Saponification of the bis(carbamic acid ester) 1,3-C6H4(CMe2NHCO2Me)2 (1), made by the addition of methanol to commercial 1,3-C6H4(CMe2NCO)2, yielded the meta-phenylene-based bis(tertiary carbinamine) 1,3-C6H4(CMe2NH2)2 (2). Dinuclear [{(η4-1,5-C8H12)RhCl}2{μ-1,3-C6H4(CMe2NH2)2}] (3) resulted ...

Publisher SummaryThis chapter discusses the development of compounds of a specific type to be used in the treatment of asthma and associated diseases. Contribution has also been made by other classes of drugs in this therapeutic area—namely, the bronchodilators (β2-adrenoreceptor stimulants, p...

Sodium cromoglycate is manufactured by a seven-stage synthetic process. There has been no previous documentation of toxicological effects of the intermediate compounds in its synthesis. This paper describes the health effects of acute exposure to the intermediates on the skin, eye and respirator...

Objectives: Disodium cromoglycate (DSCG) and nedocromil sodium are anti-asthma drugs that have a variety of physiological and biological effects. We examined whether DSCG affects the induction of cysteinyl leukotriene (cysLT) synthesis during dimethyl sulfoxide (DMSO)-induced granulocytic differ...

ABSTRACT:Modified disodium cromoglycate powders were prepared by co-spray drying with different concentrations of leucine, phenylalanine, tryptophan, methionine, asparagine, and arginine. Amorphous spherical particles of the same size and density where obtained which, however, exhibited differen...

The present study was designed to investigate the ameliorative effects of sodium cromoglycate and diethyldithiocarbamic acid in acute stress-induced behavioral alterations in rats subjected to restraint stress. The rats were placed in the restrainer (5.5 cm in diameter and 18 cm in length) for 3...

Novel syntheses of both the benzo[b]phenanthridine and the 6H-dibenzo[c,h]chromen-6-one motif are described. Reaction of (2-(3-bromo-1,4-dimethoxynaphthalen-2-yl)phenyl)methanamine with PIFA afforded benzo[b]phenanthridine-7,12-dione, while the related nonbrominated precursor, (2-(1,4,5-trimetho...

The reaction of equimolecular amounts of (E)-N-(2,6-dichlorobenzylidene)(naphthalen-1-yl)methanamine (1) and Pd(OAc)2 in acetic acid at 60 °C for 24 h produced a selective palladation at the 2 position of the naphthyl group of 1, which afforded the new acetato-bridged five-membered cyclopallada...

Using the available structural information of the chemokine receptor CXCR4, we present hit finding and hit exploration studies that make use of virtual fragment screening, design, synthesis and structure-activity relationship (SAR) studies. Fragment 2 was identified as virtual screening hit and ...

In this work results on vibrational properties of an organic substance that is used in popular medicine, the diterpene kaurane rel-(1S, 4aS, 7S,8aS)-7-(vinyl)-tetradecahydro-1,4a-dimethylphenanthrene-7,8a-carbolactone-1-carboxylic acid (C20H28O4), extracted from Croton argyrophylloides, is prese...

The piperidine catalyzed Knoevenagel condensation of 2′-aryl/alkyl-2-hydroxyacetophenones 7 and aryl/alkylaldehydes 8 in refluxing isopropyl alcohol with azeotropic removal of water affords, in high yield, equilibrium mixtures of E- and Z-chalcones 9 and cis- and trans-chroman-4-ones 10 which a...

To develop novel CDK2 inhibitors as anticancer agents, a series of novel pyrimidine-based benzothiazole derivatives were designed and synthesized. Initial biological evaluation demonstrated some of target compounds displayed potent antitumor activity in vitro against five cancer cell lines. Espe...

In this study, we investigate the solid-state structure and stability of AMG 222 (5-(2-[2-(2-cyano-pyrrolidin-1-yl)-2-oxo-ethylamino]-propyl)-5-(1H-tetrazol-5-yl)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene-2,8 dicarboxylic acid bisdimethylamide), a small molecule DPP-IV inhibitor. Crystal structu...

2-[10,11-Dihydro-5-ethoxy-5H-dibenzo[a,d]cyclohepten-5-yl]-N,N-dimethyl-ethanamine (1) has been found to possess anticytokine activity. The synthesis and structure-activity relationship study of a series of analogues are reported.

The tetra-chelating ligands 1,2-bis[(5H-dibenzo[a,d]cyclohepten-5-yl)phenylphosphanyl]-ethane, bis(troppPh)ethane, and 1,3-bis[(5H-dibenzo[a,d]cyclohepten-5-yl)phenylphosphanyl]-propane, bis(troppPh)propane, were synthesised. For the binding of transition metals, these ligands offer two olefin m...

A novel and convenient synthesis of 11-substituted dibenzo[a,d]cyclo-heptimines 10 via annelatlon of electrochemically generated aminium radicals derived from substituted 5-hydroxylamino-5-methyl-5H-dibenzo[a,d]cycloheptenes 14 is described. The scope and limitations of the reaction as well as t...

This paper presents a high-resolution 1H- and 13C-NMR study of 10,11-dihydro-5,10-ethano-5H-dibenzo[a,d]cycloheptene that provides a better attribution of the δ- and J-values for every atom. The structure of the hydrocarbon and the molecular conformation were established by the AM1 molecular or...

The metabolic fate of the anticonvulsant cyheptamide (AY-8682) has been investigated in animals and man. In the rat [14CONH2]cyheptamide is rapidly metabolized. Hydroxylation and conjugation are the major modes of metabolism. Cleavage of C-5 from the dibenzo-cycloheptadiene ring does not occur. ...

The dicarboxylic acid 8 was synthesized from dibenzosuberone by dehydrogenation, reduction of the keto group and dicarboxylation. After resolution with cinchonine the (-)-enantiomer served as starting material for various transformation products with trans-configuration of the substituents at th...

Inflammation plays a central role in the pathophysiology of many diseases. The inducible enzyme heme oxygenase-1 (HO-1) protects cells against inflammation and can be induced by electrophilic compounds like the chalcones (1,3-diphenylprop-2-enones) from the class of α,β-unsaturated carbonyl co...