Currently there are several irreversible BTK inhibitors targeting Cys481 residue under preclinical or clinical development. However, most of these inhibitors also targeted other kinases such as BMX, JAK3, and EGFR that bear the highly similar active cysteine residues. Through a structure-based d...

The novel methacrylic monomer, 4-nitro-3-methylphenyl methacrylate (NMPM) was synthesized by reacting 4-nitro-3-methylphenol dissolved in ethyl methyl ketone (EMK) with methacryloyl chloride in the presence of triethylamine as a catalyst. The homopolymer and copolymers of NMPM with glycidyl meth...

In this paper, we report the synthesis, growth and characterization of a new organic NLO single crystal of NMPMN (N′-[(Z)-(4-methylphenyl)methylidene]-4-nitrobenzohydrazide), for the first time. The single crystal was grown by slow evaporation method at room temperature. The cell dimensions obt...

In the current work a new third-order nonlinear optical organic single crystal of (2E)-3-(4-Methylphenyl)-1-(3-nitrophenyl) prop-2-en-1-one (ML3NC) has been grown with well-defined morphology using the slow evaporation solution growth technique. X-ray diffraction technique was used to confirm th...

We explored the facile alkylation of 4-nitrobenzotriazole under basic conditions and the synthesized derivatives were tested for their potential ADP induced platelet aggregation inhibition activity in comparison with standard drug ticagrelor (selective P2Y12 inhibitor). The nitro group at 4-posi...

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biologically evaluated in vitro. In addition,...

N-Acetylglucosaminylinositol (GlcNAc-Ins)-deacetylase (MshB) and mycothiol-S-conjugate amidase (Mca), structurally related amidases present in mycobacteria and other Actinomycetes, are involved in the biosynthesis of mycothiol and in the detoxification of xenobiotics as their mycothiol-S-conjuga...

New examples of substituted thiazole derivatives carrying different heterocyclic ring systems at C-2 position were prepared via the reaction of several allenyl isothiocyanates with nucleophiles such as imidazoles, pyrazoles, benzimidazoles, indazole, 1,2,3-triazole, 1,2,4-triazole, and 1H-benzot...

The objective was to identify and characterize peptides from digested total protein (DTP) and isolated protein fractions (DPF), and their potential antioxidant, anti-inflammatory and anti-atherosclerotic effects, from chia seed (Salvia hispanica L.). Total protein and protein fractions from chia...

This work describes a solid-phase synthetic method for building a compound library of N-alkyl-4-alkylamino-1-aryl-1H-pyrazolo[3,4-d]pyrimidine-6-carboxamide derivatives, that are based on the biologically active 1-aryl-1H-pyrazolo[3,4-d]pyrimidine scaffold. In the first step of this synthetic se...

A series of 4-arylmethyl-1-phenylpyrazole and 4-aryloxy-1-phenylpyrazole compounds B were designed, synthesized, and evaluated for their potential as new-generation androgen receptor (AR) antagonists therapeutically effective against castration-resistant prostate cancer (CRPC). Introduction of a...

Further investigation of the potential anticonvulsant activity of the enaminones was attempted to discern the possible role of metabolites as the active/co-active entities of the esters of the enaminones. A series of 5-methyl-2-cyclohexene enaminones, the hypothesised metabolites corresponding t...

A highly specific and efficient LC-QTOF mass spectrometric method was developed for the separation and characterization of process related substances and the major degradation products in alogliptin benzoate and its tablets. The separation was performed on Phenomenex Gemini-NX C18 column (250 mm...

Composites prepared from aerosil A380 and liquid crystals (LCs) of 4-n-alkyl-4′-cyanophenyl benzoate type, with four to six carbon atoms in the alkyl chain were investigated by infrared spectroscopy. Their high silica content (of 2–7 g aerosil/1 g of LC) was given by thermogravimetric investig...

A novel and mild method for the synthesis of fused polycyclic indoles of [1,2-a]indol-10-imines via a Cu(OTf)2-catalyzed the intramolecular cyclization of N-(2-cyanophenyl)indoles in the presence of diaryliodonium salts has been developed.

2,5-Dimethoxyphenethylamines (2C compounds) are 5-HT2A/2C receptor agonists that induce hallucinogenic effects. N-methoxybenzylation of 2C compounds markedly increases their affinity for 5-HT2A receptors, and two such analogs, 2-(4-chloro-2,5-dimethoxyphenyl)-N-[(2-methoxyphenyl)methyl]ethanamin...

Chalcone derivative of (2E)‑1‑(3‑bromo‑2‑thienyl)‑3‑(2,5‑dimethoxyphenyl) prop‑2‑en‑1‑one (BTD) molecule has been deliberated for spectroscopic properties experimentally and theoretically. The title compound was characterized by FT-IR, FT-Raman and UV–Vis analyses. The structural activity and v...

A series of 3-[2-{[(3-methyl-1-phenylbutyl)amino]carbonyl}-4-(phenoxymethyl)phenyl]propanoic acid analogs were synthesized and evaluated for their in vitro potency. In most cases, introduction of one or two substituents into the two phenyl moieties resulted in the tendency of an increase or rete...

RésuméDes feuilles du Buxus balearica Willd. ont été retirés: la cyclomicrophylline-B, les cycloprotobuxines A, C et D, la baléabuxine (N-isobutyryl-baléabuxine-F, la buxamine-E et le buxaminol-E, alcaloïdes déjà décrits, et 6 alcaloïdes nouveaux: N-isobutyryl- et N-benzoyl-baléabuxid...

Various trialkyl phosphates were investigated as model compounds for DNA-phosphotriesters for their stability in neutral or alkaline conditions. The results show that phosphotriesters were highly stable even at strongly alkaline pH, with the exception of diethyl 2-hydroxyethyl phosphate (DHP). T...