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• 2131-55-7 4-Chlorophenyl isothiocyanate 
• 20261-59-0 monoethanolammonium hydrogensulfate 
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Relevant academic research and scientific papers

Synthesis and biological activity of novel symmetrical bis-2- phenyliminothiazolidine derivatives

A series of novel symmetrical bis-2-phenyliminothiazolidine derivatives were designed and synthesized. The structures of all the title compounds were characterized by 1H NMR and, in some cases, by 13C NMR, IR, and high-resolution mas

Three-dimensional quantitative structure-activity studies of octopaminergic agonists responsible for the inhibition of sex-pheromone production in Hercoverpa armigera

The quantitative structure-activity relationship (QSAR) of octopaminergic agonists responsible for the inhibition of sex-pheromone production in Hercoverpa armigera, was analyzed using physicochemical parameters, molecular shape analysis (MSA), molecular field analysis (MFA), and receptor surface model (RSM), respectively. The dose-response studies were performed in vitro analyzing the effect of these compounds on intracellular cAMP production in the presence of pheromone biosynthesis activating neuropeptide (PBAN) at 1 pmol/intersegment. Six active derivatives were identified in the order of decreasing pheromonostatic activity: 2-(2,6- dimethylanilino)imidazolide (6) > 2-(2-methyl-4-chloroanilino)oxazolidine (1) > clonidine (5) > 2-(2,6-diethylanilino)thiazolidine (8) > 2-(3,5- dichlorobenzylamino)-2-oxazoline (4) > tolazoline (10) which were all active in the nanomolar range in inhibition of cAMP production by 1 pmol PBAN/intersegment. Four other compounds were less active having K(i) in the micromolar range. An MSA was tried to obtain QSAR equation that incorporates spatial molecular similarity data of those compounds. MFA on the training set of those compounds evaluated effectively the energy between a probe and a molecular model at a series of points defined by a rectangular or spherical grid. An RSM was generated using some subset of the most active structures. Three-dimensional energetics descriptors were calculated from RSM/ligand interaction and these three-dimensional descriptors were used in QSAR analysis. These results indicate that these derivatives could provide useful information in the characterization and differentiation of octopaminergic receptor types and subtypes. (C) 1999 Elsevier Science Ltd.

Synthesis and Octopaminergic-agonist Activity of 2-(Arylamino)thiazolidines, 2-(Aralkylamino)-2-thiazolines, and Related Compounds

2-(Arylimino)thiazolidines (AITs) were synthesized by cyclizing monoethanolamine hydrogen sulfate with arylisothyocyanates in the presence of sodium hydroxide, or by the hydrochloric acid-catalyzed cyclization of thiourea. 2-(Aralkylamino)-2-thiazolines (AATs) and thiazines were obtained by the hydrochloric acid-catalyzed cyclization of the corresponding thioureas. 2-(2,6-Diethylphenylimino)oxazolidine was obtained by cyclodesulfurizing the corresponding thiourea with yellow mercuric oxide.The activity for stimulating adenylate cyclase prepared from ventral nerve cords of the American cockroach Periplaneta americana L. by these compounds was examined at 100 μM.AIT with a 2,6-diethylphenyl group was more active than its oxazolidine derivative.Greater enzyme activation appeared to result from short-chain alkyl rather than halogen substitution at the 2,6-positions of the aromatic ring of AITs.Increasing the chain length from methyl to ethyl in 2,6-disubstituted AIT caused an increase in the enzyme activation.There was a marked decrease in the enzyme activation after alkylating the ring nitrogen or C5, and after ring expansion of potent AIT and AAT.Thus, a certain degree of bulkiness and hydrophobicity at the 2- and 6-positions on the phenyl ring of AIT and at the N-terminal of AIT and AAT were favorable for activating the adenylate cyclase.

Aminothiazines et aminothiazoles analogues ouverts du levamisole: synthese et approche du mode d'action nematicide

New compounds with thiazoline or dihydrothiazine rings substituted by alkylamino or arylamino groups were synthesized and screened in vitro against three Nematodes.Inhibition of fumarate-reductase activity was also evaluated.For all in vitro anti-parasitic tests, dihydrothiazines were more potent than corresponding thiazolines derivatives, however, thiazolines showed a greater inhibition of fumarate-reductase.