10.1016/j.bmcl.2012.04.036
The research focuses on the development of sulfonyl-morpholinopyrimidines as a novel class of selective mTOR kinase inhibitors, which are potential therapeutic targets for tumor growth inhibition. The study began with high-throughput screening, identifying compound 1 as a starting point due to its good physicochemical properties and selectivity over PI3Kα. The researchers prepared libraries of related analogs to establish structure-activity relationships (SAR), particularly noting the importance of a hydrogen bond donor motif at the 4-position of the phenyl ring. Experiments involved synthesizing various compounds, such as sulfone analogs (Scheme 1) and aryl analogs (Scheme 2), and evaluating their mTOR potency, selectivity over PI3Kα, and other pharmacokinetic properties. Key reactants included amidine hydrochloride, keto-ester, morpholine, and various thiols, among others. Analyses used to assess the compounds included enzyme assays, cellular assays, cytochrome P450 inhibition assays, hERG ion channel assays, and measurements of aqueous solubility and lipophilicity. The research resulted in the identification of urea compounds, such as 32, that showed improved mTOR inhibition in both enzyme and cellular assays while maintaining selectivity over PI3Kα.
10.1155/2012/767941
The research focuses on the synthesis, characterization, and antimicrobial studies of a new Mannich base, N-[morpholino(phenyl)methyl]acetamide (MBA), and its metal complexes with cobalt(II), nickel(II), and copper(II). The ligand MBA was synthesized using acetamide, benzaldehyde, and morpholine, and characterized by spectral studies including IR, UV-Visible, NMR, and mass spectrometry. The metal chelates were prepared by reacting MBA with metal salts, and further characterized by elemental analysis, IR, UV spectral studies, and magnetic moment measurements. The antimicrobial activities of MBA and its complexes were evaluated against various bacterial and fungal species using the disc diffusion method. The study found that the Co(II) nitrato complex exhibited the highest activity, suggesting that chelation enhances the antimicrobial properties of the ligand.
10.1016/j.ejmech.2015.05.036
The study presents the design, synthesis, and biological evaluation of novel condensed pyrrolo[1,2-c]pyrimidines featuring a morpholine moiety, which were developed as inhibitors of PI3Kα, a key enzyme in cellular survival and apoptosis pathways, often aberrantly activated in cancer. The chemicals used in the study include a series of synthesized compounds (6a-d, 8a-d, 10a,b, and 12a-e) that serve as potential PI3Kα inhibitors. These compounds were designed based on the pharmacophore model for PI3K p110α inhibitors and were tested for their inhibitory activity and selectivity towards different PI3K isoforms. The purpose of these chemicals is to potentially provide a new avenue for cancer therapy by targeting the PI3K signaling pathway, with the aim of inhibiting uncontrolled cell proliferation and migration associated with tumor formation. The study also involved molecular docking simulations to predict the binding affinity and mode of these compounds within the p110α active site, and their cytotoxic activities were evaluated against specific cancer cell lines.
10.1016/j.inoche.2008.05.023
The research aimed to develop a new microwave-assisted synthesis methodology for the preparation of ferrocene amides, which are derivatives of ferrocene with widespread applications in chemistry. The study utilized a direct 1H-Benzotriazole/SOCl2 methodology to derivatize ferrocene carboxylic acid, creating N-ferrocenoyl benzotriazole as a novel starting material for the functionalization of the ferrocene ring. This compound was then reacted with mono- and di-amines under microwave irradiation to synthesize ferrocene mono- and di-amides in high purity and good yield. The researchers concluded that microwave synthesis offers advantages in terms of reaction time and product yield compared to conventional methods, and their approach using N-ferrocenoyl benzotriazole as a starting material is a new, easy, and fast synthetic method for the preparation of ferrocene amides. The chemicals used in the process included ferrocene carboxylic acid, 1H-benzotriazole, thionyl chloride (SOCl2), and various amines such as ammonium hydroxide, cyclohexylamine, piperidine, morpholine, and others listed in Table 1 of the article.
10.1039/b905153h
The study investigates the synthesis, characterization, and biological evaluation of a series of 4,4￠-dimorpholyl-methanes (4a–h) as potential low-toxicity biocides. These compounds were synthesized using a solventless microwave-assisted method from various aldehydes and morpholine, yielding eight different biocides. The synthesized compounds were characterized using FT-IR, 1H, 13C, and 2D NMR spectroscopy, and single-crystal X-ray diffraction analysis was performed on four of the derivatives. The biocides were tested for acute toxicity using the Microtox assay with Photobacterium phosphoreum (Vibrio fischeri) and for antibacterial activity against Bacillus subtilis, Escherichia coli, and Pseudomonas fluorescens. The results showed varying degrees of toxicity and biocidal activity, with compounds 4a, 4b, and 4c exhibiting low toxicity while maintaining significant biocidal potency. A QSAR study was conducted to correlate molecular descriptors with the acute toxicity of the compounds, identifying log P, ESP, and d13C(C5) as key descriptors. The study concludes that the selected compounds could be used as ecological biocides in industrial applications, particularly in the petroleum industry.
10.1111/j.2042-7158.1968.tb09886.x
The research investigates the synthesis of 2-hydroxy-2- and 4-alkylmorpholines through ring closure of phenacyl hydroxyalkylamines and examines their pharmacological effects. The study aims to explore the influence of structure on the ring closure reaction and to understand the relationship between the synthesized compounds and the reversed esters of pethidine. Key chemicals used include phenacyl bromides, amino-alcohols, and various substituted morpholines. The researchers found that the ring closure reaction was influenced by the steric effect of additional substituents on the nitrogen atom, rather than electronic effects. The pharmacological screening revealed that some compounds produced convulsions, while others showed weak effects on the autonomic nervous system, but none demonstrated significant analgesic activity in mice. The study concludes that the analogy between 2,2-substituted morpholines and 3,3-substituted piperidines does not hold, and the pharmacological activity of these compounds is not solely dependent on their pKa values.
10.1007/s10593-008-0093-6
The study focused on the reaction of phenyl glycidyl ether with various heterocyclic compounds to synthesize new compounds with potential biological activity. The chemicals used included 5,5-dimethylhydantoin, morpholine, benzotriazole, benzimidazole, pyrrolidone, phthalimide, and 8-hydroxyquinoline. These heterocyclic compounds served as reactants to form N-(2-hydroxy-3-phenoxypropyl) derivatives, which are of interest due to their potential to contain pharmacophoric fragments that could lead to the discovery of new biologically active substances. The purpose of the study was to develop a one-stage method for synthesizing these derivatives, which could be applied in preparative chemistry and contribute to the development of new drugs.
10.1021/om900120v
This research presents the synthesis, structural characterization, and catalytic activity of a series of trisguanidinate lanthanide complexes, which were found to be efficient catalysts for the mild amidation of aldehydes with amines. The study aimed to explore the reactivity of these complexes, particularly in the context of their potential as catalysts for organic synthesis reactions. The researchers synthesized various trisguanidinate lanthanide complexes with different central metals and guanidinate anions, and tested their catalytic activity for the amidation reaction. The results showed that these complexes, especially those with lanthanum, effectively catalyzed the amidation of a wide range of substrates, including secondary cyclic amines like pyrrolidine, piperidine, and morpholine. One of the key intermediates in this process, a lanthanum amido complex, was also isolated and characterized. The chemicals used in the synthesis included anhydrous LaCl3, NdCl3, lithium salts of guanidinate ligands, and various amines and aldehydes for the catalytic tests. The research concluded that these trisguanidinate lanthanide complexes have potential applications in organic synthesis due to their high catalytic efficiency and broad substrate scope.
C
C:Corrosive;
