68223-33-6Relevant academic research and scientific papers
Toward an efficient and eco-friendly route for the synthesis of dimeric 2,4-diacetyl phloroglucinol and its potential as a SARS-CoV-2 main protease antagonist: Insight from: In silico studies
Kusumaningsih, Triana,Prasetyo, Wahyu E.,Wibowo, Fajar R.,Firdaus, Maulidan
supporting information, p. 7830 - 7843 (2021/05/13)
As a consequence of the unavailability of an anti-viral drug for SARS-CoV-2, the prospect of developing an antiviral drug is of great importance in this current emergency of the COVID-19 pandemic era. To support the enduring research on the improvement of
One pot synthesis and anticancer activity of dimeric phloroglucinols
Chauthe, Siddheshwar K.,Bharate, Sandip B.,Periyasamy, Giridharan,Khanna, Amit,Bhutani, Kamlesh K.,Mishra, Prabhu D.,Singh, Inder P.
experimental part, p. 2251 - 2256 (2012/05/04)
A series of dimeric phloroglucinol compounds were synthesized in a single step using commercially available phloroglucinol and methanesulfonic acid. Based on the reported anticancer activity of plant derived dimeric phloroglucinols, these synthesized comp
Biomimetic synthesis and anti-HIV activity of dimeric phloroglucinols
Chauthe, Siddheshwar K.,Bharate, Sandip B.,Sabde, Sudeep,Mitra, Debashis,Bhutani, Kamlesh K.,Singh, Inder P.
experimental part, p. 2029 - 2036 (2010/06/12)
Plants are an important source of a variety of bioactive compounds with different modes of action. Anti-HIV agents from plant sources can be useful in developing novel therapies for inhibiting HIV infection. Based on the reported anti-HIV activity of plant derived phloroglucinols, several new dimeric phloroglucinols were synthesized in the present study by varying substitution on aromatic ring and at methylene bridge. Some of the synthesized compounds have shown good HIV inhibitory activity in a human CD4+ T cell line (CEM-GFP) infected with HIV-1 NL4.3 virus isolate. Structure-activity studies indicate that phenyl, 4-benzyloxy-1-phenyl and cyclohexyl substitution at methylene bridge gave compounds with better anti-HIV activity. Compounds 22 and 24 showed highest anti-HIV activity with an IC50 of 0.28 μM and 2.71 μM, respectively, former was more active than the positive standard AZT in cell based assay.
Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists
Bharate, Sandip B.,Rodge, Atish,Joshi, Rajendra K.,Kaur, Jaspreet,Srinivasan, Shaila,Senthil Kumar,Kulkarni-Almeida, Asha,Balachandran, Sarala,Balakrishnan, Arun,Vishwakarma, Ram A.
scheme or table, p. 6357 - 6361 (2009/10/01)
In this letter, we report discovery of diacylphloroglucinol compounds as a new class of GPR40 (FFAR1) agonists. Several diacylphloroglucinols with varying length of acyl functionality and substitution on aromatic hydroxyls were synthesized and evaluated for GPR40 agonism using functional calcium-flux assay. Out of 17 compounds evaluated, 14, 17, 19 and 25 exhibited good GPR40 agonistic activity with EC50 values ranging from 0.07 to 8 μM (pEC50 7.12-5.09), respectively, with maximal agonistic response of 84-102%.
