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Search for "antibiotics" in Full Text gives 215 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Synthesis, characterization, antimicrobial, cytotoxic and carbonic anhydrase inhibition activities of multifunctional pyrazolo-1,2-benzothiazine acetamides
Beilstein J. Org. Chem. 2025, 21, 348–357, doi:10.3762/bjoc.21.25
- 10.3762/bjoc.21.25 Abstract The advent of antibiotic resistance in microorganisms requires the discovery and synthesis of novel antibiotics. At the same time, human pathogens are contributing to chronic and persistent inflammation. Motivated by these two concerning issues, new antibiotic drug candidates
- prepared scaffolds are valuable additions to the class of pyrazolo-1,2-benzothiazine antibiotics with selective antistaphylococcal activity. Keywords: acetamides; antibiotics; antimicrobial; benzothiazines; Staphylococcus aureus; Introduction The global crisis of antibiotic resistance has been
- progressing for decades. Reasons behind this issue include over-prescribing of FDA-approved drugs, agricultural use, rapid resistance development, and declining rates of novel antibiotic discovery [1]. In fact, the rate of discovery of new classes of antibiotics is low compared to the development of
Antibiofilm and cytotoxic metabolites from the entomopathogenic fungus Samsoniella aurantia
Beilstein J. Org. Chem. 2025, 21, 327–339, doi:10.3762/bjoc.21.23
- responses [1]. Biofilm-forming microbes were found to be up to 1,000 times more resistant to antibiotics than their planktonic forms [2]. According to the fact sheets of the National Institute of Health (NIH) and the Center for Disease Control and Prevention (CDC), 65 and 80% of all microbial and chronic
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
- metagenomics uses genetically tractable model organisms, such as Escherichia coli or Streptomyces albus, to express DNA extracted from the environment and then screen for the phenotype of interest [23][24]. This approach was used to identify BGCs that produce antibiotics, pigments, compounds that alter the
- antibiotics and secondary metabolite analysis shell (antiSMASH) further automated all of the following steps: take (meta-)genomic sequences as the input, identify BGCs for NRPs (and other natural products as well), parse out modules and domains, and finally outputs the order and identity of BBs of a predicted
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
Tandem diazotization/cyclization approach for the synthesis of a fused 1,2,3-triazinone-furazan/furoxan heterocyclic system
Beilstein J. Org. Chem. 2024, 20, 2342–2348, doi:10.3762/bjoc.20.200
- products and pharmacologically active molecules. For example, nucleic acids, proteins and enzymes, hormones and vitamins, essential for the functioning of a living organism, also contain nitrogen frameworks [1][2]. Besides that, nitrogen-containing compounds are widely used in medicine as antibiotics
Efficacy of radical reactions of isocyanides with heteroatom radicals in organic synthesis
Beilstein J. Org. Chem. 2024, 20, 2114–2128, doi:10.3762/bjoc.20.182
- yields the sequential addition products 9 in moderate to excellent yields (Scheme 5) [33]. The product can be used as a precursor for the carbapenem scaffold, one of the basic scaffolds of antibiotics. Thermal or photoirradiated decomposition of organotellurium compounds generates carbon radicals that
Allostreptopyrroles A–E, β-alkylpyrrole derivatives from an actinomycete Allostreptomyces sp. RD068384
Beilstein J. Org. Chem. 2024, 20, 1981–1987, doi:10.3762/bjoc.20.174
- of this specific composition have not been reported. The pyrrole-2-carboxyl skeleton is a recurring framework in pyrrolic natural products including microbial pyrrolostatin and aminocoumarin antibiotics [2], plant-derived brachystemidines [26], and lamellarins from marine invertebrates [6] (Figure
Access to 2-oxoazetidine-3-carboxylic acid derivatives via thermal microwave-assisted Wolff rearrangement of 3-diazotetramic acids in the presence of nucleophiles
Beilstein J. Org. Chem. 2024, 20, 1894–1899, doi:10.3762/bjoc.20.164
- (azetidin-2-one) scaffold to medicinal chemistry and drug design is self-evident. This four-membered heterocycle is a key fragment of many antibiotics [1], including penicillin and its analogues, as well as other pharmacologically important molecules [2]. Therefore, the search for new efficient and
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
- substantial threat to global public health, demanding urgent attention and action. This study focuses on lanthipeptides, ribosomally encoded peptides that display significant structural diversity and hold promising potential as antibiotics. Genome mining was employed to locate biosynthetic gene clusters (BGCs
- ], a number expected to increase exponentially. One fundamental objective of the Global Action Plan on Antimicrobial Resistance by the World Health Organization (WHO) is the investment in developing new drugs, diagnostic tools, vaccines, and other interventions [2]. In this context, many antibiotics
- compounds. For example, the discovery of teixobactin [8] has paved the way for developing antibiotics with innovative mechanisms of action. Similarly, the discovery of halicin, a molecule identified through a machine learning-based approach, has shown promise as a broad-spectrum antimicrobial agent
Methyltransferases from RiPP pathways: shaping the landscape of natural product chemistry
Beilstein J. Org. Chem. 2024, 20, 1652–1670, doi:10.3762/bjoc.20.147
- spectrum and loses all activity when unmethylated. Although the mode of action is unclear, the methylations are essential to the bioactivity. CypM methylates many oligopeptides that mimic the cypemycin N-terminal sequence, and unrelated peptide antibiotics. Additionally, CypM methylates short oligopeptides
- with N-terminal alanine, serine, threonine, glycine, and methionine residues, as well as the antibiotics nisin and haloduracin with good efficiency. Nisin was methylated on its N-terminal isoleucine and on the side chain of Lys12, where two methylations occurred. It is important to note that N
Photoswitchable glycoligands targeting Pseudomonas aeruginosa LecA
Beilstein J. Org. Chem. 2024, 20, 1486–1496, doi:10.3762/bjoc.20.132
- the leading cause of morbidity and mortality in cystic fibrosis and immunocompromised patients and as one of the leading causes of nosocomial infections [1]. Due to the existence of numerous molecular mechanisms conferring resistance to multiple classes of antibiotics, therapeutic options are
- increasingly limited for treatment of infections. PA has been classified as a priority 1 pathogen by the WHO [2][3]. Various approaches to treating PA, in addition to traditional antibiotics, have been developed including inhibition of quorum sensing, biofilm formation, iron chelation, and interfering with
- formation [5][6][7][8]. Building synthetic glycoconjugates for the inhibition and modulation of bacterial lectins responsible for biofilm formation have shown promising results [9][10]. Unlike antibiotics, lectin inhibitors could prevent pathogenicity by interfering with virulence factors instead of killing
Activity assays of NnlA homologs suggest the natural product N-nitroglycine is degraded by diverse bacteria
Beilstein J. Org. Chem. 2024, 20, 830–840, doi:10.3762/bjoc.20.75
- portion of NNG would be expected to exist as the inhibitory nitronate form at physiological pH, suggesting another potential role for nitramine groups as potent warheads in antibiotics. This antibiotic activity may also require further modification of NNG or its incorporation into a larger natural product
- of NNG. Cells were incubated overnight in 1/5 LB, 20 µM IPTG, 3 mM NNG with appropriate antibiotics, incubated overnight at 37 °C. Molecular mass determination of purified NnlA homologs by A) SDS-PAGE or B) analytical size exclusion chromatography. Homolog labeled in figure. Mobile phase and sample
Methodology for awakening the potential secondary metabolic capacity in actinomycetes
Beilstein J. Org. Chem. 2024, 20, 753–766, doi:10.3762/bjoc.20.69
- “rare actinomycetes”, and the secondary metabolites produced by these species have thus attracted increasing attention. Indeed, an increasing proportion of newly identified antibiotics are reportedly produced by rare actinomycetes [20]. Igarashi and colleagues have also focused on various rare
- [46]. Finally, several studies have reported the modulation of secondary metabolic activation in actinomycetes using small molecules. For example, Ochi et al. proposed the “ribosome engineering” technique, in which actinomycetes are cultured with antibiotics to activate secondary metabolism by
- production of antibiotics such as actinorhodin (ACT, 8), undecylprodigiosin (RED, 21), and calcium-dependent antibiotic (CDA, 22) in Streptomyces coelicolor M145 (Figure 3b). Chen et al. and Shu et al. reported that under stress associated with high concentrations of glutamate, AfsQ1/Q2 is important not only
Substrate specificity of a ketosynthase domain involved in bacillaene biosynthesis
Beilstein J. Org. Chem. 2024, 20, 734–740, doi:10.3762/bjoc.20.67
- are a large class of natural products which often exhibit potent biological activities for their application in medicine, e.g., as antibiotics or immunosuppressants [1]. Despite their high structural variability all compounds from this class are commonly made through the action of polyketide synthases
Chemoenzymatic synthesis of macrocyclic peptides and polyketides via thioesterase-catalyzed macrocyclization
Beilstein J. Org. Chem. 2024, 20, 721–733, doi:10.3762/bjoc.20.66
- candidates [4]. Many clinical pharmaceuticals with high market value, including the immunosuppressants cyclosporin and rapamycin, the antibiotics daptomycin and erythromycin, and the antitumor agent epothilone, all belong to these categories. Therefore, the rising demand for corresponding therapeutics
- type B streptogramin variants [41], including pristinamycin IE (8), which belongs to the class of depsipeptide antibiotics. Similarly, the linear peptide-SNAC was prepared through the SPPS method on 2-chlorotrityl resin, and macrolactonization was catalyzed by SnbDE TE, a thioesterase from
- pristinamycin I NRPS. This TE domain showed activity for hydroxy groups and amines to form either lactone or lactam, and the broad substrate scope made this strategy potent for modifying the bioactivity of streptogramin antibiotics. In 2007, the same laboratory identified the interactive TE domain of the
A new analog of dihydroxybenzoic acid from Saccharopolyspora sp. KR21-0001
Beilstein J. Org. Chem. 2024, 20, 497–503, doi:10.3762/bjoc.20.44
- Actinomycetes are well-known as the main producers of bioactive compounds such as antibiotics, anticancers, and immunosuppressants. Screening of natural products from actinomycetes has been an essential part of several drug discovery programs. Finding such novel biologically active metabolites is immensely
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
- ; Introduction Nonribosomal peptides (NRPs) exhibit various biological activities and have been used as therapeutic agents, such as antibiotics, anticancer agents, and immunosuppressants [1]. Additionally, NRPs function as virulence factors, such as siderophores and genotoxins [2]. Therefore, inhibiting their
- 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
Optimizations of lipid II synthesis: an essential glycolipid precursor in bacterial cell wall synthesis and a validated antibiotic target
Beilstein J. Org. Chem. 2024, 20, 220–227, doi:10.3762/bjoc.20.22
- is synthesized on the inner leaflet of the cytoplasmic membrane, before translocation to the outer leaflet, where it is then used as the monomeric building block of peptidoglycan biosynthesis. Lipid II is a validated antibiotic target for clinically prescribed antibiotics including vancomycin and
- synthesis. Thus, this strategy holds considerable promise for advancing the synthesis of a diverse range of lipid II analogues, opening avenues for further exploration into their biophysical characteristics, as well as their interactions with antibiotics. Structure of lipid II, with variable positions shown
Synthetic approach to 2-alkyl-4-quinolones and 2-alkyl-4-quinolone-3-carboxamides based on common β-keto amide precursors
Beilstein J. Org. Chem. 2023, 19, 1804–1810, doi:10.3762/bjoc.19.132
- great research interest, with many reviews published in the recent years [20][21][22]. Some of the compounds are known to act as antibiotics [23][24][25][26], while others function as quorum-sensing signal molecules which regulate the production and release of virulence factors in bacteria, thus helping
Secondary metabolites of Diaporthe cameroonensis, isolated from the Cameroonian medicinal plant Trema guineensis
Beilstein J. Org. Chem. 2023, 19, 1555–1561, doi:10.3762/bjoc.19.112
- ]. Compound 1 is a benzofuranone, structurally related to enalin A and pseudopithonone, isolated from the fungus Verruculina enalia and the marine-derived fungus Pseudopithomyces maydicus, respectively [12][29]. Its core structure is also like actiketal, a new member of the glutarimide antibiotics, previously
Synthesis and biological evaluation of Argemone mexicana-inspired antimicrobials
Beilstein J. Org. Chem. 2023, 19, 1511–1524, doi:10.3762/bjoc.19.108
- example, is a common opportunistic human pathogen, some strains of which are resistant to multiple antibiotics [3]. Such drug-resistant microbes are especially prevalent in hospital settings, where they are one of the most difficult illnesses to treat [4]. In addition to being a terrestrial cause for
Two new lanostanoid glycosides isolated from a Kenyan polypore Fomitopsis carnea
Beilstein J. Org. Chem. 2023, 19, 1161–1169, doi:10.3762/bjoc.19.84
- between 1930 and 1960 during the ‘golden era’ of antibiotics. Unfortunately, the pace of antibiotic research and development in the face of emerging resistant pathogens has not been kept up, thus raising a big concern for a return to the pre-antibiotic era [1][2]. Recently, the danger posed by previously
Synthesis of imidazo[4,5-e][1,3]thiazino[2,3-c][1,2,4]triazines via a base-induced rearrangement of functionalized imidazo[4,5-e]thiazolo[2,3-c][1,2,4]triazines
Beilstein J. Org. Chem. 2023, 19, 1047–1054, doi:10.3762/bjoc.19.80
- -aminocephalosporanic acid (7-ACA), which is a key fragment of broad-spectrum cephalosporin antibiotics [13][14]. Condensed 1,2,4-triazines attract attention of researchers due to their diverse biological activities [15] and also their application as starting materials for the constructing of new heterocyclic systems
Palladium-catalyzed enantioselective three-component synthesis of α-arylglycine derivatives from glyoxylic acid, sulfonamides and aryltrifluoroborates
Beilstein J. Org. Chem. 2023, 19, 719–726, doi:10.3762/bjoc.19.52
- several well-known natural products with interesting biological properties, such as the glycopeptide antibiotics vancomycin and teicoplanin [5] or feglymycin [6], a 13mer peptide which contains nine α-arylglycines in its backbone. α-Arylglycine derivatives are used in the production of important drugs
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
- were able to isolate product (+)-214 in good yield (75–85%) and excellent stereoselectivity (>95%) on a multigram scale. Additionally, both stereoisomers are available by simply using the ligand with the opposite stereochemistry. Pleuromutilin-based antibiotics are an essential line of defense in the
- 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
- -acquired bacterial pneumonia. Herzon et al. have demonstrated the modular synthesis of various pleuromutilins and created the foundation for the development of novel antibiotics against complicated infections. The key stereochemical information was usually introduced by a stereoselective tandem Cu
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