Synthesis and SARs of indole-based 伪-amino acids as potent HIV-1 non-nucleoside reverse transcriptase inhibitors was written by Han, Xin;Wu, Haoming;Wang, Wei;Dong, Chune;Tien, Po;Wu, Shuwen;Zhou, Hai-Bing. And the article was included in Organic & Biomolecular Chemistry in 2014.Application of 4769-96-4 This article mentions the following:
A series of non-nucleoside reverse transcriptase inhibitors derived from indole-based 伪-amino acids were designed and synthesized. Their inhibitory activities were detected by a TZM-bl cell assay on HIV virus type HIV-1IIIB. The comprehensive understanding of the SAR was obtained by utilizing the variation of the substituents of the indole-based 伪-amino acids. From the screened compounds, the novel inhibitors (I) (R1 = 5-Cl and 6-Br) were identified to be highly potent candidates with EC50 values of 0.060 渭M and 0.045 渭M resp. (CC50 values of 109.545 渭M and 49.295 渭M and SI values of 1825.8 and 1095.4). In most cases, the variation of substituents at different positions had a significant effect on the potency of activities. The results also indicate that the indole-based 伪-amino acids as efficient NNRTIs displayed comparable anti-HIV-1 activities to the reference drug NVP. We hope the identification of these indole-based amino acids as efficient NNRTIs of RT could stimulate researchers to develop more diversified anti-HIV drugs. In the experiment, the researchers used many compounds, for example, 6-Nitro-1H-indole (cas: 4769-96-4Application of 4769-96-4).
6-Nitro-1H-indole (cas: 4769-96-4) belongs to indole derivatives. Indole is an important structural motif of various drugs, therapeutic leads besides its prevalence in numerous natural products, agrochemicals, perfumery, and dyes. Due to this activity, the indole ring system has become an important component or intermediate in the synthesis of heterocycles.Application of 4769-96-4
Referemce:
Indole alkaloid derivatives as building blocks of natural products from聽Bacillus thuringiensis聽and聽Bacillus velezensis聽and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles