Herein we described the design, synthesis and evaluation of a novel series of benzo[d]thiazole derivatives toward an orally active EP1 antagonist. Lead generation studies provided benzo[d]thiazole core from the four designed scaffolds. Optimization of this scaffold in terms of EP1 antagonist pot...

A series of novel 5-benzylated 4-oxo-3,4-dihydro-5H-pyridazino[4,5-b]indoles was synthesized through a newly developed approach. All these compounds were evaluated against DYRK1A, CDK5 and PI3Kα and showed promising inhibitory activities against PI3Kα with most IC50 values in the micromolar ra...

The absorption, excitation, fluorescence and phosphorescence spectra of δ-carboline, 5H-pyrido[3,2-b]indole, have been investigated in non-aqueous solvents of various polarity at room temperature and 77 K. The δ-carboline fluorescence shows time-resolved red shifts, solvatochromic effects, non...

The rhodium-catalyzed reactions of 3-diazoindolin-2-imines with β-enamino esters furnished 2,3-diaminoindoles in excellent yields with wide functional group tolerance. The synthesized 2,3-diaminoindoles could be converted into 5H-pyrazino [2,3-b]indoles via a sequential dehydrogenation/6π-ERC/...

6,7-Dihydrobenzo[c][1,2,5]oxadiazol-4(5H)-one oxime is annelated with acetylene in the KOH/DMSO/H2O system under pressure to give NH- or N-vinyl-5,8-dihydro-4H-[1,2,5]oxadiazolo[3,4-g]indoles in 29 and 68% yields, respectively. These derivatives are readily aromatized with DDQ at room temperatur...

The crystal and molecular structures of the title 2-[(4-phenylpiperazin-1-yl)ethyl], 6, and 2-[(4-methylpiperazin-1-yl)methyl], 7, derivatives of isothiazolo[5,4-b]pyridine were determined. The molecular packing in 6 is influenced by C–H…X (X = N, O) hydrogen bonds and π…π interactions of t...

The synthesis of substituted 3-methylene-2-pyridones via SN2 displacement reaction of nucleophiles bearing a keto group on the acetyl derivative of Baylis–Hillman adducts of acrylonitrile followed by TFA/H2SO4-mediated intramolecular cyclization is described. The utility of these pyridone deriv...

Bacterial collagen-like proteins differ from vertebrate collagens in that they do not contain hydroxyproline, which is seen as a characteristic of the vertebrate collagens, and which provides a significant contribution to the stability of the collagen triple-helix at body temperature. Despite th...

A series of tridentate NˆNˆN iron(II) and cobalt(II) complexes containing N-((pyridin-2-yl)methylene)-quinolin-8-amine derivatives were synthesized and characterized by elemental and spectroscopic analyses. The molecular structure of 1a was confirmed by X-ray diffraction analyses. On treatment w...

A variety of diurethanes mostly based on at least one furanic reagent were prepared using either aliphatic, benzylic or furfurylic diols in conjunction with various monoisocyanates or aliphatic, aromatic and furanic diisocyanates in conjunction with n-butanol and 2-furfuryl alcohol. Study of the...

One of the hallmarks of cancer is increased cell proliferation. Measurements of cell proliferation by estimation of DNA synthesis with several radiolabeled nucleosides have been tested to assess tumor growth. Deoxycytidine can be phosphorylated by deoxycytidine kinase (dCK) and is incorporated i...

An isocratic, ion-paired, reversed-phase high-performance liquid chromatography technique for the quantitative determination of 5-fluoro-2′-deoxycytidine (FdCyd) and 5-trifluoromethyl-2′-deoxycytidine (F3methyldCyd) and their related antimetabolites is described. Extraction and purification of...

Thymidylate synthase (TS) is inhibited by 5-fluoro-2′-deoxycytidine 5′-monophosphate (FdCMP). From initial velocity measurements, the apparent Ki for the binary FdCMP-enzyme complex was about 20 μM. In the presence of 5,10-methylene-5,6,7,8-tetrahydrofolate (CH2H4folate), FdCMP causes a time-...

Studies were performed to determine whether 5-fluoro-2′-deoxycytidine 5′-monophosphate (FdCMP) is an inhibitor of deoxycytidylate hydroxymethylase and whether it could form an isolable covalent complex with the enzyme and the cofactor, 5,10-methylenetetrahydrofolate. The results showed that al...

Stille cross coupling protocols were utilized for the synthesis of 3-(biaryl)-8-oxabicyclo[3.2.1]oct-2-ene-2-carboxylic acid methyl esters, which furnished products in high yields where in some cases Suzuki coupling under the conditions utilized provided complex reaction mixture. Samarium iodide...

The synthesis and resolution of the trifluoromethyl-palladacycle, di-μ-chloro-bis(N,N-dimethyl-(2,2,2-trifluoro-1-phenylethyl)amine-2-C,N)palladium(II) are shown. The utility of the complex and its application in the enantiomeric excess determination of α-amino acids by 19F NMR spectroscopy is...

Due to their immunomodulatory effect, 1,3-β-G from yeast are used as functional ingredients, but reliable methods for their detection in foods are lacking. We have adapted a method based on fluorescence detection with aniline blue to quantify the amount of five commercial yeast β-glucan prepar...

The 1,3-beta-D-Glucan (BDG) assay is widely used for the diagnosis of fungal infections, especially in patients with hematologic malignancies. Some antimicrobials have been reported to cause false-positive results for BDG, but there has been no report on the effect of penicillin G (PCG) on BDG l...

Herein, we report the synthesis of a new series of amide functionalized dicationic benzimidazolium based ionic liquids (DBimILs) and appraised their efficacy towards perceptive esterification of carboxylic acids with alkyl/allyl/aryl halides in presence of triethylamine. The amide groups present...

Many reactions occur as a result of charge imbalance within or between reactive species in reaction vessels that have zero net charge. Here, chemical processes taking place within reaction vessels having net excess charge were studied. For mass spectroscopists, a familiar example of vessels that...