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http://nopr.niscpr.res.in/handle/123456789/21715| Title: | Newer potential quinazolinones as hypotensive agents |
| Authors: | Kumar, Ashok Tyagi, Mirdula Srivastava, V K |
| Issue Date: | Sep-2003 |
| Publisher: | NISCAIR-CSIR, India |
| Abstract: | A series of 3-(substitutedarylidene)hydrazinoacetylamino-2-methyl-6-bromo-quinazolin-4(3H)-ones 4a-e has been prepared by the condensation of 3-(hydrazinoacetylamino)-2-methyl-6- bromoquinazolin-4(3H)-one 3 with different aromatic aldehydes. Compounds 4a-e on treatment with chloro-acetylchloride in the presence of triethylamine are converted into 3-[2'-(substitutedaryl)-3'-chloro-4'-oxo-1'-azetidinyl] aminochloroacetylamino-2-methyl-6-bromoquinazolin-4(3H)-ones 5a-e, which undergo Mannich reaction to yield compounds 6a-c. The structures of all the new compounds have been confirmed by elemental analysis and spectral studies (IR,1H NMR and mass spectroscopy). Compounds 4a-4e, 5a-5e and 6a-6e have been evaluated for hypotensive activity and were round to exhibit activity ranging from 10-90 mmHg. The most active compound of this series is 3-[2'-(p-N-N-dimethylaminobenzylidine))-3׳-chloro-4'-oxo-]'-azetidinyl-aminoacetylamino [-2-[(p-methoxyphenyl)aminoethyl ]-2-methyl-6-bromoquinazo-lin-4(3H)-one 6d which has shown blood pressure lowering activity of 90 mmHg, which lasted for 120 min. at a dose of 2.5 mg/kg i.v. |
| Page(s): | 2142-2145 |
| ISSN: | 0975-0983(Online); 0376-4699(Print) |
| Appears in Collections: | IJC-B Vol.42B(09) [September 2003] |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| IJCB 42B(9) 2142-2145.pdf | 216.79 kB | Adobe PDF | View/Open |
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