Βeta-Lactams as Clinically Active Medicines

Basu, Shibani; Banik, Bimal K.

doi:10.1007/978-3-319-55621-5_9

Cited by 9 publications

(5 citation statements)

References 86 publications

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Section: Resultsmentioning

confidence: 93%

“…β-Lactam antibiotics can also inhibit human leucocyte elastase (HLE) 36 , which contains a serine residue within its active site. These observations suggest that the catalytic serine may be targeted by β-lactams in other enzymes 37 , possibly including FAP. Another part of Group I compounds includes prodrugs of inhibitors of hepatitis B virus (HBV) polymerase and human immunodeficiency virus (HIV) reverse transcriptase.…”

Section: The Most Potent Fda-approved Compounds Inhibiting Fap (Group I)mentioning

confidence: 93%

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Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds

Čermáková,

Šimková,

Wichterle

et al. 2024

Preprint

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Fibroblast activation protein (FAP) has been extensively studied as a cancer biomarker for decades. Recently, small-molecule FAP inhibitors have been widely adopted as a targeting moiety of experimental theranostic radiotracers. Here we present a fast qPCR-based analytical method allowing FAP inhibition screening in a high-throughput regime. In order to identify clinically relevant compounds that might interfere with FAP-targeted approaches, we focused on the library of FDA-approved drugs. Using theDNA-linkedInhibitorAntibodyAssay (DIANA), we tested a library of 2,667 compounds within just few hours and identified numerous FDA-approved drugs as novel FAP inhibitors. Notably, prodrugs of cephalosporin antibiotics, reverse-transcriptase inhibitors, and one elastase inhibitor were the most potent FAP inhibitors in our dataset. In addition, by employing FAP DIANA in quantification mode, we were able to determine FAP concentrations in human plasma samples. Together, our work expands the repertoire of FAP inhibitors, underscores the potential interference of co-administered drugs with FAP-targeting strategies, and presents a sensitive and low-consumption ELISA alternative for FAP quantification with a detection limit of 50 pg/ml.Graphical abstract

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Section: Resultsmentioning

confidence: 93%

Section: The Most Potent Fda-approved Compounds Inhibiting Fap (Group I)mentioning

confidence: 93%

Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds

Čermáková,

Šimková,

Wichterle

et al. 2024

Preprint

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“…Because of their medicinal activity and remarkable use as important molecules, synthesis and pharmacological investigations of betalactams have been performed for the past many decades [1][2][3][4][5][6][7]. A variety of work has been pursued by scientists to demonstrate the immense interest in beta lactam research [8][9][10][11][12][13][14][15][16].…”

Section: Introductionmentioning

confidence: 99%

Studies on Substituted Beta Lactams Towards Ring Opening: Elimination Versus Rearrangement

Yadav¹,

Newaz²,

Bose³

et al. 2018

Mod Chem Appl

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“…This is particularly very crucial when synthesis of a 4-membered heterocyclic ring system, for example beta lactam is the target [1][2][3][4][5][6][7]. The use of beta lactam for diverse purposes is well-known [1][2][3][4][5][6][7]. In addition to different types of medicinal applications, many heterocyclic compounds are obtained from them by chemical manipulations.…”

Section: Introductionmentioning

confidence: 99%

Cycloaddition Reaction of Imines with Acid Chlorides in the Presence of a Tertiary Base: Variation of the Methods for the Synthesis of Beta Lactams

Banik¹

2017

Mod Chem Appl

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Cycloaddition of optically active and racemic imines with diverse acid chlorides in the presence of a tertiary amine has been studied extensively for the synthesis of beta lactams. The conditions of the experiments have profound influence on the course of the reaction and stereochemistry of the products. Numerous methods are adopted for this cycloaddition reaction in order to control the yields, stereochemistry of the products, and durations of the reactions. This perspective demonstrates a few methods that are used for the synthesis of numerous beta lactams by cycloaddition reaction of imines and acid chlorides in the presence of a tertiary amine. The beta lactams are one of the most challenging heterocyclic compounds discovered in the world.

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Βeta-Lactams as Clinically Active Medicines

Cited by 9 publications

References 86 publications

Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds

Sensitive quantification of fibroblast activation protein and high-throughput screening for inhibition by FDA-approved compounds

Studies on Substituted Beta Lactams Towards Ring Opening: Elimination Versus Rearrangement

Cycloaddition Reaction of Imines with Acid Chlorides in the Presence of a Tertiary Base: Variation of the Methods for the Synthesis of Beta Lactams

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