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Literature DB >> 20810191

Aqua mediated synthesis of 2-amino-6-benzothiazol-2-ylsulfanyl-chromenes and its in vitro study, explanation of the structure-activity relationships (SARs) as antibacterial agent.

Mazaahir Kidwai¹, Roona Poddar, Saurav Bhardwaj, Satendra Singh, Pratibha Mehta Luthra.

Abstract

Multi-component reaction (MCR) involves coupling of p-bromophenol with 2-Benzothiazolethiol, malononitrile and substituted aldehydes in aqueous K(2)CO(3) as green base to synthesize 2-amino-6-benzothiazol-2-ylsulfanyl-chromenes. This multi-component reaction thus offers a higher yield and versatility in the preparation of densely functionalized oxygen heterocycles. The newly synthesized compounds were screened for their antibacterial activities against positive and gram negative pathogenic strains to bacteria. SAR analysis was performed to explore comprehensive structure-activity relationships and a statistically reliable model to explain their antibacterial activities.

Entities: Chemical Disease

Mesh：

Substances：

Year: 2010 PMID： 20810191 DOI： 10.1016/j.ejmech.2010.08.010

Source DB: PubMed Journal: Eur J Med Chem ISSN： 0223-5234 Impact factor: 6.514

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Cited

5 in total

1. Crystal structures of two 4H-chromene derivatives: 2-amino-3-cyano-4-(3,4-di-chloro-phen-yl)-7-hy-droxy-4H-benzo[1,2-b]pyran 1,4-dioxane monosolvate and 2-amino-3-cyano-4-(2,6-di-chloro-phen-yl)-7-hy-droxy-4H-benzo[1,2-b]pyran.

Authors: S Silambarasan; A Jamal Abdul Nasser; T Mohandas
Journal: Acta Crystallogr E Crystallogr Commun Date: 2019-09-27

Aqua mediated synthesis of 2-amino-6-benzothiazol-2-ylsulfanyl-chromenes and its in vitro study, explanation of the structure-activity relationships (SARs) as antibacterial agent.

1. Crystal structures of two 4H-chromene derivatives: 2-amino-3-cyano-4-(3,4-di-chloro-phen-yl)-7-hy-droxy-4H-benzo[1,2-b]pyran 1,4-dioxane monosolvate and 2-amino-3-cyano-4-(2,6-di-chloro-phen-yl)-7-hy-droxy-4H-benzo[1,2-b]pyran.

2. Crystal structure of ethyl (4R)-2-amino-7-hy-droxy-4-phenyl-4H-chromene-3-carboxyl-ate.

3. N'-[3-Cyano-4-(4-fluoro-phen-yl)-6-meth-oxy-4H-benzo[h]chromen-2-yl]-N,N-dimethyl-methanimidamide.

4. 2-Amino-4-(4-bromo-phen-yl)-6-meth-oxy-4H-benzo[h]chromene-3-carbonitrile.

Review 5. Bis[(l)prolinate-N,O]Zn: A water-soluble and recycle catalyst for various organic transformations.