SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF 2H-3-(VARIOUS SUBSTITUTED NDOL-2'-CARBOXAMIDYL)-3,4-DIHYDRO-1,3-BENZOXAZINES AND 2H-3-(2',5'-DISUBSTITUTED INDOL-3'-YL)METHYL-1,3-BENZOXAZOLES

Citation
Bhm. Mruthyunjayaswamy et al., SYNTHESIS AND PHARMACOLOGICAL ACTIVITY OF 2H-3-(VARIOUS SUBSTITUTED NDOL-2'-CARBOXAMIDYL)-3,4-DIHYDRO-1,3-BENZOXAZINES AND 2H-3-(2',5'-DISUBSTITUTED INDOL-3'-YL)METHYL-1,3-BENZOXAZOLES, Indian journal of chemistry. Sect. B: organic chemistry, including medical chemistry, 37(5), 1998, pp. 453-460
Citations number
19
Categorie Soggetti
Chemistry Inorganic & Nuclear
ISSN journal
03764699
Volume
37
Issue
5
Year of publication
1998
Pages
453 - 460
Database
ISI
SICI code
0376-4699(1998)37:5<453:SAPAO2>2.0.ZU;2-Q
Abstract
2H-3-(Various substituted indol-2'-carboxamidylimino)-5-substituted me thylphenols 3a-m obtained by the reaction of appropriately substituted indole-2-carboxyhydrazides la-h and 5-substituted salicylaldehydes 2a and b, on reduction with sodium borohydride followed by treatment wit h formaldehyde yield respective 2H-3-(various substituted ndol-2'-carb oxamidyl)-3,4-dihydro-1,3-benzoxazines 5a-m. 2-(2',5'-Disubstituted in dol-3'-yl)methyliminophenols 8a-d have been synthesised by reacting 2, 5-disubstituted indol-3-carboxaldehydes 6a-d with o-aminophenol 7. Com pounds 8a-d when reduced with sodium borohydride and subsequent treatm ent with formaldehyde yield the desired 2H-3-(2',5'-disubstituted indo l-3'-yl)methyl-1,3-benzoxazoles 10a-d. All the newly synthesised compo unds have been tested for their antimicrobial activity against E.coli, S.aureus, P.vulgaris and A.niger. Compounds 5a-f and 10a-d have been screened for their anticatatonic and analgesic activities. Only compou nds 5d, 5e and 10d are found to exhibit good anticatatonic activity an d compounds 5e and 10a show good analgesic activity.