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A Monge

Publications and source records attributed to A Monge.

84 records · Page 5Linked to original sources
PubMed1990

Diuretic and hypotensive activities of 4-anilino derivatives of 2-methylthiopyrido[2,3-d]pyrimidines.

The synthesis of a series of 12 compounds referring to 4-anilino-2-methylthiopyrido [2,3-d]pyrimidines (1-12), and the results of a study of their diuretic, saliuretic and antihypertensive activities are reported. Most of this compounds showed significant diuretic activity at the dosage of 3-24 mg/kg. The 4-Anilino-2-methylthiopirido[2,3-d]pyrimidine 1 remained active to a dosage of 1 mg/kg. The diuretic activity of these compounds implied an increase in the Na+ excretion. Some of the most active diuretics have been studied for antihypertensive effect.

Aniline Compounds↗
PubMed1990

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

New 5H-[1,3]thiazolo[3,2-a]pyrido[3,2-e]pyrimidines 1 and 6,10-dihydro-5H-pyrido[3',2':5,6]pyrimido[2,1-c] [1,2,4]triazines 4 with 5-one, 5-thione or 5-hydrazono substituents and in some cases 1,2,3,4 or 8,9 hydrogenated are synthetized. The diuretic, natriuretic and kaliuretic activities of these compounds in Wistar rats at a dose of 24 mg/kg were estimated. A series of 24 possible derivatives of 1 and 4 possessing diuretic and saliuretic activities are investigated for structure-activity relationships in light of Fujita-Ban model. The Fujita-Ban group contributions have been calculated for different structural variations on the parent ring 1a. It is observed that the hydrogenation of pyridine, [1,3]thiazole or [1,2,4]triazine rings on 1 or 4 decrease the diuretic and saliuretic activities.

Animals↗
PubMed1987

Selective thromboxane synthetase inhibitors and antihypertensive agents. New derivatives of 4-hydrazino-5H-pyridazino[4,5-b]indole, 4-hydrazinopyridazino[4,5-a]indole, and related compounds.

A series of new derivatives of 4-hydrazino-5H-pyridazino[4,5-b]indole (5) and 4-hydrazinopyridazino[4,5-a]indole (12) have been synthesized to investigate their activities as selective thromboxane synthetase inhibitors as well as antihypertensive agents. Several of the prepared compounds were found to be selective thromboxane synthetase inhibitors, in concordance with the Gorman model. The most potent were 8-(benzyloxy)-3,4-dihydro-4-oxo-5H-pyridazino[4,5-b]indole (3c) and 8-methoxy-4-hydrazino-5H-pyridazino[4,5-b]indole (5). This last compound did not inhibit prostacyclin formation and showed an antihypertensive activity similar to that of hydralazine. The acute toxicity in mice for 5a . HCl is about 2.2 times less than that for hydralazine.

Animals↗
PubMed1986

Effects of 2-indolecarbohydrazides on thromboxane synthetase activity and on in vitro and ex vivo blood platelet aggregation. New selective inhibitors.

Platelet antiaggregatory action of 42 synthetic 2-indolecarbohydrazides was studied observing their actions on arachidonic acid (AA) and adenosine-5-diphosphate (ADP) induced platelet aggregation. Radioimmunoassay studies, following AA induced aggregation, measuring thromboxane B2 (TXB2) and prostaglandin E2 (PGE2) were carried out on those compounds whose previous activities included inhibition of AA induced platelet aggregation and inhibition of the second wave of aggregation using ADP as the aggregating agent. Those compounds which demonstrated inhibition of TXB2 with increased PGE2 were subsequently tested with PGH2 as the aggregating agent. Results of this work demonstrate that 3 of the 42 compounds have specific inhibitory activity for thromboxane synthetase. The most active compounds were 1-methyl-5-hydroxyindole derivatives.

Arachidonic Acid↗
PubMed1981

Selectivity of an indole-hydrazide derivative as inhibitor of mouse brain type A monoamine oxidase.

The first indole-hydrazide, 1-[2,-(3-methyl)-5-benzyloxyindolyl]carbonyl-2-isopropyl hydrazide (IH-3), that irreversibly inhibits mouse brain type A monoamine oxidase is measured by 5-hydroxytryptamine deamination. The concentration required in vitro to inhibit this isoenzyme is about 7 X 10(-8) mol/l. Other biochemical and pharmacological features of this potential antidepressant are presented.

Animals↗
PubMed1977

Synergistic activity of gentamicin plus carbenicillin upon Pseudomonas aeruginosa: its relationship with pyocin and antibiotic susceptibility.

The synergistic effect of combinations of gentamicin and carbenicillin, as well as the type or subtype of the pyocins produced, were investigated in 170 strains of Pseudomonas aeruginosa isolated from clinical specimens. A high proportion of strains were synergistically inhibited (73.5%), but among strains producing pyocins 7, 14 and 31, synergy was infrequent or absent. The synergistic effect was more frequent upon gentamicin- or carbenicillin-susceptible strains. However, among untypable strains, synergy was more frequent among gentamicin-resistant strains. Susceptibility to both gentamicin and carbenicillin must be considered if antibiotic susceptibility is to be related to synergy.

Bacteriocins↗
PubMedDate not supplied

Synthesis and antituberculosis activity of some new 2-quinoxalinecarbonitriles.

Tuberculosis, an ancient disease undergoing recent control by public hygiene and drug therapy, has experienced a recrudescence throughout the world. New and effective therapies are rapidly needed to combat infections caused by these strains. Some new 2-quinoxalinecarbonitriles have been synthesized and tested as antituberculosis agents and interesting results have been obtained from the first screening.

Antitubercular Agents↗
PubMedDate not supplied

Interleukin-10 pharmacokinetics in intact and nephrectomized mice.

The influence of kidney function on interleukin-10 (IL-10) pharmacokinetics was assessed by comparing the disappearance of IL-10 from the circulation in the intact and acutely nephrectomized mice over 1 h following a single bolus injection of E. coli-derived recombinant h IL-10 at 250 micrograms/kg i.v. The intact mice demonstrated a C(max) of 1,172 ng/ml and an AUC(tf) of 385 n g.h/ml. By comparison, there was a 4-fold elevation in C(max) and a 7-fold increase in AUC(tf) in the anephric mice. The serum IL-10 concentration at 1 h post-injection was 87 ng/ml in the intact vs 1,684 ng/ml in the anephric mice. The results imply that IL-10, in common with other cytokines, is eliminated through the kidney.

Animals↗
PubMedDate not supplied

Melperone in the treatment of iatrogenic psychosis in Parkinson's disease.

The pharmacological management of Parkinson's disease (PD) can be complicated by psychiatric disorders induced by antiparkinsonian drugs. The reduction or withdrawal of levodopa (l-dopa) and other drugs commonly used in the treatment of PD may attenuate the psychosis but exacerbate motor impairment and disability. Melperone is an atypical antipsychotic drug showing in vivo a greater relative affinity for the 5-HT2 than the D2 receptors. A two-year study to assess the clinical efficacy and the safety of melperone in the management of iatrogenic psychosis in 30 parkinsonian patients was carried out. Neurological evaluation was performed with patients in the "off" and in the "on" state using the motor examination of the Unified Parkinson's Disease Rating Scale (UPDRS). Time spent in "on" state was evaluated using the self-evaluation diary of daily life. To assess psychiatric disturbances the modified version of the Brief Psychiatric Rating Scale (BPRS) was used. The mean BPRS score was significantly reduced when comparing baseline with individual examinations; no statistically significant differences were found between subsequent examinations. UPDRS motor score and time spent in "on" state during daily life showed no statistically significant differences when comparing baseline with subsequent examinations. Two patients dropped out because of excessive sedation problems but in the remaining 28 patients melperone proved to be optimally tolerated.

Aged↗