Top Abstract Purchase Related
Home
>
Node
>
Subnode

1,5-Benzodiazepines. X. Dialkylamino substituted 1,5-benzodiazepine and [1,2,4]triazolo [4,3-a][1,5] benzodiazepine derivatives with inhibitory activity on PAF-induced platelet aggregation

Di Braccio, M.; Roma, G.; Grossi, G.C.; Leoncini, G.; Maresca, M.

Farmaco 47(1): 77-90

1992

ISSN/ISBN: 0014-827X
PMID: 1616579
Document Number: 394447
Novel 4-(dialkylamino) substituted (4, 5 c, 8) and 2,4-bis(dialkylamino) substituted (6) 1,5-benzodiazepine derivatives were synthesized. Both these new compounds and the substituted 4H-[1,2,4]triazolo[4,3-a][1,5]benzodiazepine-5-amines 2 a-h, recently described by us, were tested in vitro for their inhibitory activity on the PAF-induced aggregation of human platelets. Actually, bicyclic compounds 4 d, 5 c and tricyclic compounds 2 g, h showed a significant activity: in all them the dialkylamino substituent was the 4-(ethoxycarbonyl)-1-piperazinyl group. On the contrary, compounds 4 d, 5 c, 2 g,h showed practically no inhibitory activity when platelet aggregation was induced by ADP, A23187, or collagen.

Document emailed within 1 workday
Secure & encrypted payments

Di Braccio, M.; Roma, G.; Leoncini, G.; Poggi, M. 1995: Pyran derivatives XIX. (Dialkylamino) substituted 1-benzopyranones and naphthopyranones with platelet antiaggregating activity Farmaco 50(10): 703-711
Schulz, U.; Freitag, M.; Schmidt, K.; Witetschek, M.; Polzin, M.; Morgenstern, O. 2014: Synthesis and structure elucidation of 2,3,5,6,7,8-hexahydro-1 H-[1,2,4]triazolo[1,2-a]pyridazine-1-thione, 3,3-disubstituted and 2-substituted derivatives and evaluation of their inhibitory activity against inducible nitric oxide synthase Die Pharmazie 69(10): 731-744
Lipp, J.A. 1973: Effect of benzodiazepine derivatives on soman-induced seizure activity and convulsions in the monkey Archives Internationales de Pharmacodynamie et de Therapie 202(2): 244-251
Roma, G.; Ermili, A.; Balbi, A. 1977: Studies on 1,5-benzodiazepine. I. Derivatives of 4-amino-1,5-benzodiazepine Il Farmaco; Edizione Scientifica 32(2): 81-91
Sansone, M.; Castellano, C.; Pavone, F.; Hano, J. 1985: Opioid benzodiazepine tifluadom and drug-induced hyperactivity in mice: lack of benzodiazepine-like effects Polish Journal of Pharmacology and Pharmacy 37(5): 585-590
Gutkowska, B.; Wasiak, J. 1984: Synthesis of various 5,5-substituted derivatives of 3-dialkylamino-alkylohydantoin with potential pharmacological activity Acta Poloniae Pharmaceutica 41(3): 307-311
Anzini, M.; Cappelli, A.; Vomero, S.; Botta, M.; Cagnotto, A. 1990: 5-HT and benzodiazepine receptor ligands. III. Synthesis and receptor affinities of 1,2,4-triazolo[4',3':1,6]pyridazino[4,5-b]quinoline and 2,3-dihydro-9-phenyl-1H-pyrrolo[3,4-b]quinoline-1-one derivatives Farmaco 45(11): 1169-1179
Parenti, C.; Costantino, L.; Di Bella, M.; Raffa, L.; Baggio, G.G. 1988: Cardiovascular activity of 1,2,4-benzothiadiazine-1,1-dioxide derivatives. Part 10(3): Dialkylamino-, pyrrolidyl- and morpholyl-alkyl-derivatives of 3-amino-1,2,4-benzothiadiazine-1,1-dioxide, 7- or 5,7-halogen substituted Die Pharmazie 43(1): 37-39
Stefancich, G.; Artico, M.; Corelli, F.; Silvestri, R.; de Feo, G.; Mazzanti, G.; Durando, L.; Palmery, M. 1985: New psychotropic agents. I. Synthesis and pharmacologic activity of derivatives of 5H-imidazo-[2,1-c][1,4]benzodiazepine Il Farmaco; Edizione Scientifica 40(6): 429-441
Balbi, A.; Roma, G.; Mazzei, M.; Sottofattori, E.; Cadel, S.; Schiantarelli, P. 1989: Chemistry and pharmacology of pyrane derivatives. XVII. Synthesis of substituted 2-(dialkylamino)-3-formylchromones and their tricyclic derivatives Farmaco 44(6): 565-577
Fatimi, J.; Lagorce, J.F.; Chabernaud, M.L.; Buxeraud, J.; Raby, C. 1994: Synthesis and inhibitory effects of 1,4,5-trialkyl-2-thioimidazole derivatives on platelet aggregation Bollettino Chimico Farmaceutico 133(3): 151-155
Koreniuk, I.I.; Iepishkin, I.V.; Hamma, T.V.; Khusainov, D.R. 2011: Effect of 1,5-benzodiazepine derivatives on the electrical activity of neurons of the Helix albescens Rossm Fiziolohichnyi Zhurnal 57(3): 49-58
Tarzia, G.; Occelli, E.; Barone, D. 1988: Benzodiazepine receptor ligands. Synthesis and pharmacological evaluation of 6-aryl-3,8-disubstituted-1,2,4-triazolo[3,4-a]phthalazines Il Farmaco; Edizione Scientifica 43(11): 921-933
Tarzia, G.; Occelli, E.; Corsico, N.; Gallico, L.; Luzzani, F.; Barone, D. 1989: Benzodiazepine receptor ligands. Synthesis and preliminary pharmacological evaluation of 2-aminoalkyl-8-chloro- and 2-aryl-1,2,4-triazolo[3,4-a]phthalazine-3(2H)-ones Farmaco 44(1): 17-28
Andronati, S.A.; Chepelev, V.M.; Iakubovskaia, L.N.; Val'dman, A.V.; Voronina, T.A. 1983: Relationship between the structure, affinity to benzodiazepine receptors and properties of 5-halogenophenyl-1,2-dihydro-3H-1,4- benzodiazepine-2-ones Bioorganicheskaia Khimiia 9(10): 1357-1361
Squires, R.F.; Klepner, C.A.; Benson, D.I. 1980: Multiple benzodiazepine receptor complexes: some benzodiazepine recognition sites are coupled to GABA receptors and ionophores Advances in Biochemical Psychopharmacology 21: 285-293
Gallager, D.W.; Wilson, M.A. 1988: Chronic benzodiazepine agonist exposure: comparison of electrophysiological changes by brain region and benzodiazepine receptor ligand Advances in Biochemical Psychopharmacology 45: 325-336
Sieghart, W.; Drexler, G.; Mayer, A.; Schuster, A. 1983: Interaction of benzodiazepine agonists and antagonists with different benzodiazepine receptors Advances in Biochemical Psychopharmacology 38: 11-19
Krajewski, T.; Pietrucha, T.; Wachowicz, B. 1989: The inhibitory effect of UV-light on thrombin-induced pig platelet aggregation Acta Physiologica Polonica 40(4): 413-417
Shader, R.I.; Greenblatt, D.J. 1997: Can you provide a table of equivalences for benzodiazepines and other marketed benzodiazepine receptor agonists? Journal of Clinical Psychopharmacology 17(4): 331