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New 5H-[1,3]thiazolo[3,2-a]pyrido[3,2-e]pyrimidin-5-one derivatives as diuretics

Monge, A.; Martinez-Merino, V.; Simon, M.A.; Sanmartin, C.

Arzneimittel-Forschung 45(3): 306-310

1995

ISSN/ISBN: 0004-4172
PMID: 7741791
Document Number: 440175
A series of new 5H-[1,3]thiazolo[3,2-a]pyrido[3,2-e] pyrimidin-5-ones 3-substituted and/or 8,9-hydrogenated was prepared and tested for their diuretic, natriuretic and kaliuretic activities on male Wistar rats at a dosage of 25 mg/kg or less. Diuretic and saliuretic activities were strongly influenced by substituents in 3-position. Quantitative structure-activity relationships show that electron withdrawn substituents in 3-position enhance both diuretic and saliuretic activities at 25 mg/kg. Global analysis of the variations introduced on pyridine, pyrimidine and thiazole rings of this tricyclic system showed an increases of diuretic and natriuretic activities when the formal charge on N9a and C9b increases. Potassium ion excretion also increases, although not as drastically a in the earlier cases. Regression equations were calculated by partial least squares method (PLS) and validated by the cross-validation (leave-one-out) technique.

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Monge, A.; Martinez-Merino, V.; Sanmartin, C.; Ochoa, M.C.; Fernandez-Alvarez, E. 1990: New 5H-[1,3]thiazolo[3,2-a]pyrido[3,2-e]pyrimidine derivatives as diuretics Arzneimittel-Forschung 40(12): 1349-1352
Di Braccio, M.; Roma, G.; Mazzei, M.; Balbi, A.; Schiantarelli, P.; Cadel, S.; Bongrani, S. 1988: Derivatives of pyrimidine 1,2-condensate. IV. Synthesis and pharmacological properties of the N,N-disubstituted 4-amino-2H-pyrido(1,2-a)pyrimidin- 2-ones and 2-amino-4H-pyrido(1,2-a)pyrmidin-4-ones Il Farmaco; Edizione Scientifica 43(9): 705-723
Ferrarini, P.L.; Mori, C.; Armani, G.; Rossi, L. 1995: Synthesis of some 4H-pyrido[1,2-a]pyrimidin-4-ones investigated as antimicrobial agents Farmaco 50(1): 69-72
Askani, U.; Neidlein, R.; Tauber, J. 1971: Synthesis of substituted thiazolo-(3.2.-d)-tetrazolylium and thiazolo-(2.3.-b)-thiazolylium salts Die Pharmazie 26(8): 463-465
Moron, J.; Rautureau, M.; Huel, C.; Pierré, A.; Berthier, L.K.; Atassi, G.; Bisagni, E. 1993: Synthesis and evaluation of 4-amino-substituted 7-methoxy (and 7-hydroxy)- 11-methyl (and 5,11-dimethyl)-10H-pyrido [2,3-b] carbazoles and 4-amino- substituted 11-methyl (and 5,11-dimethyl)-10H-pyrido[3',4':4,5] pyrrolo [3,2-g] quinolines, two new series related to antitumor ellipticine derivatives Anti-Cancer Drug Design 8(6): 399-416
Osselaere, J.P. 1974: New 4 substituted derivatives of aryl-2 pyrido(2,3-d) pyrimidines Journal de Pharmacie de Belgique 29(2): 145-151
Wagner, G.; Leistner, S.; Vieweg, H.; Krasselt, U.; Prantz, J. 1993: Synthesis of new pyrido-(3',2':4,5)-thieno-(3,2-d)-1,2,3-triazine derivatives as antianaphylactics Die Pharmazie 48(7): 514-518
Prakash, L.; Shaihla; Malik, S.; Mital, R.L. 1989: Synthesis and antibacterial activity of some new pyrido[2,3-d]pyrimidine derivatives Die Pharmazie 44(7): 490
Sayed, H.H.; Shamroukh, A.H.; Rashad, A.E. 2006: Synthesis and biological evaluation of some pyrimidine, pyrimido[2,1-b][1,3]thiazine and thiazolo[3,2-a]pyrimidine derivatives Acta Pharmaceutica 56(2): 231-244
Passarotti, C.M.; Valenti, M.; Marini, M. 1995: In the search for new antiinflammatory drugs: synthesis and antiinflammatory activity of some Thiazolo(3,2-a)pyrimidine derivatives containing a thioether group Bollettino Chimico Farmaceutico 134(11): 639-643
Fayed, A.A.; Amr, A.E.-G.E.; Al-Omar, M.A.; Mostafa, E.E. 2014: Synthesis and antimicrobial activity of some new substituted pyrido[3',2':4,5]thieno[3,2-d]-pyrimidinone derivatives Bioorganicheskaia Khimiia 40(3): 335-340
Tylińska, B.; Jasztold-Howorko, R.; Mastalarz, H.; Szczaurska-Nowak, K.; Materek, P.; Wietrzyk, J. 2011: Synthesis of new 1-phenyl-6H-pyrido[4,3-b]carbazole derivatives with potential cytostatic activity Acta Poloniae Pharmaceutica 68(1): 31-37
Liszkiewicz, H.; Nawrocka, W.P.; Sztuba, B.; Wietrzyk, J.; Jaroszewicz, J.; Nasulewicz, A.; Pełczyńska, M. 2011: Synthesis and antiproliferative activity in vitro of new pyrido[1,4-b]diazepine derivatives and imidazo[4,5-b]pyridine Acta Poloniae Pharmaceutica 68(3): 349-355
Malinka, W.; Sieklucka-Dziuba, M.; Rajtar-Cynke, G.; Gasior, M.; Kleinrok, Z. 1995: Synthesis and pharmacological study of some derivatives of pyrazolo[4,3-c]pyrido[3,2-c]-1,2-thiazine-5,5-dioxide, a novel heterocyclic ring system Farmaco 50(1): 29-35
Boido, A.; Novelli, F.; Savelli, F.; Sparatore, F.; Russo, S.; Filippelli, W.; Susanna, V.; Marmo, E. 1989: Preparation and pharmacologic activity of amido- derivatives of 3-methyl-3,4-dihydro benzo- and pyrido-1,2,4-triazin-3-acetic acids Farmaco 44(3): 279-301
Glezer, G.A. 1992: The basic groups of modern preparations. II. Loop diuretics. Osmotic diuretics. Aquaretics. Uricosuric diuretics Terapevticheskii Arkhiv 64(6): 101-106
Delarge, J.; Lapière, C.L. 1978: A new class of high ceiling diuretics : derivatives of 1-alkyl-3-(4-phenylaminopyridin-3-yl)sulfonylurea Annales Pharmaceutiques Francaises 36(7-8): 369-379
Lumholtz, I.B. 1979: Drug information. Therapeutic main group: diuretics. 12. Potassium-preserving diuretics Sygeplejersken 79(2): 27
Kawaguchi, Y.; Ogura, Y.; Kimura, Y. 1974: Kidney failure and diuretics--effectivity of the so-called potent diuretics Nihon Jinzo Gakkai Shi 16(5): 435-440
Saruta, T.; Handa, M.; Kondo, K. 1984: Pharmacological mechanism of modern diuretics. Mechanism of hypotensive diuretics. 1). Effects on the myocardium and smooth muscles Nihon Rinsho. Japanese Journal of Clinical Medicine 42(9): 2016-2020