DeepBLI: A Transferable Multichannel Model for Detecting β-Lactamase-Inhibitor Interaction
Sign Up to like & getrecommendations! Published in 2022 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.2c01008
Abstract: Pathogens producing β-lactamase pose a great challenge to antibiotic-resistant infection treatment; thus, it is urgent to discover novel β-lactamase inhibitors for drug development. Conventional high-throughput screening is very costly, and structure-based virtual screening is limited… read more here.
Keywords: lactamase inhibitor; transferable multichannel; inhibitor; deepbli transferable ... See more keywords
Orally Absorbed Derivatives of the β-Lactamase Inhibitor Avibactam. Design of Novel Prodrugs of Sulfate Containing Drugs.
Sign Up to like & getrecommendations! Published in 2018 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.8b01389
Abstract: Only one FDA-approved β-lactamase inhibitor has ever been orally available: clavulanic acid, approved in 1984. Avibactam, approved by FDA in 2015, is the first of a new class of BLIs called diazabicyclooctanes, or "DBOs". This… read more here.
Keywords: inhibitor; clavulanic acid; lactamase inhibitor; orally absorbed ... See more keywords
Metallo-β-Lactamase Inhibitor Phosphonamidate Monoesters
Sign Up to like & getrecommendations! Published in 2022 at "ACS Omega"
DOI: 10.1021/acsomega.1c06527
Abstract: Being the second leading cause of death and the leading cause of disability-adjusted life years worldwide, infectious diseases remain—contrary to earlier predictions—a major consideration for the public health of the 21st century. Resistance development of… read more here.
Keywords: lactamase inhibitor; phosphonamidate monoesters; inhibitor phosphonamidate; metallo lactamase ... See more keywords
β-lactam/β-lactamase inhibitor combinations: an update.
Sign Up to like & getrecommendations! Published in 2018 at "MedChemComm"
DOI: 10.1039/c8md00342d
Abstract: Antibiotic resistance caused by β-lactamase production continues to present a growing challenge to the efficacy of β-lactams and their role as the most important class of clinically used antibiotics. In response to this threat however,… read more here.
Keywords: lactamase inhibitors; class; inhibitor combinations; lactam lactamase ... See more keywords
Synthesis and control of process-related impurities in the β-lactamase inhibitor drug substance zidebactam
Sign Up to like & getrecommendations! Published in 2023 at "Synthetic Communications"
DOI: 10.1080/00397911.2023.2209677
Abstract: Abstract Zidebactam is a novel extended spectrum β-lactamase inhibitor (ESBLI). It’s combination with cefepime (WCK 5222) is in phase III clinical studies. Five process impurities were found in zidebactam (1) drug substance using process development… read more here.
Keywords: lactamase inhibitor; synthesis control; drug substance; process ... See more keywords
The latest advances in β-lactam/β-lactamase inhibitor combinations for the treatment of Gram-negative bacterial infections
Sign Up to like & getrecommendations! Published in 2019 at "Expert Opinion on Pharmacotherapy"
DOI: 10.1080/14656566.2019.1660772
Abstract: ABSTRACT Introduction: Antimicrobial resistance in Gram-negative pathogens is a significant threat to global health. β-Lactams (BL) are one of the safest and most-prescribed classes of antibiotics on the market today. The acquisition of β-lactamases, especially… read more here.
Keywords: gram; gram negative; treatment; bli combinations ... See more keywords
677. Activity of Novel β-Lactamase Inhibitor QPX7728 Combined with β-Lactam Agents When Tested Against Carbapenem-Resistant Enterobacteriaceae (CRE) Isolates
Sign Up to like & getrecommendations! Published in 2019 at "Open Forum Infectious Diseases"
DOI: 10.1093/ofid/ofz360.745
Abstract: Abstract Background CREs have been described worldwide and these isolates are often multidrug resistant with few therapeutic options remaining active against them. New β-lactam (BL)/β-lactamase inhibitor (BLI) combinations recently approved are active against KPC and… read more here.
Keywords: cre isolates; qpx; lactamase inhibitor; etp ... See more keywords
Safety, Pharmacokinetics, and Drug-Drug Interaction Potential of Intravenous Durlobactam, a β-Lactamase Inhibitor, in Healthy Subjects
Sign Up to like & getrecommendations! Published in 2020 at "Antimicrobial Agents and Chemotherapy"
DOI: 10.1128/aac.00071-20
Abstract: Durlobactam (DUR; also known as ETX2514) is a novel β-lactamase inhibitor with broad activity against Ambler class A, C, and D β-lactamases. Addition of DUR to sulbactam (SUL) in vitro restores SUL activity against clinical… read more here.
Keywords: drug; imi cil; lactamase inhibitor; dur ... See more keywords
New β-Lactam–β-Lactamase Inhibitor Combinations
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DOI: 10.1128/cmr.00115-20
Abstract: The limited armamentarium against drug-resistant Gram-negative bacilli has led to the development of several novel β-lactam–β-lactamase inhibitor combinations (BLBLIs). In this review, we summarize their spectrum of in vitro activities, mechanisms of resistance, and pharmacokinetic-pharmacodynamic… read more here.
Keywords: inhibitor combinations; lactam lactamase; lactamase inhibitor; drug ... See more keywords
Inhibiting Mycobacterium abscessus Cell Wall Synthesis: Using a Novel Diazabicyclooctane β-Lactamase Inhibitor To Augment β-Lactam Action
Sign Up to like & getrecommendations! Published in 2022 at "mBio"
DOI: 10.1128/mbio.03529-21
Abstract: Durlobactam (DUR) is a potent inhibitor of BlaMab and provides protection of amoxicillin and imipenem against hydrolysis. DUR has intrinsic activity and forms stable acyl-enzyme complexes with LdtMab2 and LdtMab4. The ability of DUR to… read more here.
Keywords: inhibitor; intrinsic activity; lactamase inhibitor; dur ... See more keywords
Efficacy and safety of novel carbapenem–β-lactamase inhibitor combinations: Results from phase II and III trials
Sign Up to like & getrecommendations! Published in 2022 at "Frontiers in Cellular and Infection Microbiology"
DOI: 10.3389/fcimb.2022.925662
Abstract: Objectives The addition of novel β-lactamase inhibitors to carbapenems restores the activity against multidrug-resistant Gram-negative bacteria. The aim of this study was to summarize the evidence on the efficacy and safety of novel carbapenem–β-lactamase inhibitor… read more here.
Keywords: novel carbapenem; lactamase inhibitor; carbapenem lactamase; inhibitor combinations ... See more keywords