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Biomedical subjects

S S Parmar

Publications and source records attributed to S S Parmar.

At least 73 records · Page 4Linked to original sources
PubMed1978

Anticonvulsant and antiproteolytic properties of 3,5-disubstituted oxadiazole-2-thiones and their inhibition of respiration in rat brain homogenates.

Eight 5-(3,4-methylenedioxyphenyl)-3-arylaminomethyl-1,3,4-oxadiazole-2-thiones were synthesized, characterized by their sharp melting points, elemental analyses, and IR spectra, and evaluated for anticonvulsant activity. All substituted oxadiazole-2-thiones possessed anticonvulsant activity, which was reflected by their ability to provide 10--70% protection against pentylenetetrazol-induced convulsions in mice at 100 mg/kg ip. These compounds inhibited in vitro nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, alpha-ketoglutarate, and NADH by rat brain homogenates as well as NAD-independent oxidation of succinate by rat brain homogenates. Antiproteolytic activity of these substituted oxadiazole-2-thiones was reflected by their ability to inhibit trypsin hydrolysis of bovine serum albumin. These results indicated that the inhibition of cellular respiration and antiproteolytic activity of these substituted oxadiazole-2-thiones is not the biochemical basis for their anticonvulsant activity.

Animals↗
PubMed1978

Anticonvulsant activity and inhibition of respiration in rat brain homogenates by substituted trimethoxybenzamides.

Ten N-[4-[4-(arylthiosemicarbazido)carbonyl]phenyl]-3,4,5-trimethoxybenzamides were synthesized and characterized by their sharp melting points, elemental analyses, and IR and NMR spectra. All substituted benzamides were evaluated for their anticonvulsant activity. The degree of protection afforded by these compounds (100 mg/kg ip) against pentylenetetrazol (90 mg/kg sc)-induced convulsions in mice ranged from 10 to 80%. The ability of substituted benzamides to inhibit respiratory activity was observed by inhibition of oxidation of pyruvate, alpha-ketoglutarate, NADH, and succinate by rat brain homogenates. Inhibition of pyruvic acid oxidation was concentration dependent. The anticonvulsant activity of substituted benzamides was not related to their ability to inhibit cellular respiratory activity.

Animals↗
PubMed1978

Anticonvulsant activity and selective inhibition of NAD-dependent oxidations by 1,2,4-trisubstituted-5-imidazolones.

Nine 1-(3,4-dimethoxyphenylethyl)-2-methyl-4-(substituted benzylidene)-5-imidazolones were synthesized, characterized by their sharp melting points, elemental analyses and infrared spectra and evaluated for anticonvulsant activity. All 1,2,4-trisubstituted-5-imidazolones at a dose of 100 mg/kg i.p. possessed anticonvulsant activity and the degree of protection observed against pentylenetetrazol-induced convulsions in mice ranged from 20 to 60%. These 1,2,4-trisubstituted-5-imidazolones selectively inhibited in vitro oxidation of the nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, alpha-ketoglutarate and NADH by rat brain homogenates while the NAD-independent oxidation of succinate remained unaltered. The anti-convulsant activity possessed by 1,2,4-trisubstituted-5-imidazolones was unrelated with their ability to selectively inhibit respiratory activity of rat brain homogenates.

Animals↗
PubMed1978

Anti-inflammatory and antiproteolytic properties of 2-[acyl-N-(substituted benzylidene)hydrazino]5-phenyltetrazoles.

Ten 2-[acyl-N-(substituted benzylidene)hydrazino]5-phenyltetrazoles were synthesized, characterized and evaluated for anti-inflammatory and antiproteolytic activity. The protection afforded by these tetrazoles at a dose of 100 mg/kg i.p., against carrageenin-induced edema in rats, ranged from 11 to 46%. Oxyphenbutazone (40 mg/kg i.p.), and hydrocortisone (10 mg/kg i.p.), used as reference drugs, exhibited protection of 54 and 47%, respectively. The antiproteolytic activity of these tetrazoles, as reflected by their ability to inhibit trypsin-induced hydrolysis of bovine serum albumin, ranged from 17 to 57%. The antiproteolytic activity was found to be unrelated to the anti-inflammatory activity possessed by these tetrazoles.

Animals↗
PubMed1978

Antihemolytic, antiproteolytic and anticonvulsant properties of 10-substituted hydrazonoacetyl phenothiazines.

Twelve 10-substituted hydrazonoacetyl phenothiazines were synthesized, characterized and evaluated for their antihemolytic, antiproteolytic and anticonvulsant properties. The degree of protection of the in vitro hypoosmotic hemolysis of human red blood cells by these compounds ranged from 30-65%, at a final concentration of 1 mM. All phenothiazine derivatives (1 mM) possessed antiproteolytic activity which was reflected by 25-71% protection observed with these compounds against in vitro trypsin-induced hydrolysis of bovine serum albumin. These compounds at a dose of 100 mg/kg provided 20-80% protection against pentylenetetrazol-induced convulsions in mice. All phenothiazine derivatives possessed low toxicity which was reflected by their approximate LD50 values ranging from 500- greater than 1000 mg/kg.

Animals↗
PubMed1978

Substituted oxothiazolyl acetic acids as antiinflammatory agents.

Eight 2-arylimino-3-[/3-(3,4-dimethoxyphenyl) ethy1]-4-oxothiazol-5-yl-acetic acids were synthesized, characterized, and evaluated for their antiinflammatory and antiproteolytic properties. The toxocity of the compounds was reflected by their approximate LD50 values.

Acetates↗
PubMed1978

Anticonvulsant activity and monoamine oxidase inhibitory and antihemolytic properties of some newer 4-phenylpiperidino carbamides.

Six 1-[N-acetyl(4-phenylpiperidino)]-3-aryl carbamides were synthesized, characterized and evaluated for their anticonvulsant, monoamine oxidase inhibitory and antihemolytic properties. These compounds (100 mg/kg, i.p.) provided 10--80% protection against pentylenetetrazol-induced seizures in mice. All carbamides (1 mM) inhibited (34--82%) in vitro activity of rat brain monoamine oxidase and provided 18--51% protection against in vitro hypoosmotic hemolysis of human red blood cells at a final concentration of 1 mM. Low toxicity of these carbamides was reflected by their high approximate LD50 values.

Animals↗
PubMed1977

Synthesis of 5-substituted 2-oxazolidinethiones and their antagonism to uterotropic effect of diethylstilbestrol.

5-(4-Aminophenoxymethyl)-2-oxazolidinethiones were synthesized by the cyclization of 1-(4-aminophenoxy)-3-amino-2-propanol in the presence of potassium hydroxide and carbon disulfide. This oxazolidinethione, on reaction with suitable isothiocyanates, yielded 5-[4-(substituted thiocarbamido)phenoxymethyl]-2-oxazolidinethiones. These compounds antagonized the uterotropic effects of diethylstilbestrol in female rats and possessed approximate LD50 values of 400-greater than 800 mg/kg.

Animals↗
PubMed1977

Correlation between antiinflammatory and antiproteolytic properties of substituted benzylidenes.

Twelve substituted benzylidenes were evaluated for antiinflammatory activity against carrageenin-induced edema in rats. The protection afforded by these compounds at a dose of 100 mg/kg, i.p., ranged from 30 to 60%. Sodium salicylate (100 mg/kg, i.p.), used as a reference drug, exhibited a 30% antiinflammatory activity under similar experimental conditions. The in vitro effects of substituted benzylidenes were also investigated on the activity of trypsin during hydrolysis of bovine serum albumin, serum glutamate oxaloacetate transaminase, serum glutamate pyruvate transaminase, and endogenous lipid peroxide formation by liver homogenates. These results have provided some correlation between antiinflammatory and antiproteolytic properties of substituted benzylidenes.

Animals↗
PubMed1977

Anti-inflammatory and antiproteolytic properties of substituted guanidines.

Ten N-(4-propoxyphenyl)-N'-(4-chlorophenethyl)-N"-substituted guanidines were synthesized from the corresponding 1-(4-propoxyphenyl)-3-substituted thiocarbamides and evaluated for anti-inflammatory and antiproteolytic properties. All substituted guanidines (50 mg/kg) provided 1-31% protection against carrageenin-induced edema in rats. Hydrocortisone (10 mg/kg) and oxyphenbutazone (40 mg/kg), used as reference drugs, exhibited greater anti-inflammatory activity. All substituted guanidines (1 mM) possessed antiproteolytic activity. The degree of protection observed by these compounds against trypsin-induced hydrolysis of bovine serum albumin ranged from 12.9 to 52.0% while such a protection with sodium salicylate (1 mM), used as a reference drug, was 52%. In the present study, the antiproteolytic activity possessed by these compounds was found to bear no relationship with their anti-inflammatory property.

Animals↗
PubMed1977

Anticonvulsant activity and selective inhibition of NAD-dependent oxidations by 1,4-disubstituted piperazines.

Several 1-(1-aryl-3-ethylthiocarbamido)-4-(arylaminothiocarbonyl)piperazines were synthesized, characterized by their sharp melting points and elemental analyses and evaluated for anticonvulsant activity. All disubstituted piperazines at a dose of 100 mg/kg i.p. provided 10-90% protection against pentylenetetrazol-induced convulsions in mice. These disubstituted piperazines selectively inhibited the in vitro oxidation of nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate, alpha-ketoglutarate, beta-hydroxybutyrate and NADH by rat brain homogenates. The NAD-independent oxidation of succinate remained unaltered. The anticonvulsant activity possessed by disubstituted piperazines was unrelated with their ability to selectively inhibit respiratory activity of rat brain homogenates. Amongst 1-(substituted benzyl)-4-(substituted benzoyl)piperazines exhibiting central nervous system (1, 2) depressant activity it was found that 1-(2-chlorobenzyl)-4-(2-chlorobenzoyl)piperazine possessed maximum activity (2). The ability of piperazine carbamides (3) and piperazinothiocarbamides to possess anticonvulsant activity (4) prompted synthesis of 1-(1-aryl-3-ethylthiocarbamido)-4-(arylaminothiocarbonyl)piperazines and evaluation of their anticonvulsant activity. The effects of these disubstituted piperazines were also investigated on the in vitro respiratory activity of rat brain homogenates in an attempt to elucidate the biochemical mechanism of action for their anticonvulsant activity.

Animals↗
PubMed1977

Selective induction of liver drug-metabolizing enzymes in rats exposed to a 21 ATA He-O2 environment.

The effects of prolonged exposure to a hyperbaric environment (21 ATA He-O2, 200 +/- 300 mm Hg O2, 32.5 +/- 1 degrees C) were investigated on the activity of rat liver drug-metabolizing enzyme systems, as monitored by O-dealkylation and N-dealkylation reactions. Continuous exposure of different groups of rats to a hyperbaric environment for 8, 22, 39, 57, or 84 d significantly increased the in vitro activity of drug-metabolizing enzymes in liver preparations obtained from rats subjected to prolonged exposures. The increase in the in vitro O-dealkylation of p-nitroanisole was selective; and the percent increases were 27, 146, 58, 40, 49, and 44 in liver preparations obtained from rats exposed continuously for 8, 22, 39, 57, 72, or 84 d, respectively. On the other hand, no statistically significant increase was observed in the in vitro activity of rat liver drug-metabolizing enzyme preparations during N-dealkylation of morphine and cocaine.

Animals↗
PubMed1976

Anticonvulsant activity and selective inhibition of nicotinamide adenine dinucleotide-dependent oxidations by 10-(2-arylimino-3-acetylamino-4-thiazolidonyl) phenothiazines.

Several Several 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines and their corresponding cyclized 10-(2-arylimino-3-acetylamino-4-thiazolidonyl)phenothiazines were synthetized and characterized by their sharp melting points and elemental analyses. All compounds inhibited nicotinamide adenine dinucleotide (NAD)-dependent oxidation of pyruvate and alpha-ketoglutarate selectively, whereas NAD-independent oxidation of succinate remained unaltered. All phenothiazine derivatives exhibited anticonvulsant activity, which was reflected by the 20-60% protection observed against pentylenetetrazol-induced convulsions in mice. The ability of substituted thiosemicarbazidophenothiazines to inhibit cellular respiratory activity was reduced considerably by cyclization to the corresponding substituted thiazolidinophenothiazines. On the other hand, cyclization generally resulted in increased anticonvulsant activity. Thus, the anticonvulsant activity possessed by these substituted phenothiazines bore no relationship with their ability to inhibit selectively the NAD-dependent oxidations. Selective inhibition of NAD-dependent oxidation of pyruvate and alpha-ketoglutarate in isolated rat brain mitochondria by some 10-(1-acetyl-4-arylthiosemicarbazido) phenothiazines was concentration dependent and competitive in nature.

Animals↗