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Synthesis of Some Benzimidazole-Thiophene Hybrids as Potential Urease and Lipase Inhibitors
AbstractIn this study, some benzimidazole-thiophene hybrid compounds containing isatin and salicyl moieties were synthesized and investigated for...
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Phytate metabolism is mediated by microbial cross-feeding in the gut microbiota
Dietary intake of phytate has various reported health benefits. Previous work showed that the gut microbiota can convert phytate to short-chain fatty...
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Economical and Facile Synthesis of Monolignols
Monolignols are efficiently synthesized from the corresponding cheap and readily available cinnamic acids through a borohydride reduction of the...
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Novel synthesis of some heterocycles and their molluscicidal activity against the destructive land snail, Theba pisana
BackgroundTerrestrial snails, specifically Theba pisana , represent significant agricultural pests in the Mediterranean region, particularly in...
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Two new aromatic tenvermectins from mutant Streptomyces avermitilis HU02-06
Two new aromatic tenvermectins (TVMs), 13-oleandrosyl-oleandrosyloxy ST906 ( 1 ) and aromatic TVM B ( 2 ), were isolated from the fermentation broth of Str...
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Synthesis, molecular docking and molecular dynamics simulations, drug-likeness studies, ADMET prediction and biological evaluation of novel pyrazole-carboxamides bearing sulfonamide moiety as potent carbonic anhydrase inhibitors
Pyrazoles are unique bioactive molecules with a versatile biological profile and they have gained an important place on pharmaceutical chemistry....
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Synthesis, Characterization, and Study of Anticancer Activities of New Schiff Bases and 1,3-Oxazepine Containing Drug
AbstractObjective: This study involved the synthesis of new Schiff bases and 1,3-oxazepine derivatives from the baclofen drug and study the...
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A practical guide for the preparation of C1-labeled α-amino acids using aldehyde catalysis with isotopically labeled CO2
Isotopically carbon-labeled α-amino acids are valuable synthetic targets that are increasingly needed in pharmacology and medical imaging. Existing...
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A Mechanism to Transform Complex Salicinoids with Caffeoylquinic Acids in Lepidopteran Specialist Herbivores (Notodontidae)
Larvae of the Salicaceae-adapted Notodontidae have developed a unique mechanism to metabolize the chemical defenses of their Salicaceae host plants....
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Dimeric Transmembrane Structure of the SARS-CoV-2 E Protein
The SARS-CoV-2 E protein is a transmembrane (TM) protein with its N-terminus exposed on the external surface of the virus. At debate is its...
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Host defence peptide plectasin targets bacterial cell wall precursor lipid II by a calcium-sensitive supramolecular mechanism
Antimicrobial resistance is a leading cause of mortality, calling for the development of new antibiotics. The fungal antibiotic plectasin is a...
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Structure-based drug design and characterization of novel pyrazine hydrazinylidene derivatives with a benzenesulfonate scaffold as noncovalent inhibitors of DprE1 tor tuberculosis treatment
In this study, we present a novel series of ( E )-4-((2-(pyrazine-2-carbonyl) hydrazineylidene)methyl)phenyl benzenesulfonate (T1-T8) and 4-(( E )-((( Z )-a...
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Synthesis of some new 2-(substituted-phenyl)imidazo[4,5-c] and [4,5-b]pyridine derivatives and their antimicrobial activities
The synthesis of 5 H -imidazo[4,5- c ]pyridines analogues ( 1a − 1h) and 4 H -imidazo[4,5- b ]pyridines (3a − 3c) was achieved by reacting 3,4-diaminopyridine...
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Structural basis for the dynamic chaperoning of disordered clients by Hsp90
Molecular chaperone heat shock protein 90 (Hsp90) is a ubiquitous regulator that fine-tunes and remodels diverse client proteins, exerting profound...
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Synthesis, Antioxidant, Antifungal and Antibacterial Activities of New Class of Fused Isoxazole-Pyrimidines and Pyrazole-Pyrimidines as Five and Six Membered Heterocyclic Compounds
AbstractOne series of total 5 phenylisoxazolo[4,3- d ]pyrimidine and five series of total 22 pyrazolo[4,3- d ]pyrimidine compounds were designed,...
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Regioselective synthesis and molecular docking studies of functionalized imidazo [1,2-a]pyridine derivatives through MCRs
A efficient protocol has been developed for the synthesis of regioselective imidazo[1,2- a ]pyridine and imidazo[1,2- a ]pyrimidine derivatives through...
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Design, synthesis, and biological evaluation of new biaryl derivatives of cycloalkyl diacetamide bearing chalcone moiety as type II c-MET kinase inhibitors
Many human cancers have been associated with the deregulation of the mesenchymal-epithelial transition factor tyrosine kinase (MET) receptor, a...
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3α-Hydroxybufadienolides in Bufo gallbladders: structural insights and biotransformation
Bufadienolides, naturally occurring steroids primarily found in toads, have garnered attention for their pharmacological properties and ecological...
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Design, Synthesis and Pharmacological Evaluation of Some 2-Methylsulfanyl-1,4-Dihydropyrimidines Derivatives as an Analgesic Agent
Abstract2-Methylsulfanyl-1,4-dihydropyrimidine derivatives were synthesized by alkylation of 1,2,3,4-tetrahydropyrimidines with methyl iodide in the...
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In Vitro Biological Evaluation of Some Synthesized Novel 5-Substituted-2-(substituted)hydazineyl-1,3-thiazolidin-4-ones
AbstractThe 2-[2-(1-(4-chlorophenyl)ethylidene]hydrazineyl-1,3-thiazolidin-4-one ( V ) compound was synthesized via the condensation of...
