to prevent maternal deaths.

Serendipitous identification of phenylhydrazine derivatives as potent inhibitors of carbapenem-resistant .

In the authors' previous study, 4-(2-((3-methyl-4-oxo-2-thioxo/dioxothiazolidin-5-ylidene) methyl) hydrazineyl) benzonitriles were found to demonstrate potent antibacterial activity against . Interestingly, the aforementioned compounds contain a 4-cyanophenylhydrazine motif. Intrigued by this observation, the authors focused on preparing a library of 4-cyanophenylhydrazine derivatives and studied their detailed antibacterial potential.

Pyrvinium pamoate potentiates levofloxacin against levofloxacin-resistant .

Drug repurposing is a viable approach to expediting the tedious conventional drug discovery process, given rapidly increasing bacterial resistance. In this context, we have repurposed pyrvinium pamoate (PP) for its antibacterial activity against . US FDA-approved non-antibiotics were screened against clinically relevant bacterial pathogens to identify antibacterials.