The Heck reaction of trimethylsilylacetylene with N-t-Boc-4-iodo-L-phenylalanine methyl ester gives N-t-Boc-4-ethynyl-L-phenylalanine methyl ester (2). Coupling of 2 with different alkynes yields alkyne bridged linear amino acid esters 3– 5. Also tripodal and tetrapodal amino acid esters 10 and...
Experiments were performed to determine whether F- and CF3-substituted pyridines undergo quaternization with iodomethane (1:1 molar ratio in THF) and 1,3-diiodopropane (2:1 molar ratio in MeCN). 2-Fluoropyridine and 2-(trifluoromethyl)pyridine did not react with MeI even under prolonged reflux, ...
An I2/CuI-promoted multi-component reaction from pyridines, aryl methyl ketones and electron deficient acrylates has been accomplished in a “one-pot” manner, which provides a straightforward and efficient access to C-3 acylated indolizines. The key intermediate of N-ylides is hypothesized to b...
The ten types of nicotinic acetylcholine receptor α-subunits show substantial sequence homology, yet some types confer high affinity for α-bungarotoxin, whereas others confer negligible affinity. Combining sequence alignments with structural data reveals three residues unique to α-toxin-refra...
Two novel poly(aryl ether)s were prepared from 1,2-bis(4-(4-fluorobenzoyl)-phenoxy)-hexafluorocyclobutane and aromatic bisphenols by the aromatic nucleophilic substitution reaction in a polar aprotic solvent. These polymers have good thermal stability up to 341 °C with 10% weight loss in inert ...
Cytosolic phospholipase A2α (cPLA2α) and fatty acid amide hydrolase (FAAH) are enzymes, which have emerged as attractive targets for the development of analgesic and anti-inflammatory drugs. We recently reported that certain 3-phenoxy-substituted 1-heteroarylpropan-2-ones are inhibitors of cPL...
The reaction of NiCl2·H2O with 1-benzotriazol-1-yl-[(p-X-phenyl)hydrazone]propan-2-one, X = H (HL1), X = Cl (HL2), X = Br (HL3) and X = Me (HL4), gave the complexes [(HL)NiCl2]·nH2O and [LNi(OH)]2, where L is the monobasic anion of HL2 or HL3. The nature of the products is solvent and ligand d...
A new series of iron(III) complexes are synthesized from the reaction of the polyfunctional ligands 1-benzotriazol-1-yl-1-[p-X-phenyl]hydrazono]propan-2-one (X = H, Cl, NO2, CH3 or OCH3 corresponding to HL1,HL2, HL3, HL4 or HL5, respectively, with iron(III) chloride in the presence of LiOH by th...
A new N-ethyl quinolinium derivative of 1-Ethyl-2-(2-p-tolyl-vinyl)-quinoliniumiodide (PTQI) was synthesized by knoevenagel condensation reaction and single crystal was successfully grown by slow evaporation technique. The grown crystal exhibit a centric monoclinic space group P21/C with a third...
Increasing evidence of peptide receptor overexpression in various cancer cells, warrant the development of receptor specific radiolabeled peptides for molecular imaging and therapy in nuclear medicine. Gastrin-releasing-peptide (GRP) receptor, are overexpressed in a variety of human cancer cells...
The dysfunction of spatial cognition is a character to various neurological disorders and therapeutic strategy. However, it is limited to known risk factors clinically so far. Gastrin releasing peptide (GRP) signaling is a neuropeptide system mediating emotional memory events. However, the effec...
A variety of α-amino acid derivatives were prepared as glycine transport inhibitors and their ability to block the uptake of [14C]-glycine in COS7 cells transfected with human glycine transporter-2 (hGlyT-2) was evaluated. An array of substituents at the chiral center was studied and overall, l...
In this report, the synthesis and characterization of poly (2-hydroxyethyl methacrylate)-polyaniline-polyaniline (p-HEMA-PANi) hydrogels were investigated. The hydrogels were synthesized using: 2-Hydroxyethyl methacrylate (HEMA), N-Tris (hydroxymethyl) methyl] acrylamide, 3-Sulfopropyl methacryl...
A series of group 10 transition metal complexes based on 2-(2-hydroxyphenyl)benzoxazole (HPBO) and 2-(2-hydroxyphenyl)benzothiazole (HPBT) have been prepared. Reactions of nickel or palladium acetates with HPBT and HPBO produce chelate N–O coordinated compounds respectively. Whilst reaction of ...
Luminescent complexes [fac-Re(CO)3(Y∩X)(ph-imz)] where (Y∩XH) = H2-PBI = 2-(2′-hydroxyphenyl)-1H-benzimidazole, H-PB0 = 2-(2′-hydroxyphenyl)benzoxazole for 2, and H-PBT = 2-(2′-hydroxyphenyl)benzothiazole for 3 and ph-imz = 2-phenylimidazole) were synthesized using Re2(CO)10, H2-PBI/H-PBO/H...
N-(2-hydroxyphenyl)-2-propylpentanamide (HO-AAVPA) is a novel valproic acid derivative that has shown anti-proliferative activity against epitheloid cervix carcinoma (HeLa), rhabdomyosarcoma (A204), and several breast cancer cell lines. The aim of this research was to evaluate the pharmacokineti...
Breast cancer is the most dominating malignancy in females worldwide. Treatment with conventional chemotherapeutics is associated with severe adverse effects. Thus need of new compounds, with better therapeutic potential and lesser side effects still exist. In this context the present study is p...
In this study we present a synthesis of six-membered BF2complexes with N–B–O type linkage based on 2-(2-hydroxyphenyl)-4-phenylquinazolines and 2-(2-hydroxyphenyl)quinoxaline. The photophysical properties of compounds were studied by absorption and fluorescence spectroscopy and compared with p...
The N-(2-(trimethylsilyloxy)phenyl)acetamide 1 was synthesized via reaction of N-(2-hydroxyphenyl)acetamide with chlorotrimethylsilane. Transsilylation of new compound 1 by chloro(chloromethyl)dimethylsilane leads to 4-acetyl-2,2-dimethyl-3,4-dihydro-2H-1,4,2-benzoxazasiline 3. The structures of...
We have studied the nonlinear optical properties for synthesized materials by using the Z-scan technique, in order to measure nonlinear refractive indices. The nonlinear optical properties of synthesized N-(2-hydroxyphenyl)-2-propylpentanamide (HO-AAVPA), in micellar aqueous solution of F127, we...
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