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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]

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