Novel 1,4-benzothiazine derivatives: synthesis,crystal structure,and anti-bacterial properties |
| |
Authors: | Nada Kheira Sebbar Mohamed El Mehdi Mekhzoum El Mokhtar Essassi Abdelfettah Zerzouf Ahmed Talbaoui Youssef Bakri Mohamed Saadi Lahcen El Ammari |
| |
Affiliation: | 1.Laboratoire de Chimie Organique Hétérocyclique URAC 21, P?le de Compétence Pharmacochimie, Faculté des Sciences,Université Mohammed V,Rabat,Morocco;2.Moroccan Foundation for Advanced Science, Innovation and Research (MASCIR),Rabat,Morocco;3.Laboratoire de Chimie Organique et Etudes Physico-chimique,ENS Takaddoum,Rabat,Morocco;4.Laboratoire de Biochimie et Immunologie, Faculté des Sciences,Université Mohammed V,Rabat,Morocco;5.Laboratoire de Chimie du Solide Appliquée, Faculté des Sciences,Université Mohammed V,Rabat,Morocco |
| |
Abstract: | In order to develop relatively small molecules as pharmacologically active molecules, novel 1,4-benzothiazine derivatives with triazole and oxazolidinone were synthesized. In this study, a series of 1,2,3-triazolylmethyl-1,4-benzothiazine derivatives were developed by exploiting a click chemistry reaction using a CuI-catalyzed Huisgen [3 + 2] cycloaddition. Starting from 2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one, a number of 1,4-benzothiazine derivatives were also synthesized using different alkylating agents to give a 4-(substituted)-2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one in good yields. The crystal and molecular structure of compound oxazolidin-2-one in basic benzothiazine was established by single-crystal X-ray diffraction. The newly synthesized products were subjected to in vitro biological evaluation. The result indicated that the compounds show convincing antibacterial activities against different microorganisms. All structures of the synthesized compounds were elucidated on the basis of spectral analyses and chemical reactions. |
| |
Keywords: | |
本文献已被 SpringerLink 等数据库收录! |
|