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Search for "resistance" in Full Text gives 329 result(s) in Beilstein Journal of Organic Chemistry. Showing first 200.
Rapid access to the core of malayamycin A by intramolecular dipolar cycloaddition
Beilstein J. Org. Chem. 2025, 21, 2542–2547, doi:10.3762/bjoc.21.196
- biological agents has led to a rapid emergence of resistance, which in turn diminishes the national-wide and even global-wide food security. Moreover, toxins produced by fungi in diseased crops have serious impacts on animal and human health [2]. There remains high demand to develop new antifungal compounds
- action may not be consistent with those of known fungicide classes. This encouraging characteristic indicates its potential to overcome resistance to other fungicides [6][7][8]. Structurally, malayamycin A belongs to a class of modified nucleosides that mimic UDP (uridine 5′-diphosphate)-linked
Synthesis and characterization of a isothiouronium-calix[4]arene derivative: self-assembly and anticancer activity
Beilstein J. Org. Chem. 2025, 21, 2535–2541, doi:10.3762/bjoc.21.195
- represents a promising approach to overcoming several limitations associated with traditional monovalent therapeutics, including drug resistance, off-target effects, high dosage requirements, and insufficient specificity. This strategy may pave the way for next-generation anticancer therapies more effective
Rotaxanes with integrated photoswitches: design principles, functional behavior, and emerging applications
Beilstein J. Org. Chem. 2025, 21, 2345–2366, doi:10.3762/bjoc.21.179
- proximity to the fluorescent stopper. The reported findings involving dithienylethene-based rotaxanes prove their promising future in materials applications, mainly due to their high photofatigue resistance. Spiropyran While most spiropyran-based rotaxanes have the photoswitchable unit located on the axle
Halogenated butyrolactones from the biomass-derived synthon levoglucosenone
Beilstein J. Org. Chem. 2025, 21, 2297–2301, doi:10.3762/bjoc.21.175
- sofosbuvir (2). Fluorination at C2 in the nucleoside results in metabolic stability and resistance to hydrolysis as it destabilizes the formation of a C1 oxocarbenium ion [5][6]. Trifluoromethylated γ-butyrolactones also find applications as antiviral agents, for example, lactone 4 which has activity against
C2 to C6 biobased carbonyl platforms for fine chemistry
Beilstein J. Org. Chem. 2025, 21, 2103–2172, doi:10.3762/bjoc.21.165
- -designed Pd@S-1 and H-beta zeolite catalytic system, exhibiting high resistance to coking in presence of NH3. Subsequent carboxylation with CO2 and hydrogenation over Rh/C as catalyst led to racemic proline, an important precursor for pharmaceuticals, in quantitative yield. ᴅ-Proline was then obtained in
Solar thermal fuels: azobenzene as a cyclic photon–heat transduction platform
Beilstein J. Org. Chem. 2025, 21, 2036–2047, doi:10.3762/bjoc.21.159
- [35][36][37][38][39][40][41]. Notably, the utilization of azobenzene-based materials in solar thermal storage applications is gaining considerable attention due to their advantages in low synthesis cost, facile molecular design, exceptional cycling stability, and superior fatigue resistance [6][8
- enables each azobenzene unit to store >200% more energy than isolated molecules, while achieving multi-order-of-magnitude improved storage lifetime and resistance to material degradation during repeated cycling. Feng and co-workers covalently grafted azobenzene groups onto RGO templates (Figure 3b) and
Photoswitches beyond azobenzene: a beginner’s guide
Beilstein J. Org. Chem. 2025, 21, 1808–1853, doi:10.3762/bjoc.21.143
- forward and backward isomerisation can occur simultaneously. Moreover, some unwanted photochemical side reactions ΦS can occur, as shown in the Equation 4: A is one state of the photoswitch, B the second state, and B’ a generic degradation product. Fatigue resistance measures how many times the
- photoswitch can be switched before it is degraded by side reactions. It is typically reported as cyclability Z50, which “is the number of cycles required to reduce the initial absorbance at a specific wavelength by 50%” [3]. The quantum yield ΦS of these side reactions determines the resistance to fatigue of
- the E-chair isomer [51]. All the compounds show excellent resistance to fatigue. The behaviour of some (hetero)diazocines was also studied in water and solvent mixtures [50][51]. Interestingly, N-acetyl-diazocine possesses overall comparable properties and a longer thermal half-life, and it is also
Research progress on calixarene/pillararene-based controlled drug release systems
Beilstein J. Org. Chem. 2025, 21, 1757–1785, doi:10.3762/bjoc.21.139
- focusing on the tumor microenvironment to develop supramolecular systems that are highly specific and capable of responding to multiple stimuli. These advanced systems aim to target and penetrate tumor cells effectively, mitigate drug resistance caused by tumor cell uptake, and ultimately enhance clinical
Continuous-flow-enabled intensification in nitration processes: a review of technological developments and practical applications over the past decade
Beilstein J. Org. Chem. 2025, 21, 1678–1699, doi:10.3762/bjoc.21.132
- stainless steel demonstrates corrosion resistance in individual exposures to concentrated nitric acid or sulfuric acid due to passivation layer formation. However, during nitration using both acids simultaneously, progressive HNO3 consumption and water generation may reduce acid concentrations below
Tautomerism and switching in 7-hydroxy-8-(azophenyl)quinoline and similar compounds
Beilstein J. Org. Chem. 2025, 21, 1404–1421, doi:10.3762/bjoc.21.105
- resistance [1][2][3][4]. In addition to their conventional use, azodyes have unique optical properties, defined by the E/Z isomerization [5][6] and by the tautomeric proton exchange [3][7][8][9][10][11], when a OH or NH group is present on a suitable position in the molecule. Both processes are strongly
N-Salicyl-amino acid derivatives with antiparasitic activity from Pseudomonas sp. UIAU-6B
Beilstein J. Org. Chem. 2025, 21, 1388–1396, doi:10.3762/bjoc.21.103
- Biochemistry, Federal University of Lafia, Nigeria 10.3762/bjoc.21.103 Abstract Pseudomonads strains represent a promising source of bioactive compounds with potential pharmaceutical applications. The necessity to find new drugs is underscored by the increased concern over antimicrobial resistance in the
Investigations of amination reactions on an antimalarial 1,2,4-triazolo[4,3-a]pyrazine scaffold
Beilstein J. Org. Chem. 2025, 21, 1126–1134, doi:10.3762/bjoc.21.90
- of action and a longer half-life (to improve total cure rates and forestall the development of drug resistance) [2]. Unfortunately, partial artemisinin resistance has been documented in Southeast Asia for more than a decade, and parasites with partial artemisinin resistance have been detected in
- patient isolates in African geographies [1][2]. P. falciparum isolates have also been detected in various global regions with at least some measure of resistance to all frontline ACT partner drugs [1][2]. New chemotherapeutics are urgently needed to manage malarial disease and forestall or circumvent ACT
Gold extraction at the molecular level using α- and β-cyclodextrins
Beilstein J. Org. Chem. 2025, 21, 1116–1125, doi:10.3762/bjoc.21.89
- , metallic gold is easily reduced to Au− [2]. Adding to the aforementioned properties, the excellent resistance against corrosion makes gold a vital element for use in a wide range of electronic applications. Some common devices that contain gold include smartphones, in which it is used in the circuit boards
- and/or audio, bringing the benefit of enhanced signal transmission (because of its high conductivity), reliability and durability (a direct result of its high resistance to oxidation) [7][8]. In medicine, gold is used as an inert and non-allergenic alternative metal in devices such as pacemakers [9
4-(1-Methylamino)ethylidene-1,5-disubstituted pyrrolidine-2,3-diones: synthesis, anti-inflammatory effect and in silico approaches
Beilstein J. Org. Chem. 2025, 21, 817–829, doi:10.3762/bjoc.21.65
- (3.032 eV) and 5e (2.694 eV) emphasize their strong electron-accepting capabilities, while the high IE of 5c (6.429 eV) indicates its resistance to electron donation. These findings suggest that compounds 5c and 5e are highly reactive and suitable for applications requiring active electron transfer
Recent advances in the electrochemical synthesis of organophosphorus compounds
Beilstein J. Org. Chem. 2025, 21, 770–797, doi:10.3762/bjoc.21.61
- resistance, and maintain ion balance (e.g., LiClO4, n-Bu4NBF4), and active electrolytes, which participate directly in redox reactions, acting as oxidizing or reducing agents (e.g., H2SO4, Et4NOH). Choosing the proper electrolyte affects reaction efficiency, selectivity, and overall performance. Electrodes
- was performed. The use of graphite and RVC gave good results. Nickel, graphite, and platinum electrodes were examined as the cathodes. Results showed that platinum and nickel performed better than graphite in the cathode due to their higher conductivity and lower electrical resistance. When platinum
Photocatalyzed elaboration of antibody-based bioconjugates
Beilstein J. Org. Chem. 2025, 21, 616–629, doi:10.3762/bjoc.21.49
- diseases: ADCs have shown remarkable success in treatment of highly refractory diseases. Their ability to overcome resistance makes them valuable options for patients who previously had limited treatment choices. ADCs consist of three main components (Figure 1): (1) Monoclonal antibody (mAb): The antibody
Semisynthetic derivatives of massarilactone D with cytotoxic and nematicidal activities
Beilstein J. Org. Chem. 2025, 21, 607–615, doi:10.3762/bjoc.21.48
- ; nematicidal activity; Introduction Cancer continues to be responsible for morbidity and mortality all over the world. Endophytic fungi have been shown to be an important source of secondary metabolites endowed with interesting cytotoxic activities. However, resistance to cancer therapies is a persistent
- challenge in clinical practice. This resistance often leads to treatment failure and poor survival outcomes for patients [1]. Another ongoing problem is the excessive use of chemical pesticides such as methyl bromide, carbamates, and organophosphates to control plant-parasitic nematodes that has shown a
- negative impact on the environment and human health. Prolonged and widespread applications of these substances have also increased the development of nematode resistance to pesticides [2][3][4]. However, advancements in natural products chemistry have shown that chemical modifications of certain natural
Cryptophycin unit B analogues
Beilstein J. Org. Chem. 2025, 21, 526–532, doi:10.3762/bjoc.21.40
- amines still show nanomolar activity against the MDR cell line KB-V1 (Table 1) with resistance factors FR (being the ratio between IC50 (KB-V1) and IC50 (KB-3-1)) of 25 (1) and 34 (2), thus being comparably much more potent against KB-V1 cells than for example the unit D analogues (FR ≈ 103) [19
- cryptophycins 1 and 2 showed high cytotoxicity with 313 pM (1) and 6.36 nM (2) and outstandingly low resistance factors. Furthermore, the new cryptophycin 1 confirms the correlation between degree of alkylation and cytotoxicity of m-chloro-p-amino unit B derivatives. Since MDR is responsible for over 90% of
Deep-blue emitting 9,10-bis(perfluorobenzyl)anthracene
Beilstein J. Org. Chem. 2025, 21, 515–525, doi:10.3762/bjoc.21.39
- Barnstead NANOpure Ultrapure Water system, producing water with a final resistance of at least 18 MΩ); and silica gel (Sigma-Aldrich, 70–230 mesh, 60 Å). For HPLC separations: acetonitrile (Fisher Scientific ACS grade); toluene (Fisher Scientific, ACS grade); and heptane (Mallinckrodt Chemicals, ACS grade
Synthesis of the aggregation pheromone of Tribolium castaneum
Beilstein J. Org. Chem. 2025, 21, 510–514, doi:10.3762/bjoc.21.38
- harmful to human health and this became a significant challenge to food security [6]. Long-term synthetic pesticide applications to control the red flour beetle has resulted in the development of resistance to organophosphates, pyrethroids, methyl carbamates, and neonicotinoids [7][8]. It became critical
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
- conditions on either biotic or abiotic surfaces. Structurally, biofilms are polymicrobial consortia embedded in an extracellular polymeric substance (EPS) that plays a pivotal role in surface adhesion, enhancement of gene exchange, antimicrobial resistance, and protection against host immune and inflammatory
- infections are associated with biofilm formation, respectively, including serious infections affecting mucosal membranes or on implants yielding serious threats in hospitalized patients [3][4]. Consequently, biofilm-based antibiotic resistance poses a major threat to human health and substantially
- anticancer properties [6]. With concerns about biofilm formation and resistance escalating in the medical field, entomopathogenic fungi have emerged as a promising source of novel bioactive compounds [5]. Our recent exploration of B. neobassiana highlighted this growing interest, affording one tetramic acid
Red light excitation: illuminating photocatalysis in a new spectrum
Beilstein J. Org. Chem. 2025, 21, 296–326, doi:10.3762/bjoc.21.22
- ). Despite this, their catalytic performance was not compromised. The key to their success lies in their resistance to photobleaching, which is a common issue for metal-based photocatalysts that degrade under prolonged exposure to light. The silicon-based phthalocyanin complexes maintained their structural
Synthesis of the 1,5-disubstituted tetrazole-methanesulfonylindole hybrid system via high-order multicomponent reaction
Beilstein J. Org. Chem. 2024, 20, 3077–3084, doi:10.3762/bjoc.20.256
- are found in a plethora of compounds with significant biological and pharmacological relevance [1][2][3][4]. These moieties are indispensable in the design and synthesis of novel drugs aimed at overcoming drug resistance, which is a global health threat [5][6][7]. To date, a strategy to access novel
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
- (Figure 2b). The former analyzes nucleic acid sequences to prioritize BGCs that are worth exploring [20]. For example, it has been shown that tracking characteristic biosynthetic or self-resistance gene(s) can facilitate the discovery of new congeners of a natural product family [21][22]. Function
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