Discovery of benzopyronyl imidazolidinediones as new structural skeleton of potential multitargeting antibacterial agents.

This work developed a class of unique benzopyronyl imidazolidinediones (BIs) as new structural skeleton of potential multitargeting antibacterial agents to confront dreadful Staphylococcus aureus infections. Some target compounds exhibited effective antibacterial activities against the tested strains. Especially, butyl BI 6c and 5-hydroxy BI 26d exerted excellent inhibitory activity toward Staphylococcus aureus ATCC 25923 and MRSA 43300 with a low MIC value of 0.

Comprehensive Insights Into Sulfanilamido-Based Medicinal Design and Research.

The sulfanilamido skeleton is the core part of many clinical drugs with the para-aminobenzenesulfamido scaffold. Especially as the first type of synthetic antibacterial drugs, sulfanilamides have played important roles in preventing and treating infectious diseases for more than 90 years. Increasing efforts have been contributing toward the sulfanilamido skeleton with the incorporation of various unique substituents through medicinal design, which accessed great achievements that have not only broken the classical structure-activity relationship of antibacterial sulfanilamides, but also extended the other medicinal applications of sulfanilamides except for antibacterial drugs.

Discovery of thiazolylcyanovinyl benzopyridone acids: Potential new generation antibacterial oxacins?

Here we reported a unique class of new structural thiazolylcyanovinyl benzopyridone acids (TBAs) with large potential to defeat the intractable global bacterial resistance. Some prepared TBAs demonstrated broad-spectrum antibacterial ability, especially ethyl TBA 7b gave low MIC values of 0.25-0.

Comprehensive insights into emodin compounds research in medicinal chemistry.

Emodin compounds containing three aromatic ring systems are easily to act with target sites in organisms, and thus exert numerous biological activities. Now, emodin and its derivatives have played an important role in medicinal chemistry. This work systematically reviewed the researches and developments of the whole range of emodin compounds as medicinal drugs for the reported literatures in nearly fifteen years, including anticancer, antioxidant, antiparasitic, antimicrobial, antidiabetic as well as other activities.

Merging Paired Electrolysis and Copper Catalysis Enables Electrochemical Arylation of Aziridine for the Synthesis of 1,2-Amino Tertiary Alcohols.

1,2-Amino alcohols are omnipresent in bioactive molecules. Conventional approaches to this motif require multistep reactions. Herein, we develop an electrochemical strategy for copper-catalyzed convergent paired electrolysis.

Heteroarylcyanovinyl Benzimidazoles as New Antibacterial Skeleton with Large Potential To Combat Bacterial Infections.

This work developed a class of unique heteroarylcyanovinyl benzimidazoles (HBs) as a new structural skeleton of potential multitargeting antibacterial agents to confront dreadful infections in the livestock industry. Some target compounds exhibited effective antibacterial activities against the tested strains. Especially, HB with a 5-fluorobenzimidazole ring exerted excellent inhibitory activity toward ATCC 29213 with a low MIC value of 0.

Identification of hydroxyphenyl cyanovinyl thiazoles as new structural scaffold of potential antibacterial agents.

Unique hydroxyphenyl cyanovinyl thiazoles (HCTs) as new structural scaffolds of potential antibacterial agents were developed to overcome global increasingly serious drug resistance. Some synthesized HCTs could suppress the growth of the tested strains, especially, benzothiophenyl HCT 5c exhibited superior anti-Escherichia coli activity with a lower MIC of 0.5 μg/mL to norfloxacin (MIC = 1 μg/mL).

Benzo-α-pyrone-derived multitargeting actions to enhance the antibacterial performance of sulfanilamides against Escherichia coli.

A novel class of benzopyrone-sulfanilamide hybrids was synthesized from phenols via multi-step reactions. Some prepared compounds effectively suppressed bacterial growth at low concentrations, and especially, sulfanilamide-hybridized 2-methyl-5-nitroimidazolyl benzopyrone 11c exhibited significant inhibitory potency against Escherichia coli (MIC = 0.0022 mM), which was 11-fold more active than clinical norfloxacin.

A comprehensive insight into naphthalimides as novel structural skeleton of multitargeting promising antibiotics.

The globally growing antimicrobial resistance seriously threatens human health, increasing efforts have been devoting to the development of novel antibiotics. Naphthalimides contain a special skeleton of cyclic double imides and the naphthalene framework, this unique structure can exert multitargeting abilities which are helpful to overcome the escalating issue of resistance. Therefore, research in connection with the development of naphthalimides as novel antimicrobial agents is becoming progressively active.

HFIP-driven Schmidt-type reaction enables chromone-3-carbonitriles and its applications.

Chromone-3-carbonitrile has been extensively studied in a panel of high-value transformations. However, existing protocols for the synthesis of this scaffold are often constrained by the structure of the starting materials and harsh conditions. To address these issues, we present a novel strategy that HFIP (hexafluoroisopropanol)-driven strategy, enables chromone-3-carbonitriles synthesis without undesirable side reactions.

Synthesis and antibacterial medicinal evaluation of carbothioamido hydrazonyl thiazolylquinolone with multitargeting antimicrobial potential to combat increasingly global resistance.

The global microbial resistance is a serious threat to human health, and multitargeting compounds are considered to be promising to combat microbial resistance. In this work, a series of new thiazolylquinolones with multitargeting antimicrobial potential were developed through multi-step reactions using triethoxymethane and substituted anilines as start materials. Their structures were confirmed by H NMR, C NMR and HRMS spectra.

A Unique Hybridization Route to Access Hydrazylnaphthalimidols as Novel Structural Scaffolds of Multitargeting Broad-Spectrum Antifungal Candidates.

This study developed a class of novel structural antifungal hydrazylnaphthalimidols (HNs) with multitargeting broad-spectrum potential multicomponent hybridization to confront increasingly severe fungal invasion. Some prepared HNs exhibited considerable antifungal potency; especially nitrofuryl HN (MIC = 0.001 mM) exhibited a potent antifungal activity against , which is 13-fold higher than that of fluconazole.

Cyanomethylquinolones as a New Class of Potential Multitargeting Broad-Spectrum Antibacterial Agents.

This work identified a class of cyanomethylquinolones (CQs) and their carboxyl analogues as potential multitargeting antibacterial candidates. Most of the prepared compounds showed high antibacterial activities against most of the tested bacteria, exhibiting lower MIC values (0.125-2 μg/mL) than those of clinical norfloxacin, ciprofloxacin, and clinafloxacin.

Unique aminothiazolyl coumarins as potential DNA and membrane disruptors towards Enterococcus faecalis.

Aminothiazolyl coumarins as potentially new antimicrobial agents were designed and synthesized in an effort to overcome drug resistance. Biological activity assay revealed that some target compounds exhibited significantly inhibitory efficiencies toward bacteria and fungi including drug-resistant pathogens. Especially, aminothiazolyl 7-propyl coumarin 8b and 4-dichlorobenzyl derivative 11b exhibited bactericidal potential (MBC/MIC = 2) toward clinically drug-resistant Enterococcus faecalis with low cytotoxicity to human lung adenocarcinoma A549 cells, rapidly bactericidal effects and no obvious bacterial resistance development against E.

Discovery of indolylacryloyl-derived oxacins as novel potential broad-spectrum antibacterial candidates.

The emergence of serious bacterial resistance towards clinical oxacins poses a considerable threat to global public health, necessitating the development of novel structural antibacterial agents. Seven types of novel indolylacryloyl-derived oxacins (IDOs) were designed and synthesized for the first time from commercial 3,4-difluoroaniline via an eight-step procedure. The synthesized compounds were characterized by modern spectroscopic techniques.

Hydrazyl hydroxycoumarins as new potential conquerors towards Pseudomonas aeruginosa.

A class of unique hydrazyl hydroxycoumarins (HHs) as novel structural scaffold was developed to combat dreadful bacterial infections. Some HHs could effectively suppress bacterial growth at low concentrations, especially, pyridyl HH 7 exhibited a good inhibition against Pseudomonas aeruginosa 27853 with a low MIC value of 0.5 μg/mL, which was 8-fold more active than norfloxacin.

Novel aminothiazoximone-corbelled ethoxycarbonylpyrimidones with antibiofilm activity to conquer Gram-negative bacteria through potential multitargeting effects.

The emergence of drug-resistant microorganisms threatens human health, and it is usually exacerbated by the formation of biofilm, which forces the development of new antibacterial agents with antibiofilm activity. In this work, a novel category of aminothiazoximone-corbelled ethoxycarbonylpyrimidones (ACEs) was designed and synthesized, and some of the prepared ACEs showed potent bioactivity against the tested bacteria. In particular, imidazolyl ACE 6c showed better inhibitory activity towards Acinetobacter baumannii and Escherichia coli with MIC values both of 0.

Selective α-oxidation of amides visible-light-driven iron catalysis.

Hydroxyl radicals (˙OH) as one of the highly reactive species can react unselectively with a wide range of chemicals. The ˙OH radicals are typically generated under harsh conditions. Herein, we report hydroxyl radical-induced selective -α C(sp)-H bond oxidation of amides under greener and mild conditions an Fe(NO)·9HO catalyst inner sphere pathway upon irradiation with a 30 W blue LED light strip ( = 455 nm) using NaBrO as the oxidant.

Discovery of benzopyridone cyanoacetates as new type of potential broad-spectrum antibacterial candidates.

Unique benzopyridone cyanoacetates (BCs) as new type of promising broad-spectrum antibacterial candidates were discovered with large potential to combat the lethal multidrug-resistant bacterial infections. Many prepared BCs showed broad antibacterial spectrum with low MIC values against the tested strains. Some highly active BCs exhibited rapid sterilization capacity, low resistant trend and good predictive pharmacokinetic properties.

Benzopyrone-mediated quinolones as potential multitargeting antibacterial agents.

A new type of benzopyrone-mediated quinolones (BMQs) was rationally designed and efficiently synthesized as novel potential antibacterial molecules to overcome the global increasingly serious drug resistance. Some synthesized BMQs effectively suppressed the growth of the tested strains, outperforming clinical drugs. Notably, ethylidene-derived BMQ 17a exhibited superior antibacterial potential with low MICs of 0.

Electrochemical trifluoroalkylation/annulation for the synthesis of CF-functionalized tetrahydroquinolines and dihydroquinolinones.

Tuning the electronic structure of protecting groups on the nitrogen atom of substrates has emerged as an effective strategy to achieve the tandem trifluoromethylation/C(sp)-H annulation using Langlois' reagent as the CF source for the electrochemical synthesis of functionalized tetrahydroquinolines and dihydroquinolinones.

Identification and Quantification of the Main Psychoactive Ingredients of Cannabis in Urine Using Excitation-Eemission Matrix Fluorescence Coupled with Parallel Factor Analysis.

Cannabis is the most prevalent abused substance after alcohol, and its consumption severely harms human health and thus adversely impacts society. The identification and quantification of cannabis in urine play important roles in practical forensics. Excitation-emission matrix (EEM) fluorescence spectroscopy coupled with parallel factor (PARAFAC) analysis was developed to identify and quantify the four main ingredients of cannabis in urine samples.

Identification of unique indolylcyanoethylenyl sulfonylanilines as novel structural scaffolds of potential antibacterial agents.

The increasing incidence of antibiotic resistance has forced the development of unique antimicrobials with novel multitargeting mechanisms to combat infectious diseases caused by multidrug-resistant pathogens. Structurally unique indolylcyanoethylenyl sulfonylanilines (ISs) were exploited as novel promising antibacterial agents to confront stubborn drug resistance. Some prepared ISs possessed favorable bacteriostatic action towards the tested bacteria.

Unexpected Cascade Sequence Forming the C(sp)-N/C(sp)-C(sp) Bond: Direct Access to γ-Lactam-Fused Pyridones with Anticancer Activity.

An unexpected Ugi cascade reaction was developed for the facile construction of γ-lactam-fused pyridone derivatives with high tolerance of substrates. A C(sp)-N bond and a C(sp)-C(sp) bond were formed together, accompanied by a chromone ring-opening in Ugi adducts, under the basic conditions without any metal catalyst for the whole process. Screening data of several difficult-to-inhibit cancer cell lines demonstrated that displayed a high cytotoxicity against HCT116 cells (IC = 5.