β1.4半乳糖基转移酶

A new series of nicotinonitrile derivatives 2 - 7 was designed and synthesized from the starting material ( E )-3-(4-chlorophenyl)-1-(4-methoxyphenyl)prop-2-en-1-one ( 1 ) to assess their molluscicidal activity. The newly synthesized nicotinonitrile compounds 2 - 7 were characterized based on FTIR, 1 H-NMR, and 13 C-APT NMR spectra as well as elemental microanalyses. The target compounds 2 - 7 were screened for their toxicity effect against M. cartusiana land snails and were compared to Acetamiprid as a reference compound...

A rapid, efficient, and original synthesis of novel pyrido[3,2,1- de ]phenanthridin-6-ones is reported. First, the key cinnamamide intermediates 8a - f were easily prepared from commercial substituted anilines, cinnamic acid, and 2-bromobenzylbromide in a tandem amidation and N -alkylation protocol. Then, these N -aryl- N -(2-bromobenzyl) cinnamamides 8a - f were subjected to a TFA-mediated intramolecular Friedel-Crafts alkylation followed by a Pd-catalyzed direct C-H arylation to obtain a series of potentially bioactive 4-phenyl-4,5-dihydro-6 H ,8 H -pyrido[3,2,1- de ]phenanthridin-6-one derivatives 4a - f in good yields...

The present study aimed to develop potent carbonic anhydrase inhibitors (CAIs). The design of the target compounds was based on modifying the structure of the ureido-based carbonic anhydrase inhibitor SLC-0111. Six series of a substituted benzoylthioureido core were prepared featuring different zinc-binding groups; the conventional sulphamoyl group 4a-d and 12a-c , its bioisosteric carboxylic acid group 5a-d and 13a-c or the ethyl carboxylate group 6a-d and 14a-c as potential prodrugs. All compounds were assessed for their carbonic anhydrase (CA) inhibitory activity against a panel of four physiologically relevant human CA isoforms hCA I and hCA II, and hCA IX, and hCA XII...

The nucleocapsid protein (NP) is one of the main proteins out of four structural proteins of coronaviruses including the severe acute respiratory syndrome coronavirus 2, SARS-CoV-2, discovered in 2019. NP packages the viral RNA during virus assembly and is, therefore, indispensable for virus reproduction. NP consists of two domains, i.e., the N- and C-terminal domains. RNA-binding is mainly performed by a binding pocket within the N-terminal domain (NTD). NP represents an important target for drug discovery to treat COVID-19...

The current study describes the synthesis, physicochemical characterization and cytotoxicity evaluation of a new series of pyrrole derivatives in order to identify new bioactive molecules. The new pyrroles were obtained by reaction of benzimidazolium bromide derivatives with asymmetrical acetylenes in 1,2-epoxybutane under reflux through the Huisgen [3 + 2] cycloaddition of several ylide intermediates to the corresponding dipolarophiles. The intermediates salts were obtained from corresponding benzimidazole with bromoacetonitrile...

A series of gold(I) (4a-4h, 5a-5b) and silver(I) (3a-3h) complexes of 1,2,4-triazolylidene and imidazolylidene based N-heterocyclic carbene ligands were prepared and the antibacterial activities of these complexes have been evaluated. The complexes were characterised using 1 H-NMR, 13 C-NMR, HRMS and in the cases of 3a, 3c, 4b and 5b by X-ray crystallography. The gold(I) complexes with phenyl substituents (4a-4d) were found to have potent antibacterial activity against Gram-positive bacteria, with the complexes of the 1,2,4-triazolylidene ligands being more active (4c, MIC = 4-8 μg mL-1 against Enterococcus faecium and 2 μg mL-1 against Staphylococcus aureus ) than the analogous imidazolylidene complexes 4a and 4b (4a, MIC = 64 μg mL-1 against E...

A series of alkyl/aryl/aralkylamines or amino acids appended tetrahydro-2H-1,3,5-thiadiazine-2-thiones (4a-i, 5a-g, 6 and 7) were synthesized via one pot domino synthesis. The synthesis involved reacting alkyl/aryl/aralkylamines or amino acids with carbon disulfide employing basic aqueous medium and further cyclization with formaldehyde and alkyl/aryl/aralkylamines or amino acids. In addition, the carboxy-functionalized 1,3,5-thiadiazine-2-thione 6 was further subjected to esterification. All the structures were confirmed through spectral techniques i...

Coleus (Plectranthus scutellarioides [L.] R.Br.[syn.: Solenostemon scutellarioides]) is a perennial plant in the Lamiaceae family. It produces variegated leaves of various colors. It is commonly cultivated as an ornamental plant or grown in commercial greenhouses (Garibaldi et al. 2019). Phelipanche aegyptiaca Pers. is a dicotyledonous holoparasitic flowering plant that parasitizes more than 30 food crops (e.g., tomato, sunflower, and chickpea), ornamental crops, and others in different parts of the world, causing heavy economic losses (Nosratti et al...

Encouraged by the potent anti-depression activities of incensole (1) and incensole acetate (2) isolated from the resin of Boswellia papyrifera in our previous work, different derivatives of 1 and 2 were synthesized in the present study. The reaction of 1 with m-CPBA afforded the mono-epoxide derivative 3a, while the same reaction with 2 led to three different epoxide derivatives 3a, 3b, and 3c. Oxidation of 1 with PCC to get compound 3b, however along with the target 3b, the reaction gave three interesting side products (3c-3e)...

Although 1,2σ5 λ5 -oxaphosphetanes have been known for a long time, the "low-coordinate" 1,2σ3 λ3 -oxaphosphetanes have only been known since their first synthesis in 2018 via decomplexation. Apart from ligation of this P-heterocycle to gold(I)chloride and the oxidation using ortho -chloranil, nothing on their chemistry has been reported so far. Herein, we describe the synthesis of new 1,2σ3 λ3 -oxaphosphetane complexes ( 3a - e ) and free derivatives ( 4a - e ), as well as reactions of 4a with chalcogens and/or chalcogen transfer reagents, which yielded the P -chalcogenides ( 14 - 16a ; Ch = O, S, Se)...

We introduce phosphorescent platinum aryl acetylide complexes supported by tert -butyl-isocyanide and strongly σ-donating acyclic diaminocarbene (ADC) ligands. The precursor complexes cis -[Pt(CN t Bu)2 (C≡CAr)2 ] ( 4a-4f ) are treated with diethylamine, which undergoes nucleophilic addition with one of the isocyanides to form the cis -[Pt(CN t Bu)(ADC)(C≡CAr)2 ] complexes ( 5a-5f ). The new compounds incorporate either electron-donating groups (4-OMe and 4-NMe2 ) or electron-withdrawing groups [3,5-(OMe)2 , 3,5-(CF3 )2 , 4-CN, and 4-NO2 ] on the aryl acetylide...

The bridging MeCN ligand in the dicopper(I) complexes [(DPFN)Cu2 (μ,η1  : η1 -MeCN)][X]2 (X=weakly coordinating anion, NTf2 (1 a), FAl[OC6 F10 (C6 F5 )]3 (1 b), Al[OC(CF3 )3 ]4 (1 c)) was replaced by white phosphorus (P4 ) or yellow arsenic (As4 ) to yield [(DPFN)Cu2 (μ,η2  : η2 -E4 )][X]2 (E=P (2 a-c), As (3 a-c)). The molecular structures in the solid state reveal novel coordination modes for E4 tetrahedra bonded to coinage metal ions. Experimental data and quantum chemical computations provide information concerning perturbations to the bonding in coordinated E4 tetrahedra...

Starting from [Ru(pyO)2 (nbd)] 1 and a N,P,N-tridentate ligand ( 2a : PhP(pic)2 , 2b : PhP(pyO)2 ) (nbd = 2,5-norbornadiene, pic = 2-picolyl = 2-pyridylmethyl, pyO = 2-pyridyloxy = pyridine-2-olate), the compounds [PhP(μ-pic)2 (μ-pyO)Ru(κ2 -pyO)] ( 3a ) and [PhP(μ-pyO)3 Ru(κ2 -pyO)] ( 3b ), respectively, were prepared. Reaction of compounds 3 with CO and CN t Bu afforded the opening of the Ru(κ2 -pyO) chelate motif with the formation of compounds [PhP(μ-pic)2 (μ-pyO)Ru(κ- O -pyO)(CO)] ( 4a ), [PhP(μ-pic)2 (μ-pyO)2 Ru(CN t Bu)] ( 5a ), [PhP(μ-pyO)4 Ru(CO)] ( 4b ) and [PhP(μ-pyO)4 Ru(CN t Bu)] ( 5b )...

Objectives: Alpha-amylase and alpha-glucosidase enzyme inhibition is an effective and rational approach for controlling postprandial hyperglycemia in type II diabetes mellitus (DM). Several inhibitors of this therapeutic class are in clinical use but are facing challenges of safety, efficacy, and potency. Keeping in view the importance of these therapeutic inhibitors, in this study we are reporting 10 new oxadiazole analogs 5 (a-g) & 4a (a-c) as antidiabetic agents. Materials and Methods: The newly synthesized derivatives 5 (a-g) & 4a (a-c) were characterized using different spectroscopic techniques including FTIR,1 HNMR, 13 CNMR, and elemental analysis data...

Regioselective cyclocondensation of 2,4-diacetyl-5-hydroxy-5-methyl-3-(3-nitrophenyl/4-nitrophenyl)cyclohexanones 1a , b with cyanothioacetamide afforded the corresponding 7-acetyl-4-cyano-1,6-dimethyl-6-hydroxy-8-(3- and -4-nitrophenyl)-5,6,7,8-tetrahydrosoquinoline-3(2 H )-thiones 2a , b . Reaction of compounds 2a , b with ethyl iodide, 2-chloroacetamide ( 4a ), or its N -aryl derivatives 4b - e in the presence of sodium acetate trihydrate gave 3-ethylthio-5,6,7,8-tetrahydroisoquinoline 3 and (5,6,7,8-tetrahydroisoquinolin-3-ylthio)acetamides 5a - i , respectively...

BACKGROUND: Anastomotic leakage is the most important surgical complication following esophagectomy. A major cause of leakage is ischemia of the gastric tube that is used for reconstruction of the gastrointestinal tract. Generalized cardiovascular disease, expressed by calcifications of the aorta and celiac axis stenosis on a pre-operative CT scan, is associated with an increased risk of anastomotic leakage. Laparoscopic ischemic conditioning (ISCON) aims to redistribute blood flow and increase perfusion at the anastomotic site by occluding the left gastric, left gastroepiploic and short gastric arteries prior to esophagectomy...

OBJECTIVE: The current objective was to synthesize biologically active Isatin derivatives. For this purpose, six (06) chemical entities of Isatin derivatives such as 3a-3c and 4a-4c were synthesized from Isatin substrate. METHODS: The pure compounds were characterized with the help of 1 H-NMR, FT-IR, EIMS spectroscopic techniques. The synthesized amines 3a-3c and hydrazones 4a-4c were evaluated for their toxicity potential with the help of brine shrimp bioassay...

Trifluoromethylated nucleosides, such as trifluridine, have widespread applications in pharmaceuticals as anticancer and antiviral agents. However, site-selective addition of a trifluoromethyl group onto a nucleobase typically requires either inconvenient multi-step synthesis or expensive trifluoromethylation reagents, or results in low yield. This article describes a simple, scalable, and high-yielding protocol for late-stage direct trifluoromethylation of pyrimidine nucleosides via a microwave-irradiated pathway...

A simple, efficient and eco-friendly procedure for the synthesis of isoxazole derivatives (4a-4h) using one-pot three-component reaction between substituted aldehydes (1a), methyl acetoacetate (2a) and hydroxylamine hydrochloride (3a) has been achieved in presence of Cocos nucifera L. juice, Solanum lycopersicum L. juice and Citrus limetta juice respectively. The homogeneity of synthesized compounds was confirmed by melting point and thin layer chromatography. The synthesized compounds were characterized by using 1 H NMR, FTIR and CHN analyses and evaluated for in vitro herbicidal activity against Raphanus sativus L...

Spontaneous S -alkylation of methimazole ( 1 ) with 1,2-dichloroethane (DCE) into 1,2-bis[(1-methyl-1 H -imidazole-2-yl)thio]ethane ( 2 ), that we have described recently, opened the question about its formation pathway(s). Results of the synthetic, NMR spectroscopic, crystallographic and computational studies suggest that, under given conditions, 2 is obtained by direct attack of 1 on the chloroethyl derivative 2-[(chloroethyl)thio]-1-methyl-1 H -imidazole ( 3 ), rather than through the isolated stable thiiranium ion isomer, i...