In recent years CF3- and SCF3-substituted organic compounds have attracted strong interest in medicinal chemistry due to their wide spectrum of biological and pharmacological properties. These classes of fluorine-containing compounds have also found a number of applications in agricultural chemi...

The kynurenines 3-hydroxyanthranilic acid (3-HANA) and its precursor 3-hydroxykynurenine (3-HK) are metabolites derived from tryptophan degradation. 3-HK, has been related to diverse neurodegenerative diseases including Huntington's, Alzheimer's and Parkinson's diseases that share...

A new platinum(II) complex of [PtII(L) (pn)]Cl·2H2O (1) (pn = 1,3-propanediamine) with 2-(4-methoxy-phenyl)imidazo [4,5-f]-[1,10]phenanthrolin (H-L) was synthesized and characterized. In complex 1, the platinum adopts a four-coordinated square planar geometry. Complex 1 exhibited selective cyto...

This paper describes the synthesis and characterization of N5-(hetero)arylalkyl-substituted-thiazolo [5,4-d]pyrimidine-5,7-diamine derivatives (4–19) as novel human (h) A2A adenosine receptor (AR) inverse agonists. Competition binding and cyclic AMP assays indicate that the examined compounds b...

The tetradentate Schiff base ligands (L1–L4), were synthesized by reaction between 2-amino-3,5-dibromobenzaldehyde and aliphatic diamines. Then, nickel and oxovanadium(IV) complexes of these ligands were synthesized and characterized by 1H NMR, Mass, IR, UV–Vis spectroscopy and thermogravimetr...

A practical protocol to obtain 1,1′-binaphthyl-2,2′-diamine was developed from 2-naphthol and 2-naphthylhydrazine under mild conditions: solvent-free, 125–130 °C, atmospheric pressure. The convenient procedure makes the process amenable for large-scale synthesis of the versatile compound.

The reaction of aromatic 1,2-diamines with trichloromethylcarbinols under mild, basic phase-transfer conditions provided expedient access to 3,3-disubsituted quinoxalin-2(1H)-ones in good to moderate yields. The use of unsymmetrical aryl diamines gave a regioisomeric mixture of products with the...

Polycondensation of various 2-substituted-4,6-dichloro-1,3,5-triazine such as N,N-diphenylamino (DCPT), benzylamino (BnDCT) substituents with α, ω - alkylene diamines including hexamethylene (HMDA), octamethylene (OcDA), decamethylene (DcDA), and dodecamethylene diamine (DdDA) was performed, a...

2-(Trifluoroacetyl)chromones were obtained in good yields via the Claisen condensation of 2-hydroxyacetophenones with methyl 2-methoxytetrafluoropropionate, followed by sulfuric acid-mediated deprotection of the reaction products. These compounds react with ethylenediamine in the presence of ace...

A metal-free route involving a sequential reaction of 2-alknylbenzoate and aryl-1,2-diamine is described for the generation of 2-(quinoxalin-2-yl)benzoate. The sequential reaction combines NBS-mediated diketonization of 2-alknylbenzoate and condensation reaction with aryl-1,2-diamine, and procee...

The reaction of ethylenediamine with four equivalents of chlorodiphenylphosphine in the presence of a base produced tetraphosphine [(Ph2P)2NCH2CH2N(PPh2)2] (1) which on further treatment with H2O2 (30% aq.) gave tetrakis(phosphineoxide) [(Ph2P(O))2NCH2CH2N((O)PPh2)2] (2). Treatment of 1 with two...

The simple synthesis of 1,2,3,5-substituted pyrroles from α-bromoacetophenones and 2-nitroethene-1,1-diamines in the presence of K2CO3 in DMF at 120 °C is described. A range of fused and non-fused polysubstituted pyrroles were prepared in high yields with short reaction times.

The voltage gated sodium channel NaV1.8 has been postulated to play a key role in the transmission of pain signals. Core hopping from our previously reported phenylimidazole leads has allowed the identification of a novel series of benzimidazole NaV1.8 blockers. Subsequent optimization allowed t...

Pharmacological intervention with 5-lipoxygenase (5-LO) pathway leading to suppression of leukotriene (LT) biosynthesis is a clinically validated strategy for treatment of respiratory and cardiovascular diseases such as asthma and atherosclerosis. Here we describe the synthesis of a series of C(...

Tetrabenazine (TBZ) ((±)-1) and dihydrotetrabenazines (DHTBZ) are potent inhibitors of VMAT2. Herein, a practical chemical resolution of (±)-1 and stereoselective synthesis of all eight DHTBZ stereoisomers are described. The result of VMAT2 binding assay revealed that (+)-1 (Ki = 4.47 nM) was ...

A new capillary electrophoresis method for the enantioselective analysis of cis- and trans- dihydrotetrabenazine (diHTBZ) after in vitro metabolism by human liver microsomes (HLMs) was developed. The chiral electrophoretic separations were performed by using tris-phosphate buffer (pH 2.5) contai...

PurposeWe investigated the implications of early recurrent 1R rejections for long-term outcomes after heart transplantation (HT) and evaluated the prognostic significance of 1990 ISHLT grading 1B/2 versus 1A.

Proteins have various compositions of twenty specific naturally occurring amino acids. In spite of their importance in cellular metabolism, biosynthesis mechanisms, changing control conditions, and affection of effectors are not clearly understood yet. So we have made an effort to elucidate the ...

In the present work, novel thioether xylans were synthesized via a simple procedure using water as solvent. First, allyl groups were introduced on the backbone of xylan by etherification of allyl chloride in aqueous alkaline conditions at 40 °C, providing degree of substitution (DS) values up t...

A chiral β-amino acid containing three contiguous chiral centers was synthesized efficiently in 11 steps, employing enantio-enriched β-ketoester as a key intermediate, via stereoselective catalytic hydrogenation of the corresponding enamide. Stereoselective 1,4-addition of a methyl group and p...