Biomedical subjects
Publications and source records attributed to K Shanker.
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.
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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.
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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.
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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.
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.
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