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Chinese Journal of Chemistry 2022年第22期40卷 2642-2654页

作者： Xi Yang Rasheed Syed Bo Fang cheng-he zhou Institute of Bioorganic&Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing400715China College of Pharmacy National&Local Joint Engineering Research Center of Targeted and Innovative TherapeuticsChongqing Key Laboratoryof KinaseModulators as InnovativeMedicineChongqing University of Arts and SciencesChongqing 402160China

A class of new potential antibacterial agents with distinctive pyrimidinone benzimidazole skeleton was developed through nucleophilic substitution and Biginelli reaction starting from urea,ethyl 4-chloroacetoacetate and various *** target molecules exhibited strong antibacterial activities,especially pyrimidinone benzimidazole hybrid 9e possessed the strongest inhibitory effects on the growth of *** and *** with a lower MIC value of 1μg/mL than ***,compound 9e displayed strong antibiofilm capacity,low drug resistance and excellent biosafety toward human red blood *** research revealed that compound 9e could disrupt membrane integrity and cause leakage of cellular components such as proteins and nucleic ***,compound 9e could decrease lactate dehydrogenase activity,block cell metabolism and interact with DNA in an intercalation manner.

关键词： Pyrimidinone Benzimidazole Antibacterial Resistance Membrane

Synthesis and Biological Evaluation of Quinazolonethiazoles as New Potential Conquerors towards Pseudomonas Aeruginosa

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Chinese Journal of Chemistry 2021年第5期39卷 1093-1103页

作者： Jie Wang Narsaiah Battini Mohammad Fawad Ansari cheng-he zhou Institute of Bioorgonic&Medicinal Chemistry Key Laboratory of Luminescence Analysis and Molecular Sensing(Southwest University)Ministry of EducationSchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China

Novel quinazolonthiazoles were designed and synthesized as new potential antimicrobial agents by facile multi-step procedure from o-aminobenzoic acids and 2-acetylthiazole.A series of biological evaluation showed that compound 7d was the most effective quinazolonethiazole with superior activity to reference drugs chloramphenicol and *** active molecule displayed unob-vious bacterial resistance against ***,the low toxicity to normal hepatocytes,suitable pharmacokinetics and *** preliminary biological interaction suggested that quinazolonethiazole 7d might induce bacterial death by disturbing the membrane permeability,whilst preventing bacteria from growth by integrating into DNA and binding with topoisomerase *** findings provided significant background for the further development of quinazolonethiazoles as new potential drugs in combating drug-resistant pathogens.

关键词： Thiazole Schiff bases Antimicrobial Drug design DNA

Unique Azolyl Acylhydrazonyl Hybridization of Aloe Emodins to Access Potential Antibacterial Agents

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Chinese Journal of Chemistry 2024年第15期42卷 1741-1758页

作者： Yi-Xin Wang Zhao Deng Aisha Bibi Bo Fang cheng-he zhou Institute of Bioorganic&Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China College of Pharmacy National&Local Joint Engineering Research Center of Targeted and Innovative TherapeuticsChongqing Key Laboratory of Kinase Modulators as Innovative MedicineChongqing University of Arts and SciencesChongqing 402160China

A type of unique azole-hybridized acylhydrazonyl aloe emodins(AAEs)were developed as new antibacterial agents for combating bacterial *** target AAEs showed strong antibacterial activities,especially,tetrazolylthioether AAE 27a exhibited broad antibacterial spectrum with 16-256 folds and 8-64 folds more active antibacterial efficacy than the reference drugs aloe emodin and norfloxacin,*** AAE 27a also gave low hemolysis and cytotoxicity,as well as favorable *** mechanism explorations revealed that tetrazolylthioether AAE 27a could cause bacterial membrane depolarization and damage the cell membrane,resulting in nucleic acid ***,compound 27a could intercalate into DNA to impede its replication and form supramolecular 27a-DNA gyrase complex to disturb the function of DNA *** findings would provide valuable insights for the further exploration of azolyl acylhydrazonyl aloe emodins as new potential antibacterial candidates.

关键词： Aloe emodin Hydrazone heterocycle Antibacterial Membrane damage

Discovery of Alkaloid Quinazolone-Derived Imidazolenones with Novel Structural Scaffolds of Multitargeting Antibacterial Potential

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Chinese Journal of Chemistry 2023年第24期41卷 3645-3661页

作者： Jie Dai Narsaiah Battini Zhong-Lin Zang Yan Luo cheng-he zhou Institute of Bioorganic & Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing400715 China College of Pharmacy National & Local Joint Engineering Research Center of Targeted and Innovative TherapeuticsChongqing Key Laboratory of Kinase Modulators as Innovative MedicineChongqing University of Arts and SciencesChongqing402160 China

Alkaloids are one of the prominent members in the development of new antimicrobial *** work discovered a class of alkaloid quinazolone-derived imidazolenones as novel structural type of antibacterial agents with large potential to treat severe bacterial infections in the agricultural and food *** bioactive assay displayed that some of the prepared compounds exhibited good inhibition against the tested strains,and cyclohexylimidazole-derived 7-fluoroquinazolone 22a(MIC=0.002 mmol/L)exhibited a 12.5-fold stronger inhibition than norfloxacin against Escherichia coli ATCC *** studies revealed that compound 22a not only possessed the ability of rapid bactericidal property and low propensity to develop resistance but also showed low cytotoxic effects toward red blood *** preliminary mechanism exploration indicated that compound 22a could cause membrane damage by disrupting bacterial membrane as well as depolarizing the cell ***,compound 22a could insert into DNA,which might hinder the replication of *** docking suggested that compound 22a could bind to gyrase and topoisomerase,which might be due to the suppressed expression of related ***,compound 22a could disorder the metabolism and stimulate the production of reactive oxygen species to affect bacterial *** series of investigations suggested the promise of alkaloid quinazolone-derived imidazolenones as novel multitargeting antibacterial candidates for treatment of bacterial infections.

关键词： Quinazolone Imidazole Antibacterial Enone DNA

Coumarin-derived azolyl ethanols:synthesis,antimicrobial evaluation and preliminary action mechanism

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Science China Chemistry 2016年第7期59卷 878-894页

作者： Xin-Mei Peng Kannekanti Vijaya Kumar Guri L.V. Damu cheng-he zhou Institute of Bioorganic & Medicinal Chemistry Key Laboratory of Applied chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China

A series of coumarin-derived azolyl ethanols including imidazolyl,triazolyl,tetrazolyl,benzotriazolyl,thiol-imidazolyl and thiol-triazolyl ones were conveniently synthesized and characterized by IR,~1H NMR,^(13)C NMR and high-resolution mass spectra(HRMS) *** of the prepared compounds showed appropriate logP_(ow) values and effective antibacterial and antifungal ***,compound 14 with bis-triazolyl ethanol group exhibited low minimal inhibitory concentration(MIC)value of 8 μg/mL against MRSA,which was comparable or even superior to reference drugs Norfloxacin(MIC=8μg/mL)and Chloramphenicol(MIC=16μg/mL).It could also effectively inhibit the growth of the tested fungal strains compared to *** binding studies of coumarin 14 with calf thymus DNA were investigated by UV-Vis absorption and fluorescence *** was found that compound 14 could interact with calf thymus DNA by groove binding to form14-DNA complex via both hydrogen bonds and van der Waals force,which might be the factor to exert the powerful antimicrobial activity.

关键词： coumarin imidazole triazole tetrazole antibacterial antifungal calf thymus DNA

Novel benzimidazole derived naphthalimide triazoles: synthesis, antimicrobial activity and interactions with calf thymus DNA

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Science China Chemistry 2015年第3期58卷 483-494页

作者： Yun-Lei Luo Kishore Baathulaa Vijaya Kumar Kannekanti cheng-he zhou Gui-Xin Cai Key Laboratory of Applied Chemistry of Chongqing Municipality Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical Engineering Southwest University Department of Chemistry Kakatiya University Indian Institute of Chemical Technology

A novel series of benzimidazole derived naphthalimide triazoles and some corresponding triazoliums have been successfully synthesized and characterized by 1H NMR, 13 C NMR, 1H-1H COSY, IR and HRMS spectra. All the new compounds were screened for their antimicrobial activities in vitro by two-fold serial dilution. 2-Chlorobenzyl triazolium 8g and compound 9b with octyl group exhibited the best antibacterial activities among all the tested compounds, especially against S. aureus with inhibitory concentration of 2 μg/mL which was equipotent potency to Norfloxacin(MIC=2 μg/mL) and more active than Chloromycin(MIC=7 μg/mL). Triazoliums 8g and 8f bearing 3-fluorobenzyl moiety displayed the best antifungal activities(MIC=2-19 μg/mL) against all the tested fungal strains without being toxic to PC12 cell line within concentration of 128 μg/m L. Further investigations by fluorescence and UV-Vis spectroscopic methods revealed that the compound 8g could effectively intercalate into calf thymus DNA to form the 8g-DNA complex which could block DNA replication, exerting powerful antimicrobial activities.

关键词： naphthalimide benzimidazole triazole antibacterial antifungal calf thymus DNA

Design and Synthesis of Sulfanilamide Aminophosphonates as Novel Antibacterial Agents towards Escherichia coli

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Chinese Journal of Chemistry 2021年第8期39卷 2251-2263页

作者： Juan Wang Mohammad Fawad Ansari Jian-Mei Lin cheng-he zhou Institute of Bioorganic&Medicinal Chemistry Key Laboratory of Luminescence Analysis and Molecular Sensing(Southwest University)Ministry of EducationSchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China School of Medicine University of Electronic Science and Technology of ChinaChengduSichuan 610072China

The limit ability of traditional antibiotics to treat drug resistant bacteria calls for new therapeutic alter natives.A class of unique sul-fanilamide aminophosphonates as new potential agents against microbes was syn... 详细信息

关键词： Sulfonamides Aminophosphonate Imidazole Membranes DNA

Synthesis and anticancer activities of porphyrin induced anticancer drugs

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Chinese Chemical Letters 2007年第11期18卷 1331-1334页

作者： Dong Hong Li Jun Lin Diao Ke Gui Yu cheng he zhou State Key Laboratory of Trauma Burn and Combined Injury the 2nd Department of Research Institute of Surgery the third Military Medical University Chotigqing 400042 China School of Chemistry and Chemical Engineering Southwest University Chongqing 400715 China

In view of the property of porphyrin＇s accumulation selectively in tumor, the ftorafur was modified by binding a porphyrin block to improve its tumor targeting and reduce its side effects. These novel porphyrin derivatives and metal compounds were synthesized under mild conditions with satisfactory yield, and the constructions of all these new compounds were characterized by UV, IR, MS, ^1H NMR spectra and elementary analysis. Their anticancer activities were evaluated by MTT assay; the results indicated that the anticancer activities of compounds 4a-e were twice as high as that of ftorafur.

关键词： Porphyrin Ftorafur Synthesis Anticancer activities

Study on the synthesis and antimicrobial activity of novel cationic porphyrins

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Chinese Chemical Letters 2009年第4期20卷 411-414页

作者： Ke Gui Yu Dong Hong Li cheng he zhou Jun Lin Diao State Key laboratory of Trauma Burn and Combined Injury The 2nd Department of Research Institute of Surgery Dapin Hospital Third Military Medical University Chongqing 400042 China School of Chemistry and Chemical Engineering Southwest University Chongqing 400715 China

A novel series of quaternary ammonium cationic derivatives based on tetrapyridyl-porphyrin was synthesized. All the compounds were evaluated for their in vitro antibacterial activities against S. aureus, E. coli and P. aeruginosa, and antifungal activities against C. albicans, where microorganisms were exposed and unexposed to the irradiation. The results revealed that some of these compounds, especially, 3a and 4a displayed satisfactory antibacterial activity against Gram-positive bacteria S. aureus and moderate antifungal activity against C. albicans. Unfortunately, Gram-negative bacteria P aeruginasa was resistant to all compounds. The antimicrobial activity was found to be sensitive to the functional groups attached on the aromatic ring and the complex metal in the porphyrin ring, and decreased with the increase of electron-withdrawing capability of the functional groups. These preliminary results suggested that the remarkable antibacterial efficiency against S. aureus makes these substances promising antimicrobial agents.

关键词： Cationic porphyrin Synthesis Antimicrobial activity Gram-positive bacteria Gram-negative bacteria Fungus

Design,synthesis and biological evaluation of amino organophosphorus imidazoles as a new type of potential antimicrobial agents

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Science China Chemistry 2017年第6期60卷 769-785页

作者： Wei-Wei Gao Syed Rasheed VijaiKumarReddy Tangadanchu Yi Sun Xin-Mei Peng Yu cheng Feng-Xiu Zhang Jian-Mei Lin cheng-he zhou Institute of Bioorganic&Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest UniversityChongqing 400715China School of Medicine University of Electronic Science and Technology of China Chengdu 610072China

A series of amino organophosphorus imidazoles were designed and synthesized as a novel structural type of antimicrobial *** evaluation in vitro showed that compound 3f exhibited equipotent or superior anti-methicillin-resistant Staphylococcus aureus(anti-MRSA) and anti-S. cerevisiae efficiencies(minimal inhibitory concentration(MIC)=2 μg/mL) to clinical drugs,and the combinations with antibacterial or antifungal drugs enhanced the antimicrobial efficiency. Highly active molecule 3f showed low propensity for bacteria to develop resistance, and the preliminary action mechanism studies demonstrated that 3f was membrane-active, but had no significant intercalation towards MRSA DNA. The computational study on 3f reasonably explained its high antimicrobial activity. Experimental data revealed that ground-state 3f-HSA complexes were formed mainly through hydrophobic interactions and hydrogen bonds with a spontaneous process, and the non-radioactive energy transfer from HSA to 3f occurred beyond F鰎ster resonance energy transfer theory. The participation of metal ions in 3f-HSA supramolucular system could increase the concentration of free compound 3f, and shorten its storage time and half-life in the blood to improve the maximum antimicrobial efficacy.

关键词： organophosphorus imidazole antibacterial antifungal HSA