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Synthesis and Antihypertensive Activity of 2‐Imino‐2,3‐dihydro‐ 5H ‐1,3,4‐thiadiazolo[2,3‐ b ]quinazolin‐5‐ones
Author(s) -
Liu KangChien,
Hu MingKuan
Publication year - 1987
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.19873200213
Subject(s) - chemistry , hydrazine (antidepressant) , carbon disulfide , hydrolysis , cyanogen bromide , bromide , medicinal chemistry , biological activity , organic chemistry , combinatorial chemistry , biochemistry , in vitro , peptide sequence , gene
Hydrolysis of isatoic anhydride (1) with hydrazine derivatives gave the o ‐aminobenzohydrazides 2a‐c. Treatment of these compounds with carbon disulfide provided the 3‐substituted amino‐2‐mercapto‐quinazolin‐4(3 H )‐ones 3a‐c. Compounds 3a‐c underwent cyclo‐condensation with cyanogen bromide to produce th title compounds 5a‐c in 56‐87% yields. Preliminary pharmacological evaluation of these compounds for antihypertensive activity on anesthetized rats was accomplished.