Design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates was written by Fu, Liqiang;Liu, Xin;Ling, Chenyu;Cheng, Jianjun;Guo, Xingsheng;He, Huili;Ding, Shi;Yang, Yushe. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.Recommanded Product: 6-Nitroisoindolin-1-one This article mentions the following:
We report herein the design, synthesis, and structure-activity relationship studies of conformationally restricted mutilin 14-carbamates based on the structure of SB-222734. For example, reacting benzoates I (R1 = H, MeO, NO2, R2 = H, F, NO2, R9 = H) with N-bromosuccinimide gave the brominated compounds I (R9 = Br), which cyclized to give isoindolinones II. II were then coupled with 4-epi-mutilin 14-chloroformate III and treated with a saturated solution of ZnCl2 in concentrated HCl resulting in a reverse 1,5-hydride shift to afford desired products IV. The antibacterial activities of these newly synthesized compounds were also evaluated and compared with linezolid and retapamulin. Results showed that most of the target compounds exhibit good potency in inhibiting the growth of Gram-pos. bacteria including Methicillin-susceptible Staphylococcus aureus MSSA (MIC: 0.0625-2 μg/mL), Methicillin-resistant S. aureus MRSA (MIC: 0.0625-2 μg/mL), Methicillin-susceptible Staphylococcus epidermidis MSSE (MIC: 0.0625-2 μg/mL), Methicillin-resistant S. epidermidis MRSE (MIC: 0.0625-2 μg/mL), and Streptococcus pneumonia (MIC: 0.0625-4 μg/mL). In particular, three remarkable compounds of this series IV (R1 = NH2, R2 = H; R1 = H, R2 = NH2) and isoquinolinyl derivative V exhibited comparable in vitro antibacterial profiles to that of retapamulin. In the experiment, the researchers used many compounds, for example, 6-Nitroisoindolin-1-one (cas: 110568-64-4Recommanded Product: 6-Nitroisoindolin-1-one).
6-Nitroisoindolin-1-one (cas: 110568-64-4) belongs to indole derivatives. The indole subunit is an almost ubiquitous component of biologically active natural products, and its study has been the focus of research for decades. They are capable of binding to a variety of receptors with high affinity and thus have applications in a wide range of therapeutic areas.Recommanded Product: 6-Nitroisoindolin-1-one
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles