Profile of trimazosin: An effective and safe antihypertensive agent

Taylor, Colin R.; Leader, Joan P; Singleton, W. S.; Munster, E.; Falkner, Fred C.; O'Neil, James A

doi:10.1016/0002-8703(83)90188-6

Cited by 19 publications

(4 citation statements)

References 26 publications

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“…23 Moreover, in the last decades, several amines, amides, and esters derived from 3,4,5-trimethoxybenzoic acid were synthesized, such as trimazosin an antihypertensive compound, 24 trimethoprim that present antibacterial effect, 25 and podophyllotoxin which are related to antiviral action. 26 In the aim of associate the biological activity with the presence of trimethoxybenzoic group in the structure of terpenes which practically do not exhibit collateral effects, the bornyl-3,4,5-trimetoxybenzoate was synthesized by the reaction of 3,4,5-trimethoxybenzoic acid derived from syringyl constituents of eucalyptus tar, a renewable biomass source.…”

Section: -22mentioning

confidence: 99%

Antimicrobial activity of synthetic bornyl benzoates againstTrypanosoma cruzi

Corrêa

Miranda

Duarte

et al. 2012

Pathogens and Global Health

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We report here for the first time the in vitro effects of (1S,2R,4S)-1,7,7-trimethyl-bicyclo[2.2.1]heptan-2-yl-39,49,59-trimethoxy benzoate (1) and (1S,2R,4S)-1,7,7-trimethyl-bicyclo[2.2.1]heptan-2-yl benzoate (2) on the growth and ultrastructure of Trypanosoma cruzi. These two synthetic compounds exerted an antiproliferative effect on the epimastigote forms of the parasite. The ICs 50/72h of two synthetic L-bornyl benzoates, 1 and 2, was 10.1 and 12.8 mg/ml, respectively. Both compounds were more selective against epimastigotes than HEp-2 cells. Ultrastructural analysis revealed intense cytoplasmic vacuolization and the appearance of cytoplasmic materials surrounded by membranes. The treatment of peritoneal macrophages with compounds 1 and 2 caused a significant decrease in the number of T. cruzi-infected cells. L-Bornyl benzoate derivatives may serve as a potential source for the development of more effective and safer chemotherapeutic agents against T. cruzi infections.

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Section: -22mentioning

confidence: 99%

Antimicrobial activity of synthetic bornyl benzoates againstTrypanosoma cruzi

Corrêa

Miranda

Duarte

et al. 2012

Pathogens and Global Health

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“…Prazosin represents the first highly effective alpha-adrenergic receptor antagonist useful in the management of hypertension; its efficacy vis-a-vis the earlier agents has been explained by post junctional alpha-1 receptor blockade without interference with the neuronal feedback loop via an alpha-2 adrenolytic action (Davey, 1980). In view of the success of prazosin, several other selective alpha-1 antagonists are being developed as antihypertensive drugs, e.g., triamzosin (Taylor et al, 1983), as well as drugs combining alpha-1 adrenergic receptor blockade with other pharmacological actions (see below).…”

Section: Peripheral Alpha-adrenergic Receptor Blocking Agents As Antimentioning

confidence: 99%

“…In contrast to other beta-adrenergic receptor antagonists, labetolol appears to have a favorable effect on plasma lipoprotein profile (Weber et al, 1984). This may be a result of its alpha-1 adrenergic receptor antagonist activity, since a similar effect has been observed with prazosin (Colucci, 1982) and triamzosin (Taylor et al, 1983). It has also been suggested that labetolol is effective in a larger percentage of patients compared to the beta-adrenergic receptor antagonists (Flamenbaum, 1985).…”

Section: Blockade With Other Pharmacologic Activities In the Treatmenmentioning

confidence: 99%

The alpha-1 Adrenergic Receptors

Ruffolo¹

1987

The Receptors

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All rights reservedNo part of this book may be reproduced, stored in a retrieval system, or transmitted in any form or by any means, electronic, mechanical, photocopying, microfilming, recording, or otherwise without written permission from the Publisher.Preface vii ology will allow alpha-l adrenergic receptors to be isolated and purified and their amino acid sequence to be identified. This will ultimately allow for the systematic subclassification of alpha-l adrenergic receptors and for their differential regulation to be studied in greater detail. These new advances are likely to take place within the next five years, and it is our intent for this review of alpha-l adrenergic receptor pharmacology to provide an accurate summary of the current state of knowledge relating to alpha-l adrenergic receptors, which we hope will serve as a foundation upon which to build a broader base of knowledge in the future.

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“…Other related quinazoline a-adrenoceptor blocking drugs have been found effective antihypertensives, trimazosin (Weber et al, 1982;Taylor et al, 1983), diazosin (de Leeuw et al, 1982), and terazosin (Nelson et al, 1982;Drayer et al, 1983).…”

Section: Diureticsmentioning

confidence: 99%