Discovery of aminopiperidine based potent & novel topoisomerase inhibitor with broad spectrum anti-bacterial activity

被引:0
作者
Desai, Jigar [2 ]
Patel, Bhaumin
Panchal, Nandini
Gite, Archana
Darji, Brijesh
Viswanathan, Kasinath
Trivedi, Jinal
Vyas, Purvi
Pawar, Vishwanath
Giri, Poonam
Sachchidanand, S.
Sharma, Rajiv
Jain, Mukul
Iyer, Pravin
Kumar, Sanjay [1 ]
机构
[1] Zydus Res Ctr, Sarkhej Bavla NH 8A Moraiya, Ahmadabad 382210, Gujarat, India
[2] Birla Inst Technol & Sci Pilani, K K Birla Goa Campus, Zuarinagar 403726, Goa, India
基金
美国国家卫生研究院;
关键词
DNA gyrase; MIC; NBTI; Topoisomerase;
D O I
10.1016/j.bmcl.2024.129911
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Bacterial DNA gyrase and topoisomerase IV inhibition has emerged as a promising strategy for the cure of infections caused by antibiotic-resistant bacteria. The N ovel B acterial T opoisomerase I nhibitors (NBTIs) bind to a different site from that of the quinolones with novel mechanism of action. This evades the existing target- mediated bacterial resistance associated with quinolones. This article presents our efforts to identify in vitro potent and broad-spectrum antibacterial agent 4l .
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页数:6
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共 23 条
  • [21] Sharma R, 2014, wipo patent, Patent No. [WO2014057415, 2014057415]
  • [22] Novel Tetrahydropyran-Based Bacterial Topoisomerase Inhibitors with Potent Anti-Gram Positive Activity and Improved Safety Profile
    Surivet, Jean-Philippe
    Zumbrunn, Cornelia
    Rueedi, Georg
    Bur, Daniel
    Bruyere, Thierry
    Locher, Hans
    Ritz, Daniel
    Seiler, Peter
    Kohl, Christopher
    Ertel, Eric A.
    Hess, Patrick
    Gauvin, Jean-Christophe
    Mirre, Azely
    Kaegi, Verena
    Dos Santos, Marina
    Kraemer, Stephanie
    Gaertner, Mika
    Delers, Jonathan
    Enderlin-Paput, Michel
    Weiss, Maria
    Sube, Romain
    Hadana, Hakim
    Keck, Wolfgang
    Hubschwerlen, Christian
    [J]. JOURNAL OF MEDICINAL CHEMISTRY, 2015, 58 (02) : 927 - 942
  • [23] Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review
    Zhao, Chuang
    Rakesh, K. P.
    Ravidar, L.
    Fang, Wan-Yin
    Qin, Hua-Li
    [J]. EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2019, 162 : 679 - 734