Top Abstract Purchase Preview Related
Home
>
Node
>
Subnode

Synthesis and pharmacological study of 5-aryl-6-methyl-4,5-dihydro-pyridazin-3 (2H) ones and related 5-aryl-6-methyl-pyridazin-3 (2H) ones

Pinna, G.A.; Curzu, M.M.; Barlocco, D.; Cignarella, G.; Cavalletti, E.; Germini, M.; Berger, K.

Il Farmaco; Edizione Scientifica 43(6): 539-549

1988

ISSN/ISBN: 0430-0920
PMID: 3208896
Document Number: 4674
New 5-aryl-6-methyl-4,5-dihydropyridazin-3(2H)ones (III) and related 5-aryl-6-methyl-pyridazin-3(2H)ones (IV) were synthesized in order to evaluate their pharmacological profile in comparison with that of the known class of antihypertensive and platelet aggregation inhibitors 5-methyl-6-aryl-4,5-dihydropyridazin 3(2H)ones (I). Though none of the tested derivatives was found to possess the antihypertensive potency of the reference compounds, some of them displayed significant antithrombotic and antiulcer properties. In particular, 5(p. acetylaminophenyl)-6-methyl-pyridazin-3-one (IV c) was found highly effective (ED50 = 1.2 mg/kg) in inhibiting indomethacin-induced ulcers.

Document emailed within 1 workday
Secure & encrypted payments

Synthesis and pharmacological study of 5-aryl-6-methyl-4,5-dihydro-pyridazin-3(2H)ones and related 5-aryl-6-methyl-pyridazin-3(2H)ones

Tarzia, G.; Occelli, E.; Corsico, N.; Luzzani, F.; Barone, D. 1988: Benzodiazepine receptor ligands. Synthesis and preliminary pharmacological evaluation of some 3-aryl-6-thioalkyl-, 3-aryl-6-alkylsulphinyl-, 3-aryl-6-alkylsulphonyl-, and 3-aryl-6-alkoxy-1,2,4-triazolo[3,4-a]phthalazines Il Farmaco; Edizione Scientifica 43(2): 189-201
Safak, C.; Simsek, R.; Altas, Y.; Boydag, S.; Erol, K. 1997: 2-methyl-3-acetyl-4-aryl-5-oxo-1,4-dihydro-5H indeno(1,2-b) pyridine derivatives studies and their calcium antagonistic activities Bollettino Chimico Farmaceutico 136(11): 665-669
Zawadowski, T.; Skowron, A.A.; Suski, S.; Rump, S.; Jakowicz, I. 1995: Synthesis and pharmacological profile of bicyclo[2.2.2]octane derivatives: N-(1-aryl-4-piperazinyl-butyl) derivatives of 7-isopropyl-6-methyl- and 1-isopropyl-4-methylbicyclo[2.2.2]oct-5-ene-2,3-dicarboxyimide Acta Poloniae Pharmaceutica 52(2): 129-132
Filacchioni, G.; Nacci, V.; Stefancich, G.; Artico, M. 1974: Synthesis of pyrrolnitrin analogs. IV. 1-aryl-2-methyl-4-p-nitrophenylpyrrole-3-carboxylic acids Il Farmaco; Edizione Scientifica 29(11): 872-882
Coudert, P.; Rubat, C.; Couquelet, J.; Tronche, P. 1990: Synthesis of 6-[(4-imidazol-1-yl)-phenyl]-4-phenyl 4,5-dihydro-2H-pyridazin-3-one: a potential blood platelet aggregation inhibitor Journal de Pharmacie de Belgique 45(3): 191-195
Dal Piaz, V.; Ciciani, G.; Giovannoni, M.P. 1997: Synthesis of 4,5-functionalized-2-methyl-6-(substituted aryl)-3 (2H)-pyridazinones: a new group of potent platelet aggregation inhibitors Farmaco 52(3): 173-178
Kossakowski, J.; Zawadowski, T.; Kuśmierczyk, J. 1998: Synthesis of new N-[4-(4-aryl- and 4-heteroaryl-1-piperazinyl)butyl]derivatives of 1-methyl-5-oxobicyclo[2.2.1]heptane-2,3-dicarboximide with an expected anxiolytic activity Acta Poloniae Pharmaceutica 55(4): 315-318
Ueda, M.; Masui, M.; Kawakami, M.; Matsunaga, K.; Gemba, T.; Ninomiya, M.; Nakano, A.; Torii, M.; Adachi, I.; Ito, H. 1993: Pharmacological studies on a new dihydrothienopyridine calcium antagonist. 4th communication: prophylactic and therapeutic effects of S-(+)-methyl-4,7-dihydro-3-isobutyl-6-methyl-4-(3-nitrophenyl)thieno[2, 3- b]pyridine-5-carboxylate in stroke-prone spontaneously hypertensive rats Arzneimittel-Forschung 43(12): 1291-1303
Bonina, F.; Guerrera, F.; Sarvà, M.C.; Siracusa, M.A.; Caruso, A.; Leone, M.G.; Amico Roxas, M. 1987: Synthesis and analgesic antiinflammatory activities of 2-aryl-ethenyl-4-aryl-thiazole-5-acetic acids Il Farmaco; Edizione Scientifica 42(12): 905-913
Nakajima, M.; Adachi, I.; Ueda, M. 1993: Pharmacological studies on a new Dihydrothienopyridine calcium antagonist. 2nd communication: effects of S-(+)-methyl-4,7-dihydro-3-isobutyl-6-methyl-4- (3-nitrophenyl)thieno[2,3-b]pyridine-5-carboxylate on the 1,4-dihydropyridine binding sites in the brain and on isolated arteries in the Cynomolgus monkey Arzneimittel-Forschung 43(12): 1276-1282
Sztanke, K.; Tkaczyński, T. 1997: Synthesis of new derivatives of 3-[4'-(2'-aminothiazolyl)]-8-aryl-7, 8-dihydro-6H-imidazo[2,1-c] [1,2,4]triazin-4-one Acta Poloniae Pharmaceutica 54(3): 223-224
Castanier, L.; Rubat, C.; Coudert, P.; Albuisson, E.; Chopineau, J.; Couquelet, J. 1995: Synthesis of new serotonergic 2-substituted 4,6-diaryl pyridazin-3-ones Arzneimittel-Forschung 45(9): 947-951
Zhai, Q-Qian.; Pang, J.; Li, G-Qing.; Li, C-Ran.; Wang, Y-Cheng.; Yu, L-Yan.; Li, J.; YOUm, X-Fu. 2017: Preclinical Pharmacokinetic Analysis of (E)-Methyl-4-Aryl-4-Oxabut-2-Enoate, a Novel Ser/Thr Protein Kinase B Inibitor, in Rats Acta Poloniae Pharmaceutica 74(1): 299-307
Harris, M.; Zacharewski, T.; Astroff, B.; Safe, S. 1989: Partial antagonism of 2,3,7,8-tetrachlorodibenzo-p-dioxin-mediated induction of aryl hydrocarbon hydroxylase by 6-methyl-1,3,8-trichlorodibenzofuran: mechanistic studies Molecular Pharmacology 35(5): 729-735
Kouri, R.E.; Ratrie, H.; Whitmire, C.E. 1973: Evidence of a genetic relationship between susceptibility to 3-methyl-cholanthrene-induced subcutaneous tumors and inducibility of aryl hydrocarbon hydroxylase Journal of the National Cancer Institute 51(1): 197-200
Zankowska-Jasińska, W.; Borowiec, H.; Golus, J.; Kolasa, A.; Zaleska, B.; Krzywosiński, L.; Bogdal, M.; Przemyk, B. 1990: Synthesis and pharmacological investigations of 3-(aminoalkylene)-1-aryl-2-thioxo-4,5-imidazolidinedione and 2,4,5-imidazolidinetrione derivatives Polish Journal of Pharmacology and Pharmacy 42(1): 49-58
Turło, J.; Zawadowski, T.; Rump, S.; Jakowicz, I.; Gidyńska, T.; Gałecka, E. 1994: Synthesis and pharmacological screening of some N,N'-bis-[4-(4-aryl-1-piperazinyl)butyl]-substituted derivatives of 1,8-dimethylbicyclo-[2.2.2]oct-7-ene-2,3,5,6-tetracarboxydiimide Polish Journal of Pharmacology 46(5): 451-455
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
Romanovich, A.I.; Chizhov, O.S.; Sviridov, A.F. 1988: Synthetic studies in the series of polyene macrolide antibiotics. 5. Synthesis of methyl-2,4,6-trideoxy-2,4-di-C-methyl-alpha-L- gluco-hexopyranoside and methyl-2,4,6-trideoxy-2,4-di-C-methyl- alpha-L-manno-hexopyranoside, the stereoisomers of the C33-C38 fragment of amphotericin B Bioorganicheskaia Khimiia 14(8): 1109-1112
Nawrocka, W.; Rutkowska, M.; Szelag, A.; Barczyńska, J.; Kedzierska-Goździk, L.; Błaszczyk, F.; Dziwiszek, W. 1996: Synthesis and pharmacological properties of new derivatives of 4-methyl-5-oxalo-1H-2,3,4,5-tetrahydro-1,5-benzodiazepin-2-one and beta-oxo-5-(4-methyl-1H-2,3,4,5-tetrahydro-1,5-benzodiazepin-2 -one)propionic acid Acta Poloniae Pharmaceutica 53(6): 425-430