A step forward in the field of drug design: 1,5-benzothiazepines and theirnucleosides

Citation
G. Singh et al., A step forward in the field of drug design: 1,5-benzothiazepines and theirnucleosides, RES CHEM IN, 26(5), 2000, pp. 445-453
Citations number
29
Categorie Soggetti
Chemistry
Journal title
RESEARCH ON CHEMICAL INTERMEDIATES
ISSN journal
09226168 → ACNP
Volume
26
Issue
5
Year of publication
2000
Pages
445 - 453
Database
ISI
SICI code
0922-6168(2000)26:5<445:ASFITF>2.0.ZU;2-4
Abstract
(+/-)cis-2-(4-methoxyphenyl)-3-hydroxylmethoxy-6-methoxy/8-methoxy-2,3-dihy dro-1,5-benzo-thiazepin-4-[5H/5-chloroacetyl/5-(4'-methylpiperazino-1')acet yl] -ones and nucleosides viz; (+/-)cis-2-(4-methoxyphenyl)-3,6-dimethoxy-2 ,3-dihydro-1,5-benzothiazepin4-[5-(2,3,5-tri-O-benzoyl-beta -D-ribofuranosy l)]-one and (+/-)cis-2-(4-medioxyphenyl)-3,8-dimedioxy-2,3-dihydro-1,5-benz othiazepin-4-[5-(2,3,5-tri-O-benzoyl-beta -D-ribofuranosyl)]- one have been synthesized by the condensation of substituted-2-aminobenzenethiols with m ethyl (+/-)trans-3-(4-methoxyphenyl)glycidate in xylene and by stirring the 3-methoxy derivative of 1,5-benzothiazepin-4(5H)-ones with sugar namely be ta -D-ribofuranosyl-1-acetate-2,3,5-tribenzoate at 155-160 degreesC in vacu o for 10 hours, respectively. The synthesized compounds have been characterized by the elemental analyses and spectral data and screened for their antimicrobial activity.