{"title":"潜在的下一代抗菌剂的发现和开发目标","authors":"Pooja Gupta, Pushplata Yadav, Manjul Lata, Shivani Chaudhary, Vrushti Telang, Raj Kishore, Jai Kishan, Kamini Goswami, Jesu Arockiaraj, Ravithej Singh L, Anamika Sharma, Mukesh Pasupuleti","doi":"10.1016/j.ejmech.2025.118188","DOIUrl":null,"url":null,"abstract":"Inappropriate and excessive use of antimicrobials, in addition to evolutionary process, lead to the development of antimicrobial-resistant strains at an unprecedented accelerated rate, leading to global public health crisis. Antimicrobial resistantance is a global challenge that not only causes mortality and disability but also carries, affect all the countries regardless of wealth, health care infrastructure and socio-economic conditions leading to huge economic loss. Recent studies have indicated that we are moving back to the post-antibiotic era at a faster rate as our novel antibacterial armamentarium has almost reached zero. Unfortunately, lead molecules in the preclinical pipeline are unable to tackle drug-resistant bacteria as these are either derivative of clinically used antibiotics or against the target for which resistance development has already started. Currently, the need for development of new antimicrobials with novel mechanisms is pressing more than ever due to the impending global clinical crisis and no new antibacterial agent with novel target has been added in the last 10 years. Herein, we summarized 28 feasible unexplored targets for the development of novel antibacterial agents. As antimicrobial resistance is a universal problem, this review lists novel molecules that are reported to have antibacterial activity and their potential sites in the past five years so that researchers can start on building those scaffolds to develop safe, effective and affordable drugs. Furthermore, we provide an overview of the key gaps, issues and approaches that need to be revisited is presented. This review emphasis strategy that help in harmonization of procedures and also to reduce the attrition rate in the next generation antibacterial drug development process.","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"30 1","pages":""},"PeriodicalIF":5.9000,"publicationDate":"2025-09-24","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Potential next generation targets for antibacterial agent’s discovery and development\",\"authors\":\"Pooja Gupta, Pushplata Yadav, Manjul Lata, Shivani Chaudhary, Vrushti Telang, Raj Kishore, Jai Kishan, Kamini Goswami, Jesu Arockiaraj, Ravithej Singh L, Anamika Sharma, Mukesh Pasupuleti\",\"doi\":\"10.1016/j.ejmech.2025.118188\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Inappropriate and excessive use of antimicrobials, in addition to evolutionary process, lead to the development of antimicrobial-resistant strains at an unprecedented accelerated rate, leading to global public health crisis. Antimicrobial resistantance is a global challenge that not only causes mortality and disability but also carries, affect all the countries regardless of wealth, health care infrastructure and socio-economic conditions leading to huge economic loss. Recent studies have indicated that we are moving back to the post-antibiotic era at a faster rate as our novel antibacterial armamentarium has almost reached zero. Unfortunately, lead molecules in the preclinical pipeline are unable to tackle drug-resistant bacteria as these are either derivative of clinically used antibiotics or against the target for which resistance development has already started. Currently, the need for development of new antimicrobials with novel mechanisms is pressing more than ever due to the impending global clinical crisis and no new antibacterial agent with novel target has been added in the last 10 years. Herein, we summarized 28 feasible unexplored targets for the development of novel antibacterial agents. As antimicrobial resistance is a universal problem, this review lists novel molecules that are reported to have antibacterial activity and their potential sites in the past five years so that researchers can start on building those scaffolds to develop safe, effective and affordable drugs. Furthermore, we provide an overview of the key gaps, issues and approaches that need to be revisited is presented. This review emphasis strategy that help in harmonization of procedures and also to reduce the attrition rate in the next generation antibacterial drug development process.\",\"PeriodicalId\":314,\"journal\":{\"name\":\"European Journal of Medicinal Chemistry\",\"volume\":\"30 1\",\"pages\":\"\"},\"PeriodicalIF\":5.9000,\"publicationDate\":\"2025-09-24\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"European Journal of Medicinal Chemistry\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1016/j.ejmech.2025.118188\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.ejmech.2025.118188","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
Potential next generation targets for antibacterial agent’s discovery and development
Inappropriate and excessive use of antimicrobials, in addition to evolutionary process, lead to the development of antimicrobial-resistant strains at an unprecedented accelerated rate, leading to global public health crisis. Antimicrobial resistantance is a global challenge that not only causes mortality and disability but also carries, affect all the countries regardless of wealth, health care infrastructure and socio-economic conditions leading to huge economic loss. Recent studies have indicated that we are moving back to the post-antibiotic era at a faster rate as our novel antibacterial armamentarium has almost reached zero. Unfortunately, lead molecules in the preclinical pipeline are unable to tackle drug-resistant bacteria as these are either derivative of clinically used antibiotics or against the target for which resistance development has already started. Currently, the need for development of new antimicrobials with novel mechanisms is pressing more than ever due to the impending global clinical crisis and no new antibacterial agent with novel target has been added in the last 10 years. Herein, we summarized 28 feasible unexplored targets for the development of novel antibacterial agents. As antimicrobial resistance is a universal problem, this review lists novel molecules that are reported to have antibacterial activity and their potential sites in the past five years so that researchers can start on building those scaffolds to develop safe, effective and affordable drugs. Furthermore, we provide an overview of the key gaps, issues and approaches that need to be revisited is presented. This review emphasis strategy that help in harmonization of procedures and also to reduce the attrition rate in the next generation antibacterial drug development process.
期刊介绍:
The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers.
A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.