Abstract:
:Antimicrobial resistance is one of the greatest challenges facing the world today. In the United States alone, it is responsible for the death of more than 20,000 people each year. DNA gyrase, a well-validated drug target, is involved in bacterial DNA replication, repair and decatenation. Currently, the fluoroquinolone class of antibacterials act via inhibition of the DNA gyrase enzyme. However, their efficacy is hindered by the increasing incidence of antimicrobial resistance. Therefore, in this review, we provide an account regarding the structure of DNA gyrase and quinoline and non-quinolone inhibitors published within the last five years (2015-2019). Further, we also discuss molecular interactions and structure-activity relationship studies of the published inhibitors.
journal_name
Eur J Med Chemjournal_title
European journal of medicinal chemistryauthors
Dighe SN,Collet TAdoi
10.1016/j.ejmech.2020.112326subject
Has Abstractpub_date
2020-08-01 00:00:00pages
112326eissn
0223-5234issn
1768-3254pii
S0223-5234(20)30295-6journal_volume
199pub_type
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