Effect of methiothepin on imipramine- or mianserin-induced subsensitivity of serotonergic receptors was examined in rat brain. Treatment with either imipramine plus methiothepin or mianserin plus methiothepin for 4 days resulted in a significant decrease in [3H] 5-hydroxytryptamine ([3H] 5-HT) b...
In scopolamine-treated (5.0 mg/kg, s.c.) rats hippocampal rhythmical slow activity (RSA) and neocortical low voltage fast activity (LVFA) occur only in close correlation with head movements, spontaneous changes in posture, or locomotion (Type I behavior). Previous work indicates that such scopol...
Methiothepin, a nonselective 5-HT receptor antagonist was utilized to explore the 5-HT modulation of dorsal vagal complex–TRH (thyrotropin releasing hormone) analogue stimulated gastric functional parameters. Intracisternal methiothepin pretreatment (200, 0.1 nmol) produced significant inhibiti...
The enantiomers of the 5-HT autoreceptor antagonist methiothepin have been prepared and their activity as antagonists of the 5-HT autoreceptor and at the 5-HT recognition sites present in the frontal cortex of the rat have been evaluated. At the 5-HT autoreceptor, the order of potency as antagon...
The presence of non-steroidal anti-inflammatory drugs (NSAIDs) in the environment is an emerging concern owing to their potential threat on aquatic ecosystems and living organisms. To investigate the bioremoval potential of a biological activated carbon (BAC) filter for the removal of NSAIDs, re...
Condensation of 6-nitroindoline with 5-O-trityl-L-arabinose, -D-fucose, -D-arabinose, or -L-rhamnose gave the corresponding 1-glycosyl-6-nitroindolines, from which, after acetylation, dehydrogenation, and removal of protecting groups, 1-α-and -β-L-arabinofuranosyl, 1-β-D-fucopyranosyl, 1-α-D...
A diterpene hydroxy acid, representing a new class of tricyclic diterpenes, has been isolated from Eremophila georgii Diels (Myoporaceae). Chemical and X-ray crystallographic evidence shows it to be an isoprenologue of 2-epi- (-)-a-cedrene.
In the present study, we have reported synthesis and biological evaluation of a series of fifteen 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole derivatives against both promastigotes and amastigotes of Leishmania parasites responsible for visceral (L. donovani) and cutaneous (L. amazonensis) leishman...
This study mainly focused on the modification of the X2 position in febuxostat analogs. A series of 1-phenyl-1H-1,2,3-triazole-4-carboxylic acid derivatives (1a-s) with an N atom occupying the X2 position was designed and synthesized. Evaluation of their inhibitory potency in vitro on xanthine o...
Twenty novel 2-thioxo-1, 3-thiazolidin-4-one derivatives (5a-5t) were synthesized and evaluated for their antitubercular activity. The structure of the compounds was confirmed by IR, NMR and Mass Spectroscopy methods. In addition, single-crystal X-ray diffraction was performed for compound 5a. A...
A series of beta-carbolines with other heterocycles linked by phenyl ring has been designed and synthesized. The key intermediates 3 and 5 were synthesized by condensing tryptamine and teraldehyde via Pictet- Spengler method. All the newly synthesized compounds were tested for their anticancer a...
Sagittaria trifolia L. is one of the most serious weeds in paddy fields in northeast of China and cannot be controlled effectively by bensulfuron-methyl in recent years. In this study, two suspected resistant S. trifolia populations (R1 and R2) were collected in Liaoning province of China. Whole...
In the search for new chemotherapeutic agents useful against Rubella virus (RV) infections, a solution-phase parallel approach for the synthesis of a small library of 4-alkylamino-6-(2-hydroxyethyl)-2-methylthiopyrimidines has been set up, based on previous results from our research group. Biolo...
The three-component reaction of 1-substituted imidazoles, cyanophenylacetylene, and elemental sulfur or selenium proceeds readily (for sulfur at room temperature without solvent, and for selenium in boiling MeCN) to stereoselectively afford 3-(Z)-cyanophenylethenyl-2-imidazolethiones or -selones...
A set of ferrocenyl-substituted thiazoles 2 and 3 were designed and synthesized by Pd-catalyzed Sonogashira cross-coupling reaction. Their [2+2] cycloaddition–reteroelectrocyclization reaction with tetracyanoethene resulted in strong intramolecular charge transfer (ICT) chromophores 4 and 5. Th...
Zeolite H-beta facilitated the reaction of α-chloro acetyl chloride with 1,2-bis-trimethyl silyl acetylene to give 1-chloro-4-(trimethylsilyl)but-3-yn-2-one which on treatment with thioacetamide afforded 2-methyl-4-[(trimethylsilyl)ethynyl]thiazole. l-Proline on the other hand facilitated the c...
1-(7-methoxy-2-methyl-1,2,3,4-tetrahydro-isoquinolin-4-YL)-cyclohexanol is a novel putative trace amine receptor modulator hypothesized to be useful for treatment–resistant depression. In our previous study, we have demonstrated the antidepressant-like effect of this molecule in mouse forced sw...
The β-phenylethylamines are known to act as ligands for the trace amine receptors, a novel family of G-protein-coupled receptors. The trace amines are stored and released along with various neurotransmitter agents such as norepinephrine, serotonin, and dopamine and thus work as neuromodulator o...
TGR5, a GPCR, is involved in energy and glucose homeostasis, and as such, is a target for the treatment of diabetes, obesity and other metabolic syndromes. A new class of TGR5 agonists based on a 4-phenyl pyridine scaffold was designed, synthesized and evaluated in vitro and in vivo. Extensive s...
The homocamptothecin (hCPT) represents a new class of topoisomerase inhibitor which combines enhanced plasma stability and strong antitumor activity. Fluorine imparts desirable characteristics to drugs by modulating both the pharmacokinetics and pharmacodynamic properties of a drug. Therefore, i...
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