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Novel aminothiazole-based Naphthalimides: Design, Synthesis and Biological Evaluation

Novel Aminothiazole-based Naphthalimides: Design, Synthesis ...

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中国化学会第十四届全国有机合成化学学术研讨会

作者： Ying-Ying Chen Lavanya Gopala Jie Kang Cheng-He Zhou Institute of Bioorganic ＆ Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University

aminothiazole fragment was introduced into naphthalimide to generate a type of novel aminothiazole-based naphthalimides 3a-b through bromination and cyclization in moderate yields. Compound 3b with hydroxyethylamino group exhibited potent antibacterial activity against Staphylococcus aureus 25923（MIC = 16 μg/mL）, comparable to chloromycin.

关键词： aminothiazole naphthalimide bromination cyclization antibacterial

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Synthesis of Potential MRSA DNA-targeting Naphthalimide aminothiazoles as Novel Antimicrobial Agent

Synthesis of Potential MRSA DNA-targeting Naphthalimide Amin...

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中国化学会第十四届全国有机合成化学学术研讨会

作者： Ying-Ying Chen Lavanya Gopala Cheng-He Zhou Institute of Bioorganic ＆ Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University

A series of novel naphthalimide aminothiazoles were synthesized for the first time via multi-step reactions starting from commercial 4-bromo-1,8-naphthalic *** derivatives 2a-c were accomplished successfully by the typical Hantsch thiazole synthetic *** of the C–Br bond was achieved using alicyclic amines without any *** evaluation revealed that compound 3d could inhibit the growth of MRSA at low concentration（MIC=4μg/m L）,4-fold more potent than *** 3d could also effectively intercalate into MRSA DNA to form 3d–DNA complex,which might be responsible for the powerful bioactivity.

关键词： naphthalimide aminothiazole Hantsch thiazole synthesis antibacterial MRSA

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Synthesis of DNA-targeting Antimicrobial Carbazole aminothiazoles and Supramolecular Interaction with DNA

Synthesis of DNA-targeting Antimicrobial Carbazole Aminothia...

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全国第十八届大环化学暨第十届超分子化学学术讨论会

作者： Dinesh Addla 文思奇周成合 School of Chemistry and Chemical Engineering Southwest University

＜正＞Novel carbazole aminothiazoles as new type of DNA-targeting antimicrobial agents were designed and *** them,carbazole aminothiazole 1 could effectively inhibit the growth of MRSA with MIC value of 4μg/mL,which ... 详细信息

关键词： Carbazole aminothiazole Antimicrobial DNA

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Synthesis of Novel Aminothiazolyl Tetrahydroprotoberberrubines with Multi-targeting Antimicrobial Potentiality

Synthesis of Novel Aminothiazolyl Tetrahydroprotoberberrubin...

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中国化学会第十四届全国有机合成化学学术研讨会

作者：周成合 Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University

Berberine is a natural isoquinoline quaternary alkaloid from many kinds of naturally medicinal *** has paid extensive attention as a validated antibacterial agent in China for more than 2000 ***(THPB)as one of the berberine derivatives can improve the molecular flexibility to a certain extent,which may be conducive to enhancing the water solubility and bioavailability,and is a valid structural alternative with widely medicinal *** moiety is present in a variety of clinical drugs and the successful development of many clinical aminothiazole-based drugs has been motivating more and more efforts to develop new bioactive molecules on the basis of this ***,a series of 2-aminothiazolyl THPBs as novel antibacterial agents were designed and *** preliminary research revealed that hexyloxyl THPB derivative 9c should be a new promising multi-targeting candidate with intercalating DNA and/or damaging the cell membrane towards drug-resistant Gram-negative Acinetobacter baumanii.

关键词： aminothiazole Antibacterial Acinetobacter baumanii THPB

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Novel Potentially Antibacterial Aminothiazolyl Quinolones: Design, Synthesis, and Bioactive Evaluation

Novel Potentially Antibacterial Aminothiazolyl Quinolones: D...

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中国化学会·第十五届全国有机合成化学学术研讨会

作者： Liang-Liang Wang Narsaiah Battini 周成合 Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University CSIR-Indian Institute of Integrative Medicine (IIIM) 西南大学

A series of new aminothiazolyl quinolones as potentially antimicrobial agents have been successfully synthesized via multistep reactions starting from commercial ethyl acetoacetate and triethyl *** antibacterial evaluation revealed that most of the prepared compounds exhibited good antibacterial ***, the target compound 10 c displayed superior antibacterial activity against *** ATCC 25923 with MIC value of 8 μg/mL.

关键词： quinolone aminothiazole amide antibacterial DNA

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Aminothiazolyl norfloxacin analogs: Synthesis, antibacterial activity and biosupramolecular interactions

Aminothiazolyl norfloxacin analogs: Synthesis, antibacterial...

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全国第十九届大环化学暨第十一届超分子化学学术讨论会

作者：王亮亮 Narsaiah Battini Swetha Kameswari Maddili 周成合 Institute of Bioorganic&Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University CSIR-Indian Institute of Integrative Medicine (IIIM)

＜正＞A series of aminothiazolyl Norfloxacin analogs were designed and *** of the prepared compounds exhibited good antibacterial *** research revealed that the active molecule 3 could effectively intercalate into *** DNA to form a steady supramolecular complex, which might block DNA replication to exert their powerful antimicrobial *** Norfloxacin analogs could bind with topoisomerase Ⅳ-DNA through hydrogen bonds and π–π stacking.

关键词： norfloxacin aminothiazole supramolecular interactions DNA topoisomerase Ⅳ

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New 2-aminothiazolyl quinolones as DNA intercalators

New 2-aminothiazolyl quinolones as DNA intercalators

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全国第十八届大环化学暨第十届超分子化学学术讨论会

作者：程宇 Swetha Kameswari Maddili 周成合 School of Chemistry and Chemical Engineering Southwest University

＜正＞Quinolones are one of the most commonly prescribed antibacterial drugs and have been extensively used to combat with a number of bacterial ***,with the wide use even overuse of these drugs,the resistance to quin... 详细信息

关键词： Quinolone aminothiazole DNA intercalator

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Development of Ofloxacin Analogues and Its Antimicrobial Evaluation

Development of Ofloxacin Analogues and Its Antimicrobial Eva...

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中国化学会·第十五届全国有机合成化学学术研讨会

作者： Narsaiah Battini Liang-Liang Wang 周成合 CSIR-Indian Institute of Integrative Medicine (IIIM) Institute of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University 西南大学

A series of new 2-aminothiazolyl ofloxacin analogues were successfully designed and synthesized as multi-targeting anti-infectious agents through a convenient and efficient *** antibacterial evaluation revealed that most of the target compounds exhibited good antibacterial ***, 2-aminothiazolyl ofloxacin analogue 7 b displayed better antibacterial activity against MRSA.

关键词： ofloxacin quinolone aminothiazole antimicrobial DNA

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