We studied the in vitro metabolism of 3-methylindole (3MI) in hepatic microsomes from fish. Hepatic microsomes from juvenile and adult carp (Cyprinus carpio) and rainbow trout (Oncorhynchus mykiss) were included in the study. Incubation of 3MI with hepatic microsomes revealed the time-dependent ...

Twenty-one types of novel ellipticine derivatives and pyridocarbazoles (5-methoxycarbonyl-11-methyl-6H-pyrido[4,3-b]carbazoles) with a nitrosourea moiety, linked by an oxydiethylene unit at the 2 position, were synthesized, and their cytotoxicity against HeLa S-3 cells was evaluated. Some of the...

To further investigate the structure–activity relationship (SAR) of the 5-hydroxytryptamine type 6 (5-HT6) receptor agonist 5-chloro-2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole (EMD386088, 6), a series of 2-methyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indoles were synthesized, and in ...

PKCθ is a serine/threonine kinase involved in the regulation of IL2 production in T cells. It has recently become an attractive therapeutic target for a variety of immunological disorders. We describe the optimization of the enzymatic and cellular potency of a series of 5-vinyl-3-pyridinecarbon...

The present report describes the synthesis and antiproliferative evaluation of certain 11-aminoalkylamino-substituted 5H- and 6H-indolo[2,3-b]quinolines and their methylated derivatives. These 5-Me- and 6-Me-indolo[2,3-b]quinoline derivatives 10–14, 20 were prepared by amination at the C-11 pos...

Many known 5-HT7 ligands contain either a serotonin-like or an arylpiperazine structure that, in published SAR studies, are generally supposed to bind the same receptor pocket. Conversely, we explored the hypothesis that two such moieties can co-exist in the same ligand, binding to different poc...

This study assessed the possible antinociceptive role of peripheral 5-HT1 receptor subtypes in the rat formalin test. Rats were injected into the dorsum of the hind paw with 50 μl of diluted formalin (1%). Nociceptive behavior was quantified as the number of flinches of the injected paw. Reduct...

All clinically-used antipsychotics display similar affinity for both D2 (D2R) and D3 (D3R) receptors, and they likewise act as 5-HT2A receptor antagonists. They provide therapeutic benefit for positive symptoms, but no marked or consistent improvement in neurocognitive, social cognitive or negat...

Methyl and ethyl 3-dimethylamino-2-(indol-3-yl)propenoate were prepared from alkyl 3-indoleacetates and tert-butoxy-bis(dimethylamino)methane. Upon treatment of these two N,N-dimethylenaminones with α-heteroarylamines as N,N-1,3-dinucleophiles, condensed indolylpyrimidones as meridianine analog...

Inosine 5′-monophosphate dehydrogenase (IMPDH, EC 1.1.1.205) catalyzes a crucial step in guanine nucleotide biosynthesis, thereby governing cell proliferation. In contrast to mammalian IMPDHs, microbial IMPDHs are relatively less explored as potential targets for antimicrobial drug discovery. I...

Trans-[Mo2(μ-O2CCH3)2Cl2(μ-dppma)2] (2) can be synthesized from Mo2(μ-O2CCH3)4 (1), trimethylchlorosilane and bis(diphenylphosphino)methylamine (dppma) (3) at room temperature. In contrast to the related compounds containing dppa (bis(diphenylphosphino)amine) this molecule displays significan...

The design and synthesis of a few simple N-benzyl derivatives of isobornyl amine is presented. The derivatives have been assessed as chiral solvating agents for effective discrimination of the signals of some acids in NMR analysis. The single crystal X-ray analysis of the salts of (R)-mandelic a...

This review covers compounds formed by Mannich-like reactions of coordinated amine-compounds with an α-methylene nitro-compound (usually nitroethane) and an aldehyde (predominantly formaldehyde) to form a compound with two primary amine functions joined by a –NH–(CH2)–C(NO2)(CH3)–(CH2)–NH–...

Stereochemically defined enantioenriched molecules were, are and will always be playing a pivotal role in the development of novel pharmaceutical agents. On this line, compounds having tertiary benzylic stereocenter are of special note. This has led to an increase in the development of novel syn...

Demethylation of N-methyl group in N-methyl-N-arylmethyl-α-amino esters was accomplished by the oxidation of the amino group using the N-iodosuccinimide (NIS)/acetonitrile system followed by treatment with O-methylhydroxylamine hydrochloride. This combination of reagents could provide a complem...

Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that plays an important role in decreasing high-density lipoprotein cholesterol (HDL-C) levels and increasing low-density lipoprotein cholesterol (LDL-C) levels. Inhibition of CETP may be a new therapy for treating atherosclerosi...

1-(2-Thienyl)-2-arylazo-4,4,4-trifluorobutane-1,3-diones 4, obtained by the condensation of aryldiazonium salts 2 with 1-(2-thienyl)-4,4,4-trifluoromethyl-1,3-butanedione 3, on treatment with hydroxylamine hydrochloride yielded 3-(2-thienyl)-4-arylazo-5-hydroxy-5-trifluoromethyl-Δ2-isoxazolines...

A new cycloruthenated 2-(2-thienyl)pyridine complex (1) with a benzo[e]indolium block was successfully synthesized and characterized, which has good water-solubility and displays a maximum absorption band centered at 730 nm (ε = 6.3 × 103 M−1 cm−1) in water. Moreover, its absorption edge can e...

The title compound 5-(5‑bromo‑2-thienyl)-1-(phenyl)-3-phenyl-2-pyrazoline has been synthesized and the structure was characterized using 1H NMR, 13C NMR, IR techniques and finally the structure was confirmed by X-ray diffraction studies. The IR spectrum of 5-(5‑bromo‑2-thienyl)-1-(phenyl)-3-phen...

The reactions of bis-(bromomagnesiummethyl)carboranes with dimethyldimethoxysilane were studied. It has been shown that interaction of 1,2-bis-(bromomagnesium)-o-carborane with an excess of dimethyldimethoxysilane gives the mixture of 1,2-(methoxydimethylsilylmethyl)-o-carborane and exocyclic 1,...