117449-73-7Relevant academic research and scientific papers
New 5H-[1,3]thiazolo[3,2-a]pyrido[3,2-e]pyrimidin-5-one derivatives as diuretics
Monge,Martinez-Merino,Simon,Sanmartin
, p. 306 - 310 (2007/10/02)
A series of new 5H-[1,3]thiazolo[3,2-α]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 Quantitative structure-activity relationships show that electron withdrawn substituents in 3-position enhance both diuretic and saliuretic activities at 25 mg/kg.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 increase of diuretic and natriuretic activities when the formal charge on N(9a) and C(9b) increases. Potassium ion excretion also increases, although not as drastically as in the earlier cases. Regression equations were calculated by partial least squares method (PLS) and validated by the cross-validation (leave-one-out) technique.
NEW 5-SUBSTITUTED DERIVATIVES OF ETHYL 2,3-DIHYDRO-3-OXOISOTHIAZOLOPYRIDINE-2-ACETATE
Martinez-Merino, Victor,Gil, Maria J.,Gonzalez, Alberto,Zabalza, Jose M.,Navarro, Javier,Manu, Maria A.
, p. 333 - 344 (2007/10/02)
New series of ethyl 5-substituted 2,3-dihydro-3-oxoisothiazolopyridine-2-acetate was prepared either a) directly by reaction of 5-substituted 2-chlorothio-3-pyridinecarbonyl chlorides with ethyl glycinate or b) by oxidation of the correspondent 2-mercapto-3-pyridinecarboxamides.New 5-substituted 1,2-dihydro-2-thio-3-pyridinecarboxylic acids as starting materials are described.
Benzo- and pyrido-1,4-oxazepin-5-ones and -thiones: Synthesis and structure-activity relationships of a new series of H1 antihistamines
Cale Jr.,Gero,Walker,Lo,Welstead Jr.,Jaques,Johnson,Leonard,Nolan,Johnson
, p. 2178 - 2199 (2007/10/02)
A series of novel benzo- and pyrido-1,4-oxazepinones and -thiones which represents a new structural class of compounds possessing H1 antihistaminic acitivy was synthesized, and the SARs were evaluated. The antihistamine activity was determined by blockade of histamine-induced lethality in guinea pigs. The sedative potential was determined by comparison of the EEG profiles of the compounds with those of known sedating and nonsedating antihistamines. Several of the compounds were shown to possess potent H1 antihistaminic activity and to be free of the cortical slowing with synchronized waves and spindling activity found in the EEG of sedative antihistamines. One compound, 2-[2-(dimethylamino)ethyl]-3,4-dihydro-4-methylpyrido[3,2-f]-1,4-oxazeN pine-5(2H)-thione (rocastine) is currently undergoing clinical evaluation as a nonsedating H1 antihistamine.
Fused aromatic oxazepinones, thiazepinones, diazepinones and sulfur analogs thereof
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, (2008/06/13)
Aromatic azepinones and thiones having the formula STR1 wherein; A is benzene, naphthalene, quinoline or pyridine; B is oxygen or sulfur; E is oxygen, sulfur or STR2 n is 1, 2 or 3; Z is an amino or a heterocyclic nitrogen-containing radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; Y is halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracetylamino, trifluoromethyl, phenyl or phenyl substituted by one to three Y' radicals selected from halo, loweralkyl, loweralkoxy, diloweralkylamino, nitro, amino, loweracylamino or trifluoromethyl; and having antihistaminic utility, a process for the preparation thereof and chemical intermediates therefor are disclosed.
