The reference standard N-(4-diethylamino)benzyl-4-methoxy-N-(p-tolyl)benzenesulfonamide (3c) (CB2, Ki=0.5 nM; CB1, Ki=1297 nM; selectivity CB1/CB2=2594) and its corresponding precursor N-(4-diethylamino)benzyl-4-hydroxy-N-(p-tolyl)benzenesulfonamide (3d) were synthesized from 4-(diethylamino)ben...

The experimental (UV–vis and FT-IR) and theoretical study of 2-aminonicotinic acid (C6H6N2O2) was presented in this work. The ultraviolet absorption spectrum of title molecule that dissolved in ethanol and water were examined in the range of 200–400 nm. The FT-IR spectrum of the title molecule...

A variety of N-[(ethyl-4,6-diaryl-3-pyridinecarboxylate)-2-yl]amino acid esters 6a–h were synthesized through the reaction of 2-bromonicotinates 4 with a number of primary amino acid ester hydrochlorides 5 in refluxing tetrahydrofuran in the presence of triethylamine as dehydrohalogenating agen...

Although there are many conceivable ways to funtionalize, and specifically carboxylate, 2-chloro-4-(trifluoromethyl)pyridine optionally at all three vacant positions, it is more straightforward to prepare only the 2-chloro-4-(trifluoromethyl)pyridine-3-carboxylic acid (1) from this precursor and...

Novel supramolecular catalysts for Suzuki-Miyaura coupling were prepared and characterized by NMR, FT-IR, TEM, XRD, TGA, and XPS. The resulting picolinamide-modified β-cyclodextrin/Pd(II) complex (Pd(II)@PCA-β-CD) showed very efficient catalytic activity for Suzuki-Miyaura coupling of aryl, be...

Staphylococcus aureus and Mycobacterium tuberculosis are major causative agents responsible for serious nosocomial and community-acquired infections impacting healthcare systems globally. Over several decades, these pathogens have developed resistance to multiple antibiotics significantly affect...

A new series of 4-anilinoquinazolines with C-6 ureido and thioureido side chains and various substituents at the C-4 anilino moiety was designed, synthesized and evaluated as wild type (WT) and mutant EGFR inhibitors. Most of the compounds inhibited EGFR kinase wild type (EGFR WT) with IC50 valu...

Epidermal growth factor receptor (EGFR) signaling pathway has been previously investigated for its significant role in the progression of different types of malignant tumors, where development of small molecules targeting EGFR is well known strategy for design of antitumor agents. Herein, we rep...

An efficient and high yielding protocol is reported for the synthesis of new class of 4-anilinoquinolino-quinazoline hybrids. The target compounds were prepared first by the reaction of 2-aminobenzamide with 2-chloroquinoline-3-carbaldehydes. After oxidation and chlorination, the key 2-quinolyl-...

Both c-Met and VEGFR-2 are important targets for the treatment of cancers. In this study, a series of N-(2-phenyl-1H-benzo[d]imidazol-5-yl)quinazolin-4-amine derivatives were designed and identified as dual c-Met and VEGFR-2 inhibitors. Among these compounds bearing quinazoline and benzimidazole...

BackgroundChemokine signaling through CCR3 is a key regulatory pathway for eosinophil recruitment into tissues associated with allergic inflammation and asthma. To date, none of the CCR3 antagonists have shown efficacy in clinical trials. One reason might be their unbiased mode of inhibition tha...

The chemokine C-C receptor 3 (CCR3) plays a role in the pathogenesis of Alzheimer’s disease (AD). Based on our previous observations that deletion of CCR3 prevented neurodegenerative pathologies in amyloid precursor protein/presenilin 1 (APP/PS1) double-transgenic mice, we hypothesize that CCR3...

2-hydroxy-4-methoxybenzophenone-5-sulfonic acid with a trade name of benzophenone-4, a typical anti-UV product, is increasingly detected in real aqueous environment. Few literature using cost-effective adsorption means with enough high adsorption capacity for the removal of benzophenone-4 is ava...

The present work describes the crystal structure, third-order nonlinear optical (NLO) properties and Hirshfeld Surface (HFs) analysis of 1-(4-nitrophenyl)-3-(2, 3, 4,-trimethoxyphenyl) prop-en-1-one (2, 3,4TMNC). The synthesized material was characterised by FT-IR, FT-Raman, UV–Visible, NMR [1H...

Emergence of multi-drug resistant tuberculosis (MDR-TB) and HIV-TB co-infections potentiate the development of newer antitubercular agents to combat against tuberculosis, a dreadful disease. In the present investigation a series of pyrazoline analogues were designed and synthesized based on the ...

In the present work, the title chalcone, (2E)-3-(4-fluorophenyl)-1-(4-{[(1E)-(4-fluorophenyl) methylene]amino}phenyl)prop-2-en-1-one (abbreviated as FAMFC), was synthesized and structurally characterized by single-crystal X-ray diffraction. The compound is crystallized in the monoclinic system w...

The development of checkpoint kinase 2 (Chk2) inhibitors for the treatment of cancer has been an ongoing and attractive objective in drug discovery. In this study, twenty-one feasible pyrazole-benzimidazole conjugates were synthesized to study their effect against Chk2 activity using Checkpoint ...

Twenty eight new aryloxybenzene analogues were synthesized and their in vitro binding potencies toward S1PR2 were determined using a [32P]S1P competitive binding assay. Out of these new analogues, three compounds, 28c (IC50 = 29.9 ± 3.9 nM), 28e (IC50 = 14.6 ± 1.5 nM), and 28g (IC50 = 38.5 ± ...

Stereoselectivities in the coupling reaction between 1-O-methyl-3, 5-di-O-p-toluoyl-2-deoxyribofuranoside and suitably protected purine and pyrimidine derivatives have been examined in acetonitrile with varying equivalents of SnCl4. The best result in α-nucleoside formation was obtained when th...

The objective of this study was to assess the pharmacokinetics and bioavailability of 3β-hydroxy-17-(1H-1,2,3-triazol-1-yl)androsta-5,16-diene (VN/87-1) in normal male mice and in SCID mice bearing human LNCaP tumor xenografts. VN/87-1 is a novel potent steroidal inhibitor of human testicular 1...