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Search for "new antibiotics" in Full Text gives 23 result(s) in Beilstein Journal of Organic Chemistry.
Chemical structure metagenomics of microbial natural products: surveying nonribosomal peptides and beyond
Beilstein J. Org. Chem. 2024, 20, 3050–3060, doi:10.3762/bjoc.20.253
- for nutrient and space, and that “chemical weapons” of this sort are widespread in nature. Waksman used the BGF workflow to find more than 20 new antibiotics throughout his career, wherein microbial culture extracts were fractionated and then tested for antimicrobial activity. The active fractions
- molecules were screened for various bioactivities and led to the discovery of new antibiotics, antifungals, as well as anticancer compounds (Figure 4). Importantly, the underlying mechanism of bacterial growth suppression has been identified for several Syn-BNP antibiotics, which includes both general mode
Synthesis and antimycotic activity of new derivatives of imidazo[1,2-a]pyrimidines
Beilstein J. Org. Chem. 2024, 20, 2806–2817, doi:10.3762/bjoc.20.236
- St., 344090 Rostov-on-Don, Russian Federation Clinical Laboratory Diagnostics Department, N. N. Burdenko Voronezh State Medical University, 10 Studencheskaya St., 394036 Voronezh, Russian Federation Gause Institute of New Antibiotics, 11 B. Pirogovskaya St., 119021 Moscow, Russian Federation Organic
Discovery of antimicrobial peptides clostrisin and cellulosin from Clostridium: insights into their structures, co-localized biosynthetic gene clusters, and antibiotic activity
Beilstein J. Org. Chem. 2024, 20, 1800–1816, doi:10.3762/bjoc.20.159
- peptides, coupled with their successful production in E. coli [30], has driven research to consider them a source for new antibiotics, as supported by the present study. Identifying the genetic and biochemical mechanisms underlying the production of compounds is of utmost importance in developing effective
- chemical structures of these lantibiotics make them promising candidates for treating drug-resistant pathogens, and the characterization of these compounds from Clostridium provides an opportunity to develop new antibiotics. Results and Discussion Genome mining of LanM enzymes’ sequence diversity to
- targets in S. epidermidis, a Gram-positive bacterium. Conclusion The pressing need for new antibiotics has made the search for them a top priority amongst the scientific community. In this study, we utilized genomic mining to forecast the uniqueness of two lanthipeptides derived from the Clostridium genus
Development of a chemical scaffold for inhibiting nonribosomal peptide synthetases in live bacterial cells
Beilstein J. Org. Chem. 2024, 20, 445–451, doi:10.3762/bjoc.20.39
- penetrate cells. The application of this new scaffold to NRPS inhibitors involved in the production of virulence factors could thus facilitate the development of new antibiotics. Biosynthesis of gramicidin S. Modules comprise the PCP, A, E, C, and TE domains. PCP, peptidyl carrier protein; A1, ʟ-Phe
Enolates ambushed – asymmetric tandem conjugate addition and subsequent enolate trapping with conventional and less traditional electrophiles
Beilstein J. Org. Chem. 2023, 19, 593–634, doi:10.3762/bjoc.19.44
- war against resistant bacteria strains. The tricyclic diterpene fungal metabolite (+)-pleuromutilin was isolated in 1951 [104]. Since then it has served as a starting point for developing new antibiotics, including semisynthetic derivatives effective against Gram-positive or even both types of
On drug discovery against infectious diseases and academic medicinal chemistry contributions
Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141
- issue in this regard as a major portion of published data will have to be filtered out before such methods starts to make some tangible headways [57]. For instance, a recent “deep-learning” search for new antibiotics came out with the finding that halicin (1) depicted in Figure 1 was, as many nitro
- but way better (rescaffolded?) inhibitors which would have taken the market 10–15 years later. The following is an attempt to illustrate the issues encountered in this second stage with a review of the new antibiotics discovered which are, or about to be, used in human medicine. In 2007, the
β-Lactamase inhibition profile of new amidine-substituted diazabicyclooctanes
Beilstein J. Org. Chem. 2021, 17, 711–718, doi:10.3762/bjoc.17.60
- increasing day by day thereby indicating the strength of these pathogens in compromising the efficacy of new antibiotics after a certain period of time. Recently, the WHO warned about the seriousness of carbapenemase-resistant Gram-negative bacteria as a global threat and urged for the development of new
Fabclavine diversity in Xenorhabdus bacteria
Beilstein J. Org. Chem. 2020, 16, 956–965, doi:10.3762/bjoc.16.84
- metabolite; Xenorhabdus; Introduction The constantly increasing threat of multiresistant pathogens requires the development of new antibiotics, as they are indispensable to maintain the state of health of our society [1]. Bacterial natural products, also called secondary or specialized metabolites (SM
Isolation of fungi using the diffusion chamber device FIND technology
Beilstein J. Org. Chem. 2019, 15, 2191–2203, doi:10.3762/bjoc.15.216
- -stimulating, and anticancer activities [2]. Since the World Health Organization (WHO) declared antibiotic resistance a global threat and urged the search for new antibiotics, the interest in fungal metabolites increased recently. In order to find new structural types, novel source organisms have to be
Synthesis and biological evaluation of truncated derivatives of abyssomicin C as antibacterial agents
Beilstein J. Org. Chem. 2019, 15, 1468–1474, doi:10.3762/bjoc.15.147
- develop new antibiotics, but the reevaluation of known natural products (NP) and the identification of new NPs and derivatives thereof is considered an especially important pathway in the search for more robust antibiotics [1][2]. The main reasons are the inherent high selectivity and appropriate
Protein–protein interactions in bacteria: a promising and challenging avenue towards the discovery of new antibiotics
Beilstein J. Org. Chem. 2018, 14, 2881–2896, doi:10.3762/bjoc.14.267
- represent an alternative lead discovery strategy to obtain new anti-infective molecules. Keywords: new antibiotics; protein–protein interactions; resistance; Introduction Bacterial infections are not only one of the most frequent diseases in humans and livestock, but also one of the top ten causes of
- /D)LF (8, Figure 3) [55][56]. There are several reasons that make the bacterial clamp a promising and attractive target for the development of new antibiotics: it is essential for DNA replication and repair, it is highly conserved across the different bacterial pathogens and, most importantly from a
- are other strategies that are being explored towards the discovery of new antibiotics with novel mechanisms of action such as for example inhibitors of host–pathogen interactions and of the type 3 secretion system (T3SS) in Gram-negative bacteria, nonetheless, the specific targets remain unknown or
Synthesis of pyrrolidine-based hamamelitannin analogues as quorum sensing inhibitors in Staphylococcus aureus
Beilstein J. Org. Chem. 2018, 14, 2822–2828, doi:10.3762/bjoc.14.260
- resistance problem need to be multifactorial. Next to disease prevention and the development of new antibiotics, it is essential to investigate innovative strategies to combat bacterial infections [3][4]. Recently, targeting bacterial virulence has gained a lot of attention [5][6][7]. It has been
The design and synthesis of an antibacterial phenothiazine–siderophore conjugate
Beilstein J. Org. Chem. 2018, 14, 2646–2650, doi:10.3762/bjoc.14.242
- infections [1]. To meet this challenge there is a desperate need for new antibiotics, antibiotic targets and strategies to enhance the efficacy of current antibiotics [2]. One novel strategy which is receiving significant interest is the manipulation of bacterial iron transport pathways to deliver
Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers
Beilstein J. Org. Chem. 2018, 14, 2627–2645, doi:10.3762/bjoc.14.241
- compounds also showed activity against RNA polymerase, a popular target for the development of new antibiotics [52][53]. Hitting such a target would jeopardise the principle of pathoblockers, which should only disarm the bacteria and not kill them. Hence, a follow-up study on PqsD/RNAP selectivity was
Pathoblockers or antivirulence drugs as a new option for the treatment of bacterial infections
Beilstein J. Org. Chem. 2018, 14, 2607–2617, doi:10.3762/bjoc.14.239
- to a decline in the development of new antibiotics, with very few new antibiotics addressing a novel mode of action being brought to the market over the last four decades [3]. In parallel with the decline of new antibiotics, resistance towards these widely used drugs has evolved at a high pace and
- importance, was published by the WHO [5]. Emphasizing the current crisis, in 2017 one report described a patient infected with a pan-resistant Klebsiella strain, where no available drug was efficacious and the patient finally died from septic shock [6]. Therefore, new antibiotics and new alternative
- formation and virulence in an insect infection model or a murine model [76][77][78]. Conclusion The current antimicrobial crisis poses an enormous challenge to society, and requires a joint effort for the development of novel anti-infectives. While there is an urgent need for new antibiotics with novel
Chemical probes for competitive profiling of the quorum sensing signal synthase PqsD of Pseudomonas aeruginosa
Beilstein J. Org. Chem. 2016, 12, 2784–2792, doi:10.3762/bjoc.12.277
- bacterial strains urges the rapid discovery of new antibiotics and the development of novel antiinfective strategies [1]. One of the leading causes for nosocomial infections is the opportunistic human pathogen Pseudomonas aeruginosa, which, by chronic infections, also poses a major threat for cystic
Antibiotics from predatory bacteria
Beilstein J. Org. Chem. 2016, 12, 594–607, doi:10.3762/bjoc.12.58
- example on how new antibiotics can be retrieved from predatory bacteria. The isolation of predatory bacteria from soil is typically achieved by means of baiting techniques. For this, a pea-sized sample is placed on a nutrient-poor agar medium, that was previously inoculated with potential prey microbes
- of new antibiotics [93][94]. Since the gene loci that are involved in their biosyntheses have been identified [87][92], it might even be possible to genetically engineer further derivatives in the future. The close correlation between the activity profile of the gulmirecins and the prey range of
Effective in silico prediction of new oxazolidinone antibiotics: force field simulations of the antibiotic–ribosome complex supervised by experiment and electronic structure methods
Beilstein J. Org. Chem. 2016, 12, 415–428, doi:10.3762/bjoc.12.45
- injuries can kill, is a very real possibility for the 21st century” [6]. The need for a fast but effective, structure-based strategy for the development of new antibiotics is therefore more than evident [7]. From an experimental point of view, during the last years the amount of structural data describing
De novo macrolide–glycolipid macrolactone hybrids: Synthesis, structure and antibiotic activity of carbohydrate-fused macrocycles
Beilstein J. Org. Chem. 2014, 10, 2215–2221, doi:10.3762/bjoc.10.229
- antibacterial activity [7][8]. Over time, antibiotic use has created a selection pressure that has led to bacterial resistance and a subsequent need for continuous development of new antibiotics. Despite cumbersome syntheses, erythromycin analogs continue to be used as front line antibiotics while the clinical
Application of cyclic phosphonamide reagents in the total synthesis of natural products and biologically active molecules
Beilstein J. Org. Chem. 2014, 10, 1848–1877, doi:10.3762/bjoc.10.195
- antibiotics has dictated the need for continuous development of existing and discovery of new antibiotics ever since the introduction of the first antibacterial agents in the first half of the 20th century. In recent years, this trend has become a serious threat for public health with the emergence of
The total synthesis of D-chalcose and its C-3 epimer
Beilstein J. Org. Chem. 2013, 9, 2620–2624, doi:10.3762/bjoc.9.296
- sourced material and unsatisfactory overall yield. As part of our study concerning the structure–activity relationships and chemistry of new antibiotics, we sought to develop a reliable and efficient synthetic route starting from inexpensive, commercial sources to provide access to chalcose. We describe a
Modulating the activity of short arginine-tryptophan containing antibacterial peptides with N-terminal metallocenoyl groups
Beilstein J. Org. Chem. 2012, 8, 1753–1764, doi:10.3762/bjoc.8.200
- ; medicinal organometallic chemistry; metallocenoyl; peptides; tryptophan; Introduction New antibacterial agents need to be discovered since established antibiotics are increasingly losing ground against resistant bacteria and at the same time the pipeline that is supposed to produce new antibiotics is
Synthetic studies towards bottromycin
Beilstein J. Org. Chem. 2012, 8, 1652–1656, doi:10.3762/bjoc.8.189
- ring system in a straightforward manner. Keywords: amidines; antibiotics; bottromycin; peptides; thiopeptides; Ugi reactions; Introduction Natural products are excellent sources as lead structures for the development of new antibiotics. Over millions of years microorganisms, such as bacteria and
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