Document Detail

Antihypertensive thiadiazoles. 2. Vasodilator activity of some 2-aryl-5-guanidino-1,3,4-thiadiazoles.
MedLine Citation:
PMID:  3361579     Owner:  NLM     Status:  MEDLINE    
Some 2-aryl-5-guanidino-(or N-substituted guanidino)-1,3,4-thiadiazoles and closely related analogues were found to lower blood pressure in metacorticoid (DOCA) hypertensive rats. In the unsubstituted guanidines that exhibited low toxicity, optimum activity resulted when the aryl group was a 2-methylphenyl ring (11). Modifications to the guanidine group did not increase antihypertensive activity, but, in the 2-methylphenyl series, the N-n-butyl- and N-(2-methoxyethyl)guanidines (63 and 78) and the related iminoimidazolidine 93 were of comparable activity to that of the unsubstituted guanidine 11. The iminoimidazolidine 93 showed a somewhat longer duration of action than the guanidine derivatives. Preliminary studies in a pithed rat preparation indicated that these thiadiazole derivatives (11, 63, and 93) lowered blood pressure by a direct relaxant effect on vascular smooth muscle.
S Turner; M Myers; B Gadie; S A Hale; A Horsley; A J Nelson; R Pape; J F Saville; J C Doxey; T L Berridge
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Journal of medicinal chemistry     Volume:  31     ISSN:  0022-2623     ISO Abbreviation:  J. Med. Chem.     Publication Date:  1988 May 
Date Detail:
Created Date:  1988-06-07     Completed Date:  1988-06-07     Revised Date:  2008-11-21    
Medline Journal Info:
Nlm Unique ID:  9716531     Medline TA:  J Med Chem     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  906-13     Citation Subset:  IM    
Department of Medicinal Chemistry, Reckitt and Colman plc, Kingston-upon-Hull, United Kingdom.
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MeSH Terms
Antihypertensive Agents / chemical synthesis*
Blood Pressure / drug effects*
Chemical Phenomena
Decerebrate State
Guanidines / chemical synthesis,  pharmacology*
Muscle, Smooth, Vascular / drug effects
Structure-Activity Relationship
Thiadiazoles / chemical synthesis,  pharmacology*
Reg. No./Substance:
0/Antihypertensive Agents; 0/Guanidines; 0/Thiadiazoles

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