Anti-hypertensive activities

A substituted thiazole ring attached to a reduced imidazole moiety is present in a compound that displays anti hypertensive activity. Reaction of thiourea 61 with methyl iodide to... 

It is difficult to draw firm conclusions about the relevance of this central action of 3-blockers in animals to their clinical anti-hypertensive activity bearing in mind that brain concentrations of the different drugs varies widely... 

Takano, T. 2002. Anti-hypertensive activity of fermented dairy products containing biogenic peptides. Antonie van Leeuwenhoek 82, 333-340. 

A similar study of the anti-hypertensive activity of the alkaloids of Kopsia teoi were also carried out which were also prompted by positive results from preliminary screening of alkaloidal extracts. The major aspidofractinine alkaloid kopsingine (191) was found to produce dose-related decreases in mean arterial blood pressure and heart rate in anaesthetized spontaneously hypertensive rats (SHR) which were similar to those elicited in normotensive controls. The same depressor response was shown by the 12-demethoxy derivative (kopsaporine, 192) and the semisynthetic 14,15-dihydto derivative of kopsingine 252, indicating that minor modifications to the basic structure of kopsingine do not significantly alter... 

The oligosaccharides prepared from alginate can exhibit a variety of biological activities, including anti-allergy properties, anti-hypertensive activity, an ability to enhance the growth of human endothelial cells and keratinocytes, and an ability to induce cytokine production [157]. 

Reaction of sulphamide 337 with a series of amines has led to the synthesis of 2-sulphamido-1.3,4.6.7,11b-2-hexahydro-2//-benzo[V]-quinolizines (349), R3 = NHS02NH2, and the anti-hypertensive activity of the compounds in rats has been reported355. 

Labetalol (12.20), a recent analogue, has four stereoisomers because it has two centres of asymmetry (marked with stars). The (R,S) and the (S,S) isomers are virtually inactive, the (S,R) isomer has most of the a-adrenergic blocking activity, and the (R,R) has virtually all of the jS-adrenergic blocking activity and is the only isomer with anti-hypertensive activity comparable to propranolol (Gold etal., 1982). 

Table 3.2 ACE-inhibitory and anti-hypertensive activity in spontaneously hypertensive rats of peptides produced by fermentation of milk and soybean... 

Some of the ACE-inhibitory peptide fractions from cheese have shown in vivo activities in SHR. A water-soluble peptide preparation isolated from Gouda ripened for 8 months was found to have the most potent anti-hypertensive activity (maximum decrease in SBP=24.7 ( 0.3) mmHg (E<0.01) after 6h) when administered to SHR by gastric intubation at doses between 6.1 and 7.5mg/kg body weight. Three peptide fractions were isolated from water-soluble extract by hydrophobic chromatography using different concentrations of acetonitrile (Saito et al., 2000). 

Compounds affecting adrenergic transmitters - Fusaric acid amide (XIV, Sch 10595) is a very active inhibitor of dopamine-3"hydroxy1ase in vivo (but not in vitro), and it lowers the blood pressure of DOCA hypertensive rats for many hours in a dose-related manner.53 The cyclohexylamino-oxazoline (XV, BAY a678i) probably exerts its hypotensive effect by preventing the release of catecholamines from the adrenal gland.5 3-Ethyl-a-methyltyrosine (XVl) is a competitive inhibitor of tyrosine hydroxylase and exhibits significant anti hypertensive activity in DOCA rats at 25 mg/kg. It may be preferable to a-methyltyrosine because it should not be metabolised into a catechol amine.55... 

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