Showing papers in "European Journal of Medicinal Chemistry in 1987"

TL;DR: AzasQualenes, bis-azasqualenes and derivatives, designed as inhibitors of squalene 2,3-epoxide cyclase, a key enzyme in sterol biosynthesis, were synthesized and their in vitro activities against a variety of yeasts, fungi, gram-positive and gram-negative bacteria were determined.

TL;DR: The synthesis of dimethylaminoacetohydrazones of 5-formylimidazo[2,1-b]thiazoles and thiazolines was reported in this paper.

TL;DR: In this paper, Halogenated 3(2H)-isoflavenes and (±)isoflavans were synthesized in order to study their in vitro activity against rhinovirus 1B by comparison with the known anti-viral compound, 4′, 6-dichloroflavan.

TL;DR: The authors decrivent la synthese d'une serie d'acides dihydro-4,7 ethyl-7 oxo-4 thieno(2,3b)pyridine carboxyliques-5 originaux differemment substitues in position 2.

TL;DR: In this article, twelve mixed-ligand complexes of Fe(III), Ni(II), Cu(II) and Zn(II)-with Schiff bases of N,N -diethylamino-dithiocarbamate and thiocyanate as ligands, have been synthesized and characterized on the basis of elemental analysis, infrared and electronic spectral studies, as well as magnetic measurements.

TL;DR: In this paper, the authors compare three types of nematodes: imidazo[2,1-b]thiazole, dihydro-2,3 imidazole, thiazole and benzothiazole.

TL;DR: In this paper, the synthese et les resultats de l'etude des proprietes serotoninergiques et/ou anti-dopaminergiques d'une serie of (tetrahydro-1,2,3,6 pyridinyl-4)-3 1H-indoles substitues ou non sur le noyau indolique sont presentes.

TL;DR: A series of substituted sulfinyl benzimidazoles were prepared and tested for gastric anti-secretory activity as discussed by the authors, and two compounds were tested for anti-ulcer activity.

TL;DR: Several p-substituted diethyl benzylphosphonates related to the calcium antagonist Diethyl 4-(2-benzothiazolyl)benzylphophosphonate (fostedil) have been studied as discussed by the authors.

TL;DR: The main mecanisme d'action des anti-inflammatoires non steroidiens (AINS) actuellement utilises en therapeutique is the inhibition de la synthese des prostaglandines.

TL;DR: In this paper, auteurs etudient les voies d'acces a des (dihydro-1,4 pyridinylidene-4)-2 indanediones 1,3 diverse substituees sur le noyau benzenique and sur l'heterocycle, ainsi que leurs proprietes anti-inflammatoires realizee sur le compose de base par introduction sur lazote d'enchainements a fonctions oxygenee ou soufree s'est revelee peu fruct

TL;DR: In this article, Δ 1-pyrrolines with activated malonates were used to synthesize 7.7-hydroxy-2,3-dihydro-1H-indolizin-5-ones with various substituents and pyranno annelated derivatives.

TL;DR: In this article, a reduction of 1-methyl-and 1-benzyl-diethyl pyrazole with diisobutylaluminium hydride in toluene gave 3,5-bis-(hydroxymethyl)pyrazoles 4a and 4b in very good yields.

TL;DR: Ketonucleosides 1, 2, 3 and 5 inhibited DNA synthesis in leukemic REH 6 cells more markedly than RNA and protein syntheses and the degree of this activity was independent of the anomeric configuration, axial or equatorial position of the bases and the l or d configuration of the sugar.

TL;DR: Several classes of pyrido analogues of 10H-pyrido[3,4-b][1,4]-benzothiazine were synthesized and all exhibited significant analgesic activity relative to acetylsalicylic acid and dextropropoxypypoxyphene as mentioned in this paper.

TL;DR: In this paper, the dinitro-2,7 benzo[1,2-b:4,3-b′]-difuranne is obtenu par nitration directe du naphto-2 benzofuranne lui-meme et que les nitro-1 naphtoofurannes sont generalement plus actifs contre les bacteries.

TL;DR: In this article, a serie de triazine-1,2,3 ones-4 a ete synthetisee et etudiee pour son activite antidepressive potentielle comparativement a la trazodone 2.

TL;DR: In this paper, the substitution pattern at positions 1 and 2 of the heterocyclic rings and by introducing an ethylene chain between nitrogen atoms were modified to achieve anti-inflammatory properties.

TL;DR: In this paper, a serie formee d'acides biphenyl-4, methylene-2 ou 3, oxo-4 butyriques substitues, de leurs isomeres et des acides selectivement reduits sur le carbonyle and la double liaison a ete synthetisee.

TL;DR: In this article, eight derivatives of 8-aminoalkyl substituted xanthine have been synthesized and all have demonstrated a potent anti-bronchoconstrictive effect in the guinea pig and some of them have a very long duration of action (> 48 h.

TL;DR: In this paper, a comparison of trente-deux molecules was made between the sites of fixation of the [ 3 H]PCP (phencyclidine tritiee) and TPCP ((thieny1-2)-1 cyclohexylpiperidine tritee) in terms of structure or conformation.

TL;DR: In this article, 4-methoxy-and 4-hydroxy-3-nitrocoumarins were synthesized from 4.4-Amino-1,2-dihydro-5-(2-hydroxyphenyl)-3H-pyrazol-3.1.

TL;DR: In this paper, the authors developpe une analyse globale des correlations entre structure chimique and type d'activite anti-parasitaires, au moyen d'une analyse factorielle des correspondances realisee sur ordinateur.

TL;DR: As a part of a research project on anti- microbial agents, a series of 5-arylazo-3-benzyl-4-thioxothiazolidin-2-ones 4 and some of their 4-oxo 5, 4-hydroximino 6 and 4-phenylhydrazono 7 derivatives were prepared and evaluated as potential anti-microbial agents.

TL;DR: A high yielding unambiguous synthesis of (±)-6-alkyl-5,6,7,8-tetrahydropterin 5a–f hydrochlorides starting from ethyl α-isocyanoacetate 1 and the respective alkanoic anhydrides or alkanoyl chlorides in four steps is described.

TL;DR: The electronic structure of 1-(2,5-dimethoxy-4-nitrophenyl)-2-aminopropane (DON) was calculated at the CND0/2 level, and the racemic compound was synthesized and found to be hallucinogenic at doses of 4 mg as discussed by the authors.

TL;DR: The SAR for H1-antagonistic activity of this series of compounds on the ileum was found to be analogous to that on the trachea, and a significant difference was found between the H2-SAR on the right atrium and gastric fundus.