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

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Abstract

(±)cis-2-(4-methoxyphenyl)-3-hydroxy/methoxy-6-methoxy/8-methoxy-2,3-dihydro-1,5-benzothiazepin-4-[5H/5-chloroacetyl/5-(4′-methylpiperazino-1′)acetyl]-ones and nucleosides viz; (±)cis-2-(4-methoxyphenyl)-3,6-dimethoxy-2,3-dihydro-1,5-benzothiazepin-4-[5-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)]-one and (±)cis-2-(4-methoxyphenyl)-3,8-dimethoxy-2,3-dihydro-1,5-benzothiazepin-4-[5-(2,3,5-tri-O-benzoyl-β-D-ribofuranosyl)]-one have been synthesized by the condensation of substituted-2-aminobenzenethiols with methyl (±)trans-3-(4-methoxyphenyl)glycidate in xylene and by stirring the 3-methoxy derivative of 1,5-benzothiazepin-4(5H)-ones with sugar namely β-D-ribofuranosyl-1-acetate-2,3,5-tribenzoate at 155–160 °C in vacuo for 10 hours, respectively.

The synthesized compounds have been characterized by the elemental analyses and spectral data and screened for their antimicrobial activity.

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  1. Department of Chemistry, University of Rajasthan, Jaipur, 302004, India

    Gajendra Singh, Anoop K. Sharma, Neeraj Kumar & L. Prakash

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  1. Gajendra Singh
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  2. Anoop K. Sharma
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Singh, G., Sharma, A.K., Kumar, N. et al. A step forward in the field of drug design: 1,5-benzothiazepines and their nucleosides. Res Chem Intermed 26, 445–453 (2000). https://doi.org/10.1163/156856700X00444

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