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Chalcone-Benzotriazole Conjugates as New Potential Antimicrobial Agents： Design, Synthesis, Biological Evaluation and Synergism with Clinical Drugs

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Chinese Journal of Chemistry 2017年第4期35卷 483-496页

作者： Hanbo Liu Lavanya Gopala srinivasa rao avula Ponmani Jeyakkumar Xinmei Peng Chenghe Zhou Rongxia Geng Institute of Bioorganic & Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing Municipality School of Chemistry and Chemical Engineering Southwest University Chongqing 400715 China School of Chemistry and Chemical Engineering Qiannan Normal University for Nationalities Duyun Guizhou 558000 China

A series of chalcone-benzotriazole conjugates as new potential antimicrobial agents were synthesized and char- acterized by ^1H NMR, ^13C NMR, IR and HRMS spectra. Antimicrobial assay manifested that some target com- pounds gave moderate to good antibacterial and antifungal activities. The N- 1 derived benzotriazole 5e and N-2 de- rived benzotriazole 6a exhibited valuable inhibitory efficacy against some tested strains. Especially, derivative 6a gave superior antifungal efficacies against C. utilis, S. cerevisiae and A. flavus （MIC^0.01, 0.02, 0.02 gmol/mL, respectively） to Fluconazole. The drug combination of compound 5e or 6a with antibacterial Chloromycin, Nor- floxacin and antifungal Fluconazole respectively showed stronger antimicrobial efficiency with less dosage and broader antimicrobial spectrum than their separated use alone. The preliminary interaction with calf thymus DNA revealed that compound 6a could intercalate into DNA to form 6a-DNA supramolecular complex which might be a factor to exert its powerful bioactivity. Molecular docking study indicated strong binding of compound 6a with DNA gyrase. The structural parameters such as molecular orbital energy and molecular electrostatic potential of compound 6a were also investigated, which provided better understanding for its good antimicrobial activity.

关键词： chalcone benzotriazole antimicrobial calf thymus DNA DNA gyrase

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Synthesis and Biological Activity of Coumarin-Metronidazole Hybrids as Potential Antibacterial Agents

Synthesis and Biological Activity of Coumarin-Metronidazole ...

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中国化学会第九届全国有机化学学术会议

作者：彭莘媚 srinivasa rao avula 周成合 Laboratory of Bioorganic & Medicinal Chemistry Key Laboratory of Applied Chemistry of Chongqing MunicipalitySchool of Chemistry and Chemical EngineeringSouthwest University CSIR-Central Drug Research Institute

＜正＞The increasing emergence of drug-resistant bacterial strains and the extensive or abused use of currently clinical antimicrobial drugs promote an urgent need to develop new effective antibacterial *** coumarins as new potential antibacterial agents with similar structural skeleton to clinical antibacterial quinolones（benzopyridones）have received specific interest,especially due to their ability against resistant *** is a well known clinical drug against

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Antimicrobial Berberine Benzimidazoles:Novel DNA Targeting Supramolecular Interaction

Antimicrobial Berberine Benzimidazoles:Novel DNA Targeting S...

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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： Ponmani Jeyakkumar 张玲 srinivasa rao avula 周成合 School of Chemistry and Chemical Engineering Southwest University CSIR-Central Drug Research Institute

＜正＞A novel series of DNA targeting antibacterial berberine-benzimidazoles were *** 5d was found to exhibit good bioactivity against antibacterial and antifungal strains in comparison with Norfloxacin and *** membrane permeabilization,Gel electrophoresis and Molecular modelling suggested the possible antibacterial mechanism against

关键词： berberine benzimidazole antibacterial DNA-targeting supramolecule

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Synthesis of Selective and High-affinity Chalcone-benzothiazole Hybrids as Brugia malayi thymidylate kinase inhibitors:in vitro alidation and Docking Studies

Synthesis of Selective and High-affinity Chalcone-benzothiaz...

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中国化学会第九届全国有机化学学术会议

作者： srinivasa rao avula Koneni V.Sashidhara 周成合 Medicinal and Process Chemistry Division CSIR-Central Drug Research Institute Laboratory of Bioorganic & Medicinal Chemistry School of Chemistry and Chemical EngineeringSouthwest University CSIR-Central Drug Research Institute Indian Institute of Chemical Technology

＜正＞In our continuing search for safe and efficacious antifilarial drug,a series of novel chalcone-benzothiazole hybrids have been synthesized and evaluated for their Brugia malayi thymidylate kinase（BmTMK）enzyme inhibition *** selectivity towards BmTMK was studied and compared to the human TMK（HsTMK）by an in silico *** of seventeen derivatives,compounds 34 and 42 showed higher interactions with the BmTMK active site.

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磺胺类药物化学研究新进展

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中国科学：化学 2016年第9期46卷 823-847页

作者：何世超 Ponmani Jeyakkumar avula srinivasa rao 王宪龙张慧珍周成合西南大学化学化工学院重庆市高校应用化学重点实验室重庆400715 临沂大学药学院山东省鲁南中药材资源开发工程技术研究中心临沂276000

磺胺是应用最早的一类化学合成抗菌药,在治疗感染性疾病中起着重要作用,因此许多研究致力于磺胺类化合物的深入开发.母体结构对氨基苯磺酰胺经化学结构修饰后呈现广泛的生物活性,显示出巨大的药用潜力和开发价值,相关研究异常活跃.结合... 详细信息

磺胺是应用最早的一类化学合成抗菌药,在治疗感染性疾病中起着重要作用,因此许多研究致力于磺胺类化合物的深入开发.母体结构对氨基苯磺酰胺经化学结构修饰后呈现广泛的生物活性,显示出巨大的药用潜力和开发价值,相关研究异常活跃.结合本课题组研究,参考国内外近5年文献,本文系统地综述了磺胺母体结构不同部位的化学结构修饰及其衍生物,包括其金属超分子络合物在抗微生物、抗癌、抗寄生虫、消炎镇痛、抗惊厥、抗青光眼、抗糖尿病、抗癫痫及相关神经性疾病和利尿药等药用研发新情况,并展望了其发展趋势.希望为广谱性、高活性和低毒性磺胺类新药分子的合理设计提供指导,为开拓磺胺类化合物的用途提供新思路.

关键词：磺胺氮杂环抗菌抗癌抗寄生虫超分子络合物

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A Facile Synthesis of Coumarin-quinolone Hybrids as Potential Novel Antimicrobial Agents

A Facile Synthesis of Coumarin-quinolone Hybrids as Potentia...

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中国化学会全国第十二届有机合成化学学术研讨会

作者： Peng,Xin-Mei Kannekanti,Vijaya Kumar srinivasa,rao avula Zhou,Cheng-He School of Chemistry and Chemical Engineering Southwest University

Quinolones containing 3-carboxylic benzopyridone skeletons are an important kind of synthetic antibacterial agents as they are generally well tolerated with good treatment effectiveness,broad antibacterial spectrum and favorable pharmacokinetic *** the first quinolone drug was discovered in 1960 s,the related structural modifications based on 3-carboxylic benzopyridone skeletons have become an extremely attractive topic in antibacterial field,and much effort has been focusing on this *** represent an important type of aromatic oxygen heterocyclic compounds with typical 1,2-benzopyrone framework and possess large π-conjugated system,desirable electronic,charge-transport properties,as well as easily structural modification of coumarin ring by various functional *** structural features result in widely potential applications of coumarin compounds in the fields of bromatology（food additives and perfumes）,material and supramolecular chemistry（dyes,luminescence materials,chemical sensors and fluorescent probes,etc.） as well as pharmacochemistry（agrochemical and medicinal agents）.Numerous efforts,including the separation and purification of naturally occurring coumarins from a variety of plants as well as artificial synthesis of coumarin compounds with novel structures and properties have been *** the importance of quinolones and coumarins,herein we reported a facile synthetic approach of the coumarin-quinolone hybrids as potential novel antimicrobial agents.

关键词： amination coumarin quinolone

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Design and Synthesis of Berberine-derived Thiazolidinediones as Multi-targeting Antimicrobial Potentiators

Design and Synthesis of Berberine-derived Thiazolidinediones...

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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： Hang Sun Jeyakkumar Ponmani Guo-Biao Zhang srinivasa rao avula 周成合 College of Chemistry and Chemical Engineering Southwest University CSIR-Central Drug Research Institute 西南大学

A series of novel berberine-derived thiazolidinediones were designed, synthesized and characterised by NMR, IR and HRMS *** antimicrobial evaluation showed that some prepared compounds exhibited excellent inhibitory activity against fungal pathogens Candida albicans ATCC 90023 and Candida parapsilosis ATCC *** strong active compounds showed multi-targeting antimicrobial potential.

关键词： berberine thiazolidinedione antimicrobial DNA HSA

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Crimean-Congo hemorrhagic fever:Pathogenesis,transmission and public health challenges

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World Journal of Virology 2025年第1期14卷 63-72页

作者： Sita Kumari Karanam Kandra Nagvishnu Praveen Kumar Uppala Sandhya Edhi srinivasa rao Varri Department of Pharmaceutical Biotechnology Maharajah’s College of PharmacyVizianagaram 535002Andhra PradeshIndia Department of Pharmacology Santhiram Medical College and General HospitalNandyal 518501Andhra PradeshIndia Department of Pharmacology Santhiram Medical College and General HospitalNandyal 518501Andhra PradeshIndia Department of Pharmaceutical AnalysisMaharajah's College of PharmacyVizianagaram 535002Andhra PradeshIndia

The dangerous Crimean-Congo hemorrhagic fever virus(CCHFV),an encapsulated negative-sense RNA virus of the family Nairoviridae,is transmitted from person to person via *** a case fatality rate between 10%to 40%,the most common ways that the disease may spread to humans are via tick bites or coming into touch with infected animals'blood or ***,the transfer of bodily fluids between individuals is another potential route of *** is a wide range of symptoms experienced by patients throughout each stage,from myalgia and fever to extreme bruising and excess *** management measures include minimising the spread of ticks from one species to another and from people to animals via the use of protective clothing,repellents,and proper animal *** order to prevent the spread of illness,healthcare workers must adhere to stringent *** the lack of an authorised vaccine,the main components of treatment now consist of preventative measures and supportive care,which may include the antiviral medicine *** still don't know very much about the virus's mechanisms,even though advances in molecular virology and animal models have improved our understanding of the pathogenesis of CCHFV.A critical need for vaccination that is both safe and effective,as well as for quick diagnosis and efficient treatments to lessen the disease's impact in areas where it is most *** steps towards lowering Crimean-Congo hemorrhagic fever mortality and morbidity rates were to anticipatethe future availability of immunoglobulin products.

关键词： Crimean-congo haemorrhagic fever Tick-borne illness Immunoglobulins Viral hemorrhagic fever Antiviral therapy

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Controversies in fecal incontinence

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World Journal of Gastroenterology 2025年第3期31卷 113-119页

作者： Andreia Albuquerque Satish S C rao School of Medicine and Biomedical Sciences Fernando Pessoa UniversityGondomar 4420-096PortoPortugal Precancerous Lesions and Early Cancer Management Research Group RISE@CI-IPO(Health Research Network) Portuguese Oncology Institute of PortoPorto 4200-072Portugal Division of Gastroenterology and Hepatology Department of Internal MedicineAugusta UniversityAugustaGA 30912United States

Fecal incontinence is a common condition that can significantly impact patients’quality of *** anal sphincter injury and anorectal surgeries are common *** ultrasound and anorectal manometry are important diagnostic tools for evaluating *** are various treatment options,including diet,lifestyle modifications,drugs,biofeedback therapy,tibial and sacral nerve neuromodulation therapy,and *** this editorial,we will discuss current controversies and novel approaches to fecal *** for asymptomatic anal sphincter defects after obstetric anal sphincter injury and in patients with inflammatory bowel disease is not generally recommended,but may be helpful in selected *** Garg incontinence score is a new score that includes the assessment of solid,liquid,flatus,mucous,stress and urge fecal *** tests such as translumbosacral anorectal magnetic stimulation and novel therapies such as translumbosacral neuromodulation therapy are promising diagnostic and treatment options,for both fecal incontinence and *** biofeedback therapy can overcome some limitations of the office-based *** muscle-derived cell implantation of the external anal sphincter has been further studied as a possible treatment *** neuromodulation may be useful in scleroderma,congenital fecal incontinence and inflammatory bowel disease but merits further study.

关键词： Fecal incontinence Endoanal ultrasound Anal sphincter defects Biofeedback Neuropathy Sacral neuromodulation

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Infrared small target detection based on spatial attention density peaks searching

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Optoelectronics Letters 2025年第2期21卷 90-96页

作者： rao Junmin LU Siyu LIU Shijian LI Fanming CAS Key Laboratory of Infrared System Detection and Imaging Technology Shanghai Institute of Technical PhysicsShanghai 200083China University of Chinese Academy of Sciences Beijing 100049China Shanghai Institute of Technical Physics Chinese Academy of SciencesShanghai 200083China School of Information Science and Technology ShanghaiTech UniversityShanghai 201210China

The detection of small targets poses a significant challenge for infrared search and tracking (IRST) systems,as they must strike a delicate balance between accuracy and *** this paper,we propose a detection algorithm based on spatial attention density peaks searching (SADPS) and an adaptive window selection ***,the difference-of-Gaussians (DoG) filter is introduced for preprocessing raw infrared ***,the image is processed by ***,an adaptive window selection scheme is applied to obtain window templates for the target scale ***,the small target feature is used to enhance the target and suppress the ***,the true targets are segmented through a *** experimental results show that compared with the seven state-of-the-art small targets detection baseline algorithms,the proposed method not only has better detection accuracy,but also has reasonable time consumption.

关键词： template searching Infrared

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