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Biomedical subjects

K Kishor

Publications and source records attributed to K Kishor.

At least 19 recordsLinked to original sources
PubMed1984

New guanine deaminase inhibitors.

2-Aryl/alkyl-3-(5'-carboxamido-imidazol-4'-yl)-quinazolin-4-(3H)-o nes have been reported as Guanine deaminase inhibitors. These compounds were prepared from 4-amino-5-imidazol-carboxamide and suitable 2-aryl/alkyl-benzoxazin-4-ones. Compounds were characterized by their m.ps., elemental analyses and I. R. spectra. These compounds have shown significant inhibition, aryl substituent was more effective than alkyl group. This is the first report when quinazolones have been reported as Guanine deaminase inhibitors. Inhibitors of this enzyme can enhance the bioavailability of purine antagonists and in turn are helpful for the chemotherapy of cancer.

Aminohydrolases↗
PubMed1982

Monoamine oxidase inhibitory and CNS activities of some quinazolinones.

16 new compounds have been synthesised in the series of 3-aryl-2-(1'-aryl-piperazin-4'-yl-carboxamidomethyl)-mercapto-quinazolinones. The compounds showed interesting results in anticonvulsant, hypnotic and monoamine oxidase (MAO) inhibitory screenings and are non-toxic. SAR were evaluated.

Animals↗
PubMed1982

Amoebicidal and fungicidal activities of new quinazolones.

Eleven quinazolones were synthesized by condensing 2-phenylanthranil with a suitable peptide in pyridine. The compounds synthesized were characterised by their sharp melting points, elemental analysis and IR spectra. The newly synthesized compounds were tested for their amoebicidal and fungicidal activities. Some of the compounds showed promising results.

Amebicides↗
PubMed1981

Synthesis and biological activities of quinoline hydrochlorides as anthelmintics.

In the present paper twenty five benzene substituted-4-amino quinoline derivatives were synthesized by condensation of 4-chloroquinolines with alkyl p-aminobenzoate or salicylate. The compounds were screened for antiacetylcholinesterase activity and also anthelmintic activity against Hymenolepis nana. Some of these compounds have shown interesting results.

Animals↗
PubMed1981

Some new 5-substituted benzylidene-1-phenyl-3-(2'-pyridinobutan-4'-yl) thiobarbituric acids as psychopharmacological agents.

Ten substituted thiobarbiturates have been prepared in order to evaluate their anticonvulsant activity in vivo and MAO inhibitory activity in vitro. All the compounds have been found good MAO and convulsion inhibitors. 5-(4-N,N-dimethylaminobenzylidene)-1-phenyl-3-(2'-pyridinobutan-4'-yl)thiobarbi turic acid has been found to be best in both these activities.

Animals↗
PubMed1981

Derivatives of n-aryl-N-amino piperazines as potential cardiovascular agents.

24 new substituted piperazino guanidines and 34 substituted benzylideno- or benzylamino-4-phenyl piperazines were synthesized and evaluated for their cardiovascular activity. Several compounds of the above two series exhibited vasopressor or vasodepressor activity without modifying the carotid occlusion (CO) and noradrenaline (NA) induced pressor responses.

Animals↗
PubMed1980

New imidazolylthiocarbamides as guanine deaminase inhibitors.

Guanine deaminase is an important enzyme of purine catabolism which irreversibly deaminates guanine (1) to xanthine (2) and also 8-azaguanine to 8-azaxanthine. 8-Azaguanine is a carcinostatic agent whereas 8-azaxanthine is non-carcinostatic. It has been proposed that the selective action of thioguanine and 8-azaguinine on certain tissue is due to lack of guanine deaminase in these susceptible cell lines. Inhibitors of guanine deaminase are important because it is reasonable to postulate that it will inhibit the conversion of 8-azaguanine to 8-azaxanthine and these could be used with advantage along with thioguanine and 8-azaguanine. This paper reports synthesis of new imidazolylthiocarbamides as guanine deaminase inhibitors.

Aminohydrolases↗
PubMed1979

Synthesis of some newer piperazinoquinazolones as cardiovascular agents.

Twenty nine new substituted 2-methyl-3-(gamma-piperazino-propiophenyl)-4-quinazolone hydrochlorides were synthesised by the Mannich reaction of substituted quinazolones with substituted piperazines and evaluated for their cardiovascular activity. Several compounds of the series exhibited marked and sustained hypotensive activity.

Animals↗
PubMed1979

New CNS-active 3-methyl-4-substituted methyl-delta 2-isoxazolin-5-ones.

Eight 3-methyl-4-substituted methyl-delta 2-isoxazolin-5-ones were synthesized and evaluated for central nervous system (CNS) activity. All compounds at a concentration of 1 . 10(-3) mol/l inhibited rat brain monoamine oxidase (MAO) in vitro and provided protection against pentetrazole-induced convulsions in mice at a dose of 100 mg/kg i.p. Compounds 2 and 6 showed 80% protection. All isoxazolines (100 mg/kg i.p.) potentiated pentobarbital sleeping time in mice.

Animals↗
PubMed1978

3-Methoxy-4-hydroxyphenylglycol in cerebrospinal fluid and vanillylmandelic acid in urine of humans with hypertension.

3-Methoxy-4-hydroxyphenylglycol (MHPG) was measured in lumbar spinal fluid of 20 subjects with hypertension of varied etiology and severity. There was a significant correlation between the concentration of MHPG and the severity of hypertension. However, changes in the concentration of vanillylmandelic acid in the urine of these subjects were insignificant. In six subjects, administration of clonidine or alpha-methyldopa, two centrally acting antihypertensive drugs, was associated with a significant lowering of MHPG concentrations. These data support the hypothesis that central catecholamines are involved in clinical hypertension.

Blood Pressure↗
PubMed1978

Selective inhibition of xanthine oxidase by substituted pyridopyrimidines.

Six 2-methyl-3-substituted-pyrido-(2,3-d)-pyrimidine 4 (3H)-ones were synthesized and evaluated for their ability to inhibit xanthine oxidase and other purine catabolizing enzymes of rat liver. All compounds inhibited xanthine oxidase selectively when tested at a final concentration of 0.5 mM in vitro. Adenosine deaminase, guanosine deaminase and guanine deaminase were unaffected. The inhibition of xanthine oxidase was found to be competitive in nature.

Aminohydrolases↗
PubMed1978

New indolic hypotensive agents.

Seven substituted piperazino indoles were synthesized by the condensation of substituted piperazines with substituted indole-3-aldehyde, and evaluated for hypotensive activity. Only compound 2 exhibited promising hypotensive activity.

Animals↗