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Biomedical subjects

S S Parmar

Publications and source records attributed to S S Parmar.

At least 91 records · Page 5Linked to original sources
PubMed1976

Synthesis of substituted thiobenzoxazoles/benzothiazoles: inhibition of cellular respiratory and monoamine oxidase activities and anticonvulsant property.

Several 2-(substituted alkoxy/hydrazinocarbonyl acetanilidothio)benzoxazoles/benzothiazoles were synthesized and characterized by their sharp melting points, elemental analyses, and IR spectra. All thiobenzoxazoles/benzothiazoles possessed low anticonvulsant activity, which was reflected by the 10-40% protection afforded by these compounds against pentylenetetrazol-induced convulsions. All thiobenzoxazoles/benzothiazoles inhibited selectively the nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, DL-isocitrate, and alpha-ketoglutarate by rat brain homogenates. NAD-independent oxidation of succinate remained unaltered. All 2-(substituted hydrazinocarbonyl acetanilidothio)benzoxazoles/benzothiazoles inhibited monoamine oxidase activity of rat brain homogenates. Greater monoamine oxidase inhibition was observed with thiobenzothiazoles than with the corresponding thiobenzoxazoles/benzothiazoles was found to be unrelated with their ability to inhibit cellular respiratory and monoamine oxidase activities of rat brain homogenates.

Animals↗
PubMed1976

Synthesis of N,N'-bis(3-substituted benzylideneaminopropyl)-piperazines and their anti-inflammatory, antiproteolytic, and anticonvulsant properties.

Some N,N'-bis(3-substituted benzylideneaminopropyl) piperazines were synthesized and characterized by their sharp melting points and elemental analyses. These substituted piperazines possessed anti-inflammatory activity, and the protection afforded by these compounds against carrageenan-induced edema ranged from 23 to 67%. The antiproteolytic activity of these piperazines was reflected by their ability to inhibit in vitro hydrolysis of bovine serum albumin and casein by trypsin. The inhibition of trypsin-induced hydrolysis was concentration dependent and competitive in nature.

Animals↗
PubMed1976

CNS depressant activity of pyrimidylthiazolidones and their selective inhibition of NAD-dependent pyruvate oxidation.

Several 1-aryl-3-(2-pyrimidyl)thiocarbamides and their corresponding cyclized 2-arylimino-3-(2-pyrimidyl)thiazolid-4-ones were synthesized and characterized by their sharp melting points and elemental analyses. These thiocarbamides and thiazolidones possessed anticonvulsant activity against pentylenetetrazol-induced convulsions and potentiated pentobarbital-induced hypnosis in mice. Most of these thiocarbamides and thiazolidones selectively inhibited nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, where the use of added NAD dether hand, remained unaltered. The anticonvulsant activity of thiocarbamides and thiazolidones was unrelated to their ability to inhibit the respiratory activity of rat brain homogenates during oxidation of sodium pyruvate. Cyclization of thiocarbamides to the corresponding thiazolidones in general enhanced their CNS depressant and enzyme inhibitory effectiveness.

Animals↗
PubMed1976

Antihemolytic and antiproteolytic properties of substituted thiosemicarbazidophenothiazines and thiazolidonylphenothiazines.

Antihemolytic and antiproteolytic properties of several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl) phenothiazines were investigated. In vitro protection of hypoosmotic hemolysis of human red blood cells by substituted thiosemicarbazidophenothiazines and substituted thiazolidonyl-phenothiazines was concentration dependent; the degree of protection ranged from 19 to 32 and 26 to 42%, respectively, at a final concentration of 0.1 mM. All phenothiazines exhibited antiproteolytic activity. The in vitro inhibition of trypsin-induced hydrolysis of bovine serum albumin by these phenothiazines was concentration dependent and competitive in nature; the degree of inhibition ranged from 30 to 50 and 32 to 79% for substituted thiosemicarbazidophenothiazines and substituted thiazolidonlyphenothiazines, respectively, at a concentration of 1mM. Cyclization of substituted thiosemicarbazidophenothiazines into the corresponding cyclized substitited thiazolidonlyphenothiazines increased the antihemolytic and antiproteolytic effectiveness of these phenothiazines.

Depression, Chemical↗
PubMed1976

Anticonvulsant activity and inhibition of cellular respiratory activity by substituted imidazolocarbamides.

Several 1-(1-aryl-2-mercaptoacetylimidazole)-3-alkylcarbamides were synthesized and characterized by their sharp melting points, elemental analyses, and IR spectra. These substituted imidazolocarbamides possessed anticonvulsant activity, which was reflected by the 20-80% protection observed with these compounds against pentylenetetrazol-induced convulsions in mice. These substituted imidazolocarbamides selectively inhibited the in vitro oxidation of nicotinamide adenine dinucleotide (NAD)-dependent oxidations of pyruvate, alpha-ketoglutarate, beta-hydroxybutyrate, and NADH by rat brain homogenates. However, NAD-independent oxidation of succinate was not affected. The anticonvulsant activity possessed by 1-(1-aryl-2-mercaptoacetylimidazole)-3-alkylcarbamides had no relationship to their ability to inhibit cellular respiratory activity.

Animals↗
PubMed1976

Anti-inflammatory and antiproteolytic properties of 1-(1-naphthylacetyl)-3-substituted carbamides.

Several 1-(1-naphthylacetyl)-3-substituted carbamides were synthesized, characterized, and evaluated for anti-inflammatory and antiproteolytic activity. The protection afforded by most of these carbamides against carrageenan-induced edema in rats at a dose of 100 mg/kg ranged from 4.4 to 50%. Some of these carbamides, which showed higher protection against carrageenan-induced edema, were further evaluated for their antigranulation effect against cotton pellet-induced granuloma formation in rats. All carbamides showed a poor degree of protection against granuloma formation. The antiproteolytic activity of these carbamides, as reflected by their ability to inhibit trypsin-induced hydrolysis of the bovine serum albumin, was of a low order and was unrelated to their anti-inflammatory activity.

Animals↗
PubMed1976

Synthesis of substituted anilino-3-methoxy-4-substituted acetoxy) benzylidenes and their monoamine oxidase inhibitory and anticonvulsant properties.

Several substituted anilino-(3-methoxy-4-substituted acetoxy) benzylidenes were synthesized and characterized by their sharp melting points and elemental analyses. All substituted benzylidenes competitively inhibited the in vitro monoamine oxidase activity of rat brain homogenates and possessed anticonvulsant activity against pentylenetetrazol-induced convulsions in mice.

Animals↗
PubMed1976

Protection of carrageenin edema and trypsin hydrolysis of bovine serum albumin by naphthylthiosemicarbazides and their cyclized oxadiazoles.

Seven 1-(naphth-1-ylacetyl)-4-substituted thiosemicarbazides were synthesized and cyclized to the corresponding 2-(naphth-1-ylmethyl)-5-arylamino-1,3,4-oxadiazoles. All compounds, with the exception of two slbstituted oxadiazoles, possessed low anti-inflammatory activity. The protection afforded by these compounds against carrageen-in-induced edema ranged from 3 to 43% where cyclization, in general, decreased anti-inflammatory activity. All compounds (1 mM), possessed antiproteolytic activity where in vitro protection of trypsin-induced hydrolysis of bovine serum albumin, in most cases was greater with oxadiazoles.

Animals↗
PubMed1976

Effects of a hyperbaric environment on respiratory and monoamine oxidase activities.

The effects of a prolonged hyperbaric environment (21 ATA He-O2, 200 +/- 30 mm Hg O2, 32.5 +/- 1 degrees C) were investigated on the respiratory activity of rat liver homogenates and the activity of monoamine oxidase in isolated rat-liver preparations. Exposure to a hyperbaric environment for 84 days caused selective in vitro inhibition of nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, D-isocitrate, and alpha-ketoglutarate by rat-liver homogenates. The addition of NAD to the reaction mixture decreased the degree of such an inhibition. No effects on the in vitro activity of liver monoamine oxidase and its inhibition by pheniprazine were observed during exposure of animals to a prolonged high-pressure environment.

Animals↗
PubMed1975

Anticonvulsant activity of N,N'-bis[3-(3-substituted urea)propyl]piperazines.

Several N,N'-bis[3-(3-substituted urea)propyl]piperazines were synthesized and characterized by their sharp melting points, elemental analyses, and IR spectra. All substituted piperazines were found to possess anticonvulsant activity, which was reflected by 20-70% protection observed against pentylenetetrazol-induced seizures in mice. Some of these compounds inhibited oxidation of pyruvic acid by rat brain homogenate. No correlation could be observed between the anticonvulsant activity possessed by these substituted piperazines and their ability to inhibit the oxidation of pyruvic acid.

Animals↗
PubMed1975

Substituted thiazolidones: selective inhibition of nicotinamide adenine dinucleotide-dependent oxidations and evaluation of their CNS activity.

Eight 2-arylimino-3-(3-N-morpholinopropyl) thiazolid-4-ones were synthesized from the corresponding 1-aryl-3-(3-N-morpholinopropyl) thiocarbamides, characterized, and tested for their effects on the cellular respiratory activity of rat brain homogenates. All substituted 4-thiazolidones selectively inhibited nicotinamide adenine dinucleotide (NAD)-dependent oxidations of pyruvate, citrate, DL-isocitrate, alpha-ketoglutarate, malate, beta-hydroxybutyrate, L-glutamate, and NADH, while the NAD-independent oxidation of succinate remained unaltered. All thiazolidones possessed some degree of anticonvulsant activity against pentylenetetrazol-induced convulsions, and the protection afforded by these compounds at a dose of 100 mg/kg ranged from 30 to 80%. The low toxicity possessed by most of these thiazolidones was reflected by their approximate LD-50 values from 300 mg/kg to greater than 1000 mg/kg. In the present study, the anticonvulsant activity possessed by these substituted 4-thiazolidones was unrelated to their ability to inhibit selectively the NAD-dependent oxidations by rat brain homogenates. These thiazolidones exhibited depression of the CNS activity which, in some cases, was associated with the increase in respiration. All thiazolidones potentiated pentobarbital (sodium) sleeping time in mice when administered in a dose of 100 mg/kg.

Animals↗
PubMed1975

Synthesis of 2-(N-arylcarboxamide)-3-substituted ethoxyindoles and their monoamine oxidase inhibitory and anticonvulsant activities.

2-(N-Arylcarboxamide)-3-substituted ethoxyindoles were synthesized by the reaction of 2-(N-arylcarboxamide)-3-hydroxyindoles, which were obtained by the cyclization of 2-carbomethoxyphenylglycine-substituted anilides. These 2-(N-arylcarboxamide)-3-substituted ethoxyindoles were evaluated for their in vitro monoamine oxidase inhibitory ability and in vivo monamine oxidase inhibitory property as evidence by reserpine reversal response. Their anticonvulsant activity also was determined against pentylenetetrazol-induced seizures. No definite correlation could be observed between chemical structure and biological activity.

Anticonvulsants↗
PubMed1975

Synthesis of 2-(4-arylthiosemicarbazidocarbonylthio)benzthiazoles and their monoamine oxidase inhibitory and anticonvulsant properties.

Ten 2-(4-arylthiosemicarbazidocarbonylthio)benzthiazoles were synthesized, characterized, and evaluated for their monoamine oxidase inhibitory and anticonvulsant activities. All substituted benzthiazoles inhibited activity of monoamine oxidase in rat brain homogenate where the degree of enzyme inhibition was higher with kynuramine as compared to tyramine and 5-hydroxytryptamine as the substrates. All substituted benzthiazoles possessed measurable anticonvulsant activity against pentylenetetrazol-induced convulsions.

Animals↗
PubMed1975

Antihemolytic and anticonvulsant activities of 1-(2,4-dichloro/2,4,5-trichlorophenoxyacetyl)-4-alkyl/arylthiosemicarbazides and their inhibition of NAD-dependent oxidations and monoamine oxidase.

Several 1-(2,4-dichloro and 2,4,5-trichlorophenoxyacetyl)-4-alkyl/arythiosemicarbazides were synthesized and characterized by their sharp melting points and elemental analyses. All substituted thiosemicarbazides protected in vitro hypoosmotic hemolysis of dog red blood cells. These thiosemicarbazides selectively inhibited nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate and alpha-ketoglutarate, while NAD-independent oxidation of succinate was not affected. These compounds inhibited the activity of monamine oxidase in rat brain homogenate, and the degree of inhibition ranged from 26.5 to 89.2 percent at a final concentration of 0.03mM, with kynuramine as the substrate. Almost all thiosemicarbazides possessed anticonvulsant activity; protection against pentylenetetrazol-induced convulsions in mice ranged from 10 to 70 percent at a dose of 100 mg/kg ip. These results provided evidence of some similarity between the membrane-stabilizing property of these substituted thiosemicarbazides with their ability to exhibit selective inhibition of NAD-dependent oxidations and inhibition of monoamine oxidase. On the other hand, the anticonvulsant activity possessed by these substituted thiosemicarbazides was unrelated to their in vitro antihemolytic and enzyme inhibitory properties.

Animals↗