Search results

Search for "antibiotics" in Full Text gives 215 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.

Strategies to access the [5-8] bicyclic core encountered in the sesquiterpene, diterpene and sesterterpene series

  • Cécile Alleman,
  • Charlène Gadais,
  • Laurent Legentil and
  • François-Hugues Porée

Beilstein J. Org. Chem. 2023, 19, 245–281, doi:10.3762/bjoc.19.23

Graphical Abstract
  • delivered cyclooctene 81, an advanced intermediate in the synthesis of (±)-asteriscanolide (2). Pleuromutilin (1) is the flagship representative of a recent class of antibiotics which displays a propellane-like structure (Scheme 14) [41][42][43][44]. Indeed, these compounds possess a compact tricyclic
PDF
Album
Review
Published 03 Mar 2023

Combining the best of both worlds: radical-based divergent total synthesis

  • Kyriaki Gennaiou,
  • Antonios Kelesidis,
  • Maria Kourgiantaki and
  • Alexandros L. Zografos

Beilstein J. Org. Chem. 2023, 19, 1–26, doi:10.3762/bjoc.19.1

Graphical Abstract
  • maydis in 2014 and were reported to possess antibacterial activity against a small panel of both gram-positive and -negative bacteria [89][90]. Interestingly, their chemical structure bears no resemblance to recognize antibiotics and their mechanism of action remains unknown. Based on the knowledge
PDF
Album
Review
Published 02 Jan 2023

Digyalipopeptide A, an antiparasitic cyclic peptide from the Ghanaian Bacillus sp. strain DE2B

  • Adwoa P. Nartey,
  • Aboagye K. Dofuor,
  • Kofi B. A. Owusu,
  • Anil S. Camas,
  • Hai Deng,
  • Marcel Jaspars and
  • Kwaku Kyeremeh

Beilstein J. Org. Chem. 2022, 18, 1763–1771, doi:10.3762/bjoc.18.185

Graphical Abstract
  • proven to be of clinical, health, industrial research and agrochemical importance [7][8][9][10][11][12]. Interestingly, the resistance of Bacillus spores to heat, radiation, and disinfection coupled with an inherent biosynthetic potential that enables them to grow even in the presence of antibiotics such
PDF
Album
Supp Info
Full Research Paper
Published 28 Dec 2022

Navigating and expanding the roadmap of natural product genome mining tools

  • Friederike Biermann,
  • Sebastian L. Wenski and
  • Eric J. N. Helfrich

Beilstein J. Org. Chem. 2022, 18, 1656–1671, doi:10.3762/bjoc.18.178

Graphical Abstract
  • ., bongkrekic acid (4) [11]), antibacterial (e.g., vancomycin (5) [12]) or antifungal compounds (e.g., amphotericin B (6) [13]) (Figure 1). The identification of almost all clinically relevant antibiotics using bioactivity-guided fractionation approaches long before the beginning of the post-genomic era
  • ). Moreover, since these assembly line-like pathways follow the same biosynthetic principle, they often form hybrids with other biosynthetic assembly line-like pathways [21]. Prominent examples of the usage of pHMMs are the original algorithm of the antibiotics & Secondary Metabolite Analysis Shell (antiSMASH
PDF
Album
Perspective
Published 06 Dec 2022

Efficient synthesis of aziridinecyclooctanediol and 3-aminocyclooctanetriol

  • Emine Salamci and
  • Ayse Kilic Lafzi

Beilstein J. Org. Chem. 2022, 18, 1539–1543, doi:10.3762/bjoc.18.163

Graphical Abstract
  • ]. Furthermore, aziridine derivatives are valuable precursors for the synthesis of aminocyclitols, which can be found in nature in several families of natural and clinically important antibiotics [10]. Aminocyclitols containing the amino alcohol motif are important structural components for modifying bioactive
PDF
Album
Supp Info
Full Research Paper
Published 11 Nov 2022

On drug discovery against infectious diseases and academic medicinal chemistry contributions

  • Yves L. Janin

Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141

Graphical Abstract
  • 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
  • antibacterial research department of GSK reported the results of their genome-driven seven-year long quest for original antibiotics. This target-based approach actually failed although 300 bacterial genes had been considered and 70 high-throughput screening campaigns, focusing on the corresponding proteins, had
PDF
Album
Perspective
Published 29 Sep 2022

Synthesis of tryptophan-dehydrobutyrine diketopiperazine and biological activity of hangtaimycin and its co-metabolites

  • Houchao Xu,
  • Anne Wochele,
  • Minghe Luo,
  • Gregor Schnakenburg,
  • Yuhui Sun,
  • Heike Brötz-Oesterhelt and
  • Jeroen S. Dickschat

Beilstein J. Org. Chem. 2022, 18, 1159–1165, doi:10.3762/bjoc.18.120

Graphical Abstract
  • hangtaimycin, TDD and the hangtaimycin degradation product HTM222 are given. Keywords: antibiotics; enantioselective synthesis; peptides; racemisation; Streptomyces; Introduction Hangtaimycin (1, Scheme 1) was first isolated from Streptomyces spectabilis and shown to possess weak antimicrobial activity
PDF
Album
Supp Info
Letter
Published 07 Sep 2022

Anti-inflammatory aromadendrane- and cadinane-type sesquiterpenoids from the South China Sea sponge Acanthella cavernosa

  • Shou-Mao Shen,
  • Qing Yang,
  • Yi Zang,
  • Jia Li,
  • Xueting Liu and
  • Yue-Wei Guo

Beilstein J. Org. Chem. 2022, 18, 916–925, doi:10.3762/bjoc.18.91

Graphical Abstract
  • purchased from American Type Culture Collection (ATCC, Manassas, VA, USA). RAW264.7 cells were cultured in DMEM (Dulbecco’s modified Eagle medium) supplemented with 10% fetal bovine serum, antibiotics (100 U/mL penicillin and 100 U/mL streptomycin), and maintained at 37 °C in a humidified incubator of 5
PDF
Album
Supp Info
Full Research Paper
Published 25 Jul 2022

Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment

  • Anas J. Rasras,
  • Mohamed El-Naggar,
  • Nesreen A. Safwat and
  • Raed A. Al-Qawasmeh

Beilstein J. Org. Chem. 2022, 18, 631–638, doi:10.3762/bjoc.18.63

Graphical Abstract
  • the development of multidrug resistant bacteria due to excessive use of antibiotics [2][4]. Heterocyclic compounds are the key components for drug design and synthesis. Among them, 1,3,4-oxadiazole derivatives are attractive and have been investigated for decades. This is due to their promising
PDF
Album
Supp Info
Full Research Paper
Published 31 May 2022

Synthesis of 3,4,5-trisubstituted isoxazoles in water via a [3 + 2]-cycloaddition of nitrile oxides and 1,3-diketones, β-ketoesters, or β-ketoamides

  • Md Imran Hossain,
  • Md Imdadul H. Khan,
  • Seong Jong Kim and
  • Hoang V. Le

Beilstein J. Org. Chem. 2022, 18, 446–458, doi:10.3762/bjoc.18.47

Graphical Abstract
  • , and bio-orthogonal chemistry). Our method could also find potential applications in the production of important 3,4,5-trisubstituted isoxazoles, such as the precursors of many β-lactamase-resistant antibiotics like oxacillin, cloxacillin, dicloxacillin, and flucloxacillin (Figure 9), which share a
  • plausible mechanism for the formation of the 3,4,5-trisubstituted isoxazoles 3 in the presence of DIPEA in polar solvents like water or methanol. Structures of β-lactamase-resistant antibiotics oxacillin, cloxacillin, dicloxacillin, and flucloxacillin. Optimization of the reaction conditions for the
PDF
Album
Supp Info
Full Research Paper
Published 22 Apr 2022

The asymmetric Henry reaction as synthetic tool for the preparation of the drugs linezolid and rivaroxaban

  • Martin Vrbický,
  • Karel Macek,
  • Jaroslav Pochobradský,
  • Jan Svoboda,
  • Miloš Sedlák and
  • Pavel Drabina

Beilstein J. Org. Chem. 2022, 18, 438–445, doi:10.3762/bjoc.18.46

Graphical Abstract
  • pharmaceutical substances [1][2][3]. This class includes for instance oxazolidine-type antibiotics [3], e.g., linezolid (1) [4] (sold under the trade name Zyvox® (Figure 1) or tedizolid [5] (sold under the trade name Sivextro®), and the anticoagulant rivaroxaban (2) [6][7] (Figure 1), a member of DOACs (direct
  • -2-one antibiotics only the S-enantiomers are able to block bacterial ribosomes, which leads to the prevention of translation processes in bacteria [9][10]. With regards to these facts, a high enantiomeric purity is one of the fundamental requirements in the production of such pharmaceutical
PDF
Album
Supp Info
Full Research Paper
Published 14 Apr 2022

Unsaturated fatty acids and a prenylated tryptophan derivative from a rare actinomycete of the genus Couchioplanes

  • Shun Saito,
  • Kanji Indo,
  • Naoya Oku,
  • Hisayuki Komaki,
  • Masashi Kawasaki and
  • Yasuhiro Igarashi

Beilstein J. Org. Chem. 2021, 17, 2939–2949, doi:10.3762/bjoc.17.203

Graphical Abstract
  • -dienoyl motif in 3 is seen in many antibiotics but that with a C10 chain length is only precedented by manumycin C [29], TMC-1 C [30], and phialomustins [26] (Figure 7). In the family Micromonosporaceae, a strain belonging to the genus Plantactinospora is known to produce U-62162, a manumycin-type
PDF
Album
Supp Info
Full Research Paper
Published 16 Dec 2021

Host–guest interaction and properties of cucurbit[8]uril with chloramphenicol

  • Lin Zhang,
  • Jun Zheng,
  • Guangyan Luo,
  • Xiaoyue Li,
  • Yunqian Zhang,
  • Zhu Tao and
  • Qianjun Zhang

Beilstein J. Org. Chem. 2021, 17, 2832–2839, doi:10.3762/bjoc.17.194

Graphical Abstract
  • sustained-release ability of drug molecules [31][33][34]. However, previous studies rarely reported the interaction between Q[8] and antibiotics, and did not explore the effect of Q[8] on antibacterial activity of antibiotics. Herein, Q[8] was selected as the host and the host–guest interaction between Q[8
PDF
Album
Supp Info
Full Research Paper
Published 03 Dec 2021

Biological properties and conformational studies of amphiphilic Pd(II) and Ni(II) complexes bearing functionalized aroylaminocarbo-N-thioylpyrrolinate units

  • Samet Poyraz,
  • Samet Belveren,
  • Sabriye Aydınoğlu,
  • Mahmut Ulger,
  • Abel de Cózar,
  • Maria de Gracia Retamosa,
  • Jose M. Sansano and
  • H. Ali Döndaş

Beilstein J. Org. Chem. 2021, 17, 2812–2821, doi:10.3762/bjoc.17.192

Graphical Abstract
  • then, 250–0.12 μg/mL final concentration ranges of the compounds were obtained. In each anti-TB activity determination, a sterility control (without H37Rv working solution) and a growth control (containing no antibiotics) were included in each plate. Effects of DMSO were controlled by inoculated broth
PDF
Album
Supp Info
Full Research Paper
Published 02 Dec 2021

Recent advances in organocatalytic asymmetric aza-Michael reactions of amines and amides

  • Pratibha Sharma,
  • Raakhi Gupta and
  • Raj K. Bansal

Beilstein J. Org. Chem. 2021, 17, 2585–2610, doi:10.3762/bjoc.17.173

Graphical Abstract
  • as an important synthetic strategy for the preparation of a large variety of β-amino carbonyl and similar motifs which are present in many bioactive natural products [8][9], antibiotics [10][11][12] and chiral auxiliaries [13][14][15]. However, the reaction of many nitrogen-nucleophiles, such as
PDF
Album
Review
Published 18 Oct 2021

Isolation and characterization of new phenolic siderophores with antimicrobial properties from Pseudomonas sp. UIAU-6B

  • Emmanuel T. Oluwabusola,
  • Olusoji O. Adebisi,
  • Fernando Reyes,
  • Kojo S. Acquah,
  • Mercedes De La Cruz,
  • Larry L. Mweetwa,
  • Joy E. Rajakulendran,
  • Digby F. Warner,
  • Deng Hai,
  • Rainer Ebel and
  • Marcel Jaspars

Beilstein J. Org. Chem. 2021, 17, 2390–2398, doi:10.3762/bjoc.17.156

Graphical Abstract
  • pseudomonine [28] are produced under iron deficiency by various Pseudomonas species to acquire iron which is essential for cell metabolism and growth [29][30]. Studies show that siderophore–antibiotic complexes may be used as a Trojan horse strategy in which the antibiotics utilize the iron-siderophore
PDF
Album
Supp Info
Full Research Paper
Published 13 Sep 2021

Nomimicins B–D, new tetronate-class polyketides from a marine-derived actinomycete of the genus Actinomadura

  • Zhiwei Zhang,
  • Tao Zhou,
  • Taehui Yang,
  • Keisuke Fukaya,
  • Enjuro Harunari,
  • Shun Saito,
  • Katsuhisa Yamada,
  • Chiaki Imada,
  • Daisuke Urabe and
  • Yasuhiro Igarashi

Beilstein J. Org. Chem. 2021, 17, 2194–2202, doi:10.3762/bjoc.17.141

Graphical Abstract
  • cytotoxicity against P388 murine leukemia cells with IC50 values of 33 and 89 μM, respectively. Keywords: Actinomadura; nomimicin; polyketide; spirotetronate; Introduction Actinomycetes are a valuable source of bioactive compounds, accounting for approximately two thirds of all known antibiotics, and more
  • with a known congener, nomimicin A (4), from Actinomadura sp. AKA43. Compounds 1 and 2 are new members of the spirotetronate-class antibiotics, characterized by a macrocyclic structure containing a trans-decalin unit and a tetronic acid moiety spiro-linked with a cyclohexene ring. To date, more than
  • intramolecular Diels–Alder reaction [20][25]. Compound 3 is very likely a biosynthetic precursor of 4. This is the first report on the isolation of a biosynthetic precursor of spirotetronate antibiotics as an innate metabolite from a wild-type strain, while such an intermediate was previously obtained from a
PDF
Album
Supp Info
Full Research Paper
Published 27 Aug 2021

Natural products in the predatory defence of the filamentous fungal pathogen Aspergillus fumigatus

  • Jana M. Boysen,
  • Nauman Saeed and
  • Falk Hillmann

Beilstein J. Org. Chem. 2021, 17, 1814–1827, doi:10.3762/bjoc.17.124

Graphical Abstract
  • ]. Penicillium species belong to the Pezizomycotina, a subdivision within the Ascomycotina including several species that are closely associated with humans at many different levels. Aside from being a source of many medically relevant compounds including antibiotics like penicillin they offer food sources in
PDF
Album
Review
Published 28 Jul 2021

Chemical approaches to discover the full potential of peptide nucleic acids in biomedical applications

  • Nikita Brodyagin,
  • Martins Katkevics,
  • Venubabu Kotikam,
  • Christopher A. Ryan and
  • Eriks Rozners

Beilstein J. Org. Chem. 2021, 17, 1641–1688, doi:10.3762/bjoc.17.116

Graphical Abstract
PDF
Album
Review
Published 19 Jul 2021

Copper-mediated oxidative C−H/N−H activations with alkynes by removable hydrazides

  • Feng Xiong,
  • Bo Li,
  • Chenrui Yang,
  • Liang Zou,
  • Wenbo Ma,
  • Linghui Gu,
  • Ruhuai Mei and
  • Lutz Ackermann

Beilstein J. Org. Chem. 2021, 17, 1591–1599, doi:10.3762/bjoc.17.113

Graphical Abstract
  • Feng Xiong Bo Li Chenrui Yang Liang Zou Wenbo Ma Linghui Gu Ruhuai Mei Lutz Ackermann Key Laboratory of Coarse Cereal Processing, Ministry of Agriculture and Rural Affairs, College of Food and Biological Engineering, Chengdu University, Chengdu 610106, P.R. China Antibiotics Research and Re
  • -evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, School of Pharmacy, Chengdu University, Chengdu 610052, P.R. China Institut für Organische und Biomolekulare Chemie, Georg-August-Universität Göttingen, Tammannstraße 2, 37077 Göttingen, Germany and 4Wöhler Research
PDF
Album
Supp Info
Full Research Paper
Published 08 Jul 2021

Analogs of the carotane antibiotic fulvoferruginin from submerged cultures of a Thai Marasmius sp.

  • Birthe Sandargo,
  • Leon Kaysan,
  • Rémy B. Teponno,
  • Christian Richter,
  • Benjarong Thongbai,
  • Frank Surup and
  • Marc Stadler

Beilstein J. Org. Chem. 2021, 17, 1385–1391, doi:10.3762/bjoc.17.97

Graphical Abstract
  • : antibiotics; Basidiomycota; carotane; fulvoferruginin; Marasmius; sesquiterpenoid; Introduction The family Marasmiaceae (Agaricomycetes, Basidiomycota) presently contains ten genera with Marasmius Fr. being the predominant one (currently comprising over 600 recognized species). Most of these fungi are
PDF
Album
Supp Info
Full Research Paper
Published 04 Jun 2021

N-tert-Butanesulfinyl imines in the asymmetric synthesis of nitrogen-containing heterocycles

  • Joseane A. Mendes,
  • Paulo R. R. Costa,
  • Miguel Yus,
  • Francisco Foubelo and
  • Camilla D. Buarque

Beilstein J. Org. Chem. 2021, 17, 1096–1140, doi:10.3762/bjoc.17.86

Graphical Abstract
  • the asymmetric synthesis of a variety of aromatic, heteroaromatic, and aliphatic 1-substituted 2,6-diazaspiro[3.3]heptanes 48, with overall yields ranging from 74 to 94% (Scheme 16). Asymmetric synthesis of β–lactams β-Lactam antibiotics are important drug class of antibacterial agents [83] and in the
PDF
Album
Review
Published 12 May 2021

Prins cyclization-mediated stereoselective synthesis of tetrahydropyrans and dihydropyrans: an inspection of twenty years

  • Asha Budakoti,
  • Pradip Kumar Mondal,
  • Prachi Verma and
  • Jagadish Khamrai

Beilstein J. Org. Chem. 2021, 17, 932–963, doi:10.3762/bjoc.17.77

Graphical Abstract
  • ; Prins cyclization; stereoselective; tetrahydropyran; Introduction 6-Membered saturated oxygen heterocycles, known as tetrahydropyran (THP), are recognized as privileged scaffolds, present in a variety of biologically important natural products, such as polyether antibiotics, marine toxins, pheromones
PDF
Album
Review
Published 29 Apr 2021

β-Lactamase inhibition profile of new amidine-substituted diazabicyclooctanes

  • Zafar Iqbal,
  • Lijuan Zhai,
  • Yuanyu Gao,
  • Dong Tang,
  • Xueqin Ma,
  • Jinbo Ji,
  • Jian Sun,
  • Jingwen Ji,
  • Yuanbai Liu,
  • Rui Jiang,
  • Yangxiu Mu,
  • Lili He,
  • Haikang Yang and
  • Zhixiang Yang

Beilstein J. Org. Chem. 2021, 17, 711–718, doi:10.3762/bjoc.17.60

Graphical Abstract
  • mechanisms [1] in microorganisms ultimately leading to the initiation of antibiotic resistance and survival of the microorganisms [2]. In case of Gram-negative pathogenic bacteria, production of β-lactamases [3] is the main arsenal of these microorganisms against antibiotics. The number of β-lactamases is
  • 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
  • remedies [4]. β-Lactams (BL) have served as the first line antibiotics since the introduction of penicillin. However, due to existence and continuous increase in β-lactamases [5], multidrug therapy is becoming the new modality of bacterial treatment against multiple-drug resistant (MDR) bacteria. Multidrug
PDF
Album
Supp Info
Full Research Paper
Published 12 Mar 2021

Stereoselective syntheses of 3-aminocyclooctanetriols and halocyclooctanetriols

  • Emine Salamci and
  • Yunus Zozik

Beilstein J. Org. Chem. 2021, 17, 705–710, doi:10.3762/bjoc.17.59

Graphical Abstract
  • of the most important conduramines 4 is valienamine (3) [17], which is found as a building block in several aminoglycoside antibiotics [2]. Furthermore, conduramines 4 and their derivatives are used as both inhibitors of glycosidases and useful intermediates in organic synthesis [18]. Halocyclitols
PDF
Album
Supp Info
Full Research Paper
Published 11 Mar 2021
Other Beilstein-Institut Open Science Activities