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Biomedical subjects

K C Joshi

Publications and source records attributed to K C Joshi.

At least 19 recordsLinked to original sources
PubMed1986

Synthesis and antifertility activity of some new fluorine containing 2-([2-(fluoroaryl)-1H-indol-3- yl]methylene)hydrazinecarbothioamides and 2-(fluoroaryl)-([5-(substituted benzylidene)-4-oxo-2-thiazolidinylidene]hydrazone)- 1H-indole-3-carboxaldehydes.

New fluorine containing 2-(fluoroaryl)-1H-indole-3-carboxaldehydes have been synthesized and subjected to reaction with thiosemicarbazide to give corresponding 2-([2- (fluoroaryl)-1H-indol-3-yl]methylene)hydrazinecarbothiamides which were cyclized in the presence of chloroacetic acid, sodium acetate and substituted benzaldehydes to 2-(fluoroaryl)-([5- (substituted benzylidene)-4-oxo-2-thiazolidinylidene]hydrazone)- 1H-indole-3-carboxaldehydes as potential antifertility agents. In preliminary screening, 2-(4'-fluorophenyl)- ([5-(methylene-3,4-dioxyphenyl)-4-oxo-2- thiazolidinylidene]hydrazone)-1H-indole-3-carbocaldehyde exhibited pronounced antifertility activity. All these new compounds have been characterized by analytical and spectral (IR, PMR, MS) studies.

Animals↗
PubMed1985

Studies in spiro heterocycles. Part 4(1): Investigation of the reactions of fluorinated 3-aroylmethylene-indol-2-ones with hydrazine and phenylhydrazine and synthesis of spiro [indole-3,3'-pyrazol]-2-ones.

Reactions of various 3-aroylmethylene-indol-2-ones with hydrazine and phenylhydrazine under exactly similar conditions have been carried out. The reaction with phenylhydrazine has not been investigated earlier. It was found that although the reaction with hydrazine hydrate afforded a spiro derivative viz., spiro[3H-indole-3,3'-(3H)pyrazol]-2(1H)-one, that with phenylhydrazine yielded simply a hydrazone derivative. Representative spiro compounds have been screened for antifertility activity but none was found active at a dose of 10 mg/kg in adult female rats.

Animals↗
PubMed1984

Synthesis and central nervous system activities of certain fluorine-containing 3-substituted indol-2-ones.

Several fluorine-containing 3- aroylmethyl -3-hydroxyindol-2-ones (4a-g), 3- aroylmethyleneindol -2-ones (5a-g) and 3- aroylmethylindol -2-ones (6a-g) were synthesized from the corresponding fluorine-containing indole-2,3-diones and appropriate ketones. The compounds were characterized by spectral studies. Representative compounds of each series were tested on mice for CNS activities, viz. analgesic and anticonvulsant and the effects were also observed against amphetamine-induced stereotypy, on conditioned avoidance response and on potentiation of pentobarbitone sodium hypnosis. Of the compounds examined, the greatest degree of activity was observed in 3- aroyl - methyleneindol -2-ones with a pronounced unsaturation in the system.

Analgesics↗
PubMed1981

Studies in potential organo-fluorine antibacterial agents. Part 6: Synthesis and antibacterial activity of some new fluorine containing 1,3,4,5,7-pentasubstituted dipyrazolo[3,4-b,; 4,3-3]pyridines.

Ten new fluorine containing dipyrazolo [3,4-b;4,3-3]pyridines have been synthesized as possible antibacterial agents. The synthesis involves the condensation of 5-amino-1,3-disubstituted pyrazoles with an appropriate arylaldehyde at 220-240 degrees C. The synthesized compounds have been characterized by their m. p.'s elemental analysis, TLC, IR, 1H-NMR and 19F-NMR. A representative number of compounds have also been screened for their antibacterial activity and most of them were found to inhibit the growth of different bacteria.

Anti-Bacterial Agents↗
PubMed1980

Studies of potential organo-fluorine antibacterial agents. Part 5: Synthesis and antibacterial activity of some new fluorine-containing indole-2,3-dione derivatives.

A series of new 1-dialkylaminoacetyl-5/6-fluoroindole-2,3-diones and 3-arylhydrazino-5/6-fluoro-1-morpholinomethylindol-2-ones have been synthesized; the former by the reaction of different secondary amines with N-chloro-acetyl-5/6-fluoroindole-2,3-diones and the latter, by the condensation of substituted phenylhydrazines with 5/6-fluoro-1-morpholinomethylindole-2,3-diones. All synthesized compounds have been characterized by their IR, 1H-NMR and elemental analysis. These compounds have been screened for their antibacterial activity against the Gram positive bacterium Staphylococcus albus and the Gram negative bacterium Escherichia coli.

Anti-Bacterial Agents↗
PubMed1980

Effect of phenelzine, a monoamine oxidase inhibitor, on isoproterenol-induced myocardial damage.

The effect of phenelzine on isoproterenol-induced myocardial necrosis was studied in rats. Male albino rats were pretreated with 20 mg/kg body wt of phenelzine, intraperitoneally, on 4 consecutive days. The same animals were given 80 mg/kg of isoproterenol subcutaneously on the third and fourth days of the study. After 48 hr of isoproterenol, ECG was recorded, the animals were killed, and blood, heart, and adrenal glands were removed for biochemical and histopathological studies. Phenelzine returned toward normal the isoproterenol-induced decreased in cardiac glycogen but decreased serum lactic acid only slightly toward normal. The serum enzymes, serum glutamic oxaloacetic transaminase (SGOT) and serum glutamic pyruvic transaminase (SGPT), showed the protective effect of phenelzine. The increase in isoproterenol-induced free fatty acid (FFA) was significantly reduced in the group pretreated with phenelzine. Our studies on adrenal ascorbic acid suggest that the animals pretreated with phenelzine suffered less stress compared to the group treated with isoproterenol alone. Histopathological changes including focal areas of necrosis and characteristic cellular exudation were less marked in the hearts of rats pretreated with phenelzine. S-T segment elevation was more marked in the group treated with isoproterenol only.

Alanine Transaminase↗
PubMed1979

Studies in potential organo-fluorine antibacterial agents. Part 2: Synthesis and antibacterial activity of some new fluorine-containing 3.5-disubstituted isoxazoles.

A series of new fluorine-containing 3,5-disubstituted aryl/alkylisoxazoles has been synthesized by the condensation of hydroxylamine with appropriate beta-diketones in the presence of pyridine and characterized by IR and 1H NMR spectral studies. These isoxazoles have been screened for their antibacterial activity against the gram positive bacteria, Staphylococcus albus, Streptococcus nonhemolyticus and the gram negative bacterium Escherichia coli.

Anti-Bacterial Agents↗
PubMed1979

Possible psychopharmacological agents. Part 3: Synthesis and CNS activity of some new fluorine-containing pyrazolo[3,4-e][1,4]thiazepines.

A series of new fluorine-containing pyrazolo [3,4-e][1,4]thiazepines has been synthesized by the condensation of 5-amino-3/1, 3-substituted pyrazole with appropriate arylaldehydes or ketones and mercaptoacetic acid in dry toluene. All synthesized compounds have been characterized by their m.p.'s elemental analysis, IR, H-NMR and F-NMR. A representative number of compounds has also been screened for their CNS activity and found to act as mild stimulants.

Analgesics↗
PubMed1979

Possible psychopharmacological agents. Part 7: Synthesis and CNS activity of some fluorinated 2,4,7/8-trisubstituted-3H-1,5-benzodiazepinium monoperchlorates.

A series of new fluorinated 2,4'7/8-trisubstituted-3H-1,5-benzodiazepinium monoperchlorates have been synthesized and characterized by IR and NMR spectral studies. Representative compounds have been screened for their CNS activity viz., behavioural, analgesic, anticonvulsant and antireserpine. 8-Chloro-2-(4'-fluorophenyl)-4-phenyl-3H-1,5-benzodiazepinium monoperchlorate has shown pronounced antireserpine activity.

Analgesics↗
PubMed1979

Possible psychopharmacological agents. Part 9: Synthesis and CNS activity of some new fluorine-containing 1,2,4-triazolo[4,3-b]pyridazines.

A number of new fluorine-containing 1,2,4-triazolo[4,3-b]pyridazines have been synthesized by the condensation of 4-amino-(4H)-1,2,4-triazole with appropriate fluorinated beta-diketones in glacial acetic acid. All synthesized compounds were characterized by their m.p.'s, nitrogen analysis, IR, 1H NMR and 19F NMR. A representative number of compounds was screened for their CNS activity and found to be mild stimulants.

Analgesics↗