Category: indole-building-block. Recently I am researching about DRUG DISCOVERY; ANTITUBERCULAR ACTIVITY; BIOLOGICAL EVALUATION; CRYSTAL-STRUCTURES; DIRECT INHIBITORS; DPRE1 INHIBITORS; DERIVATIVES; ANTIOXIDANT; SCAFFOLD; TARGET, Saw an article supported by the DSTDepartment of Science & Technology (India) [DST/INSPIRE Fellowship/IF170273]; Pondicherry UniversityPondicherry University; University Grants Commission (UGC), New DelhiUniversity Grants Commission, India [F.540/6/DSA-1/2016/(SAP1)]. Published in ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER in ISSY-LES-MOULINEAUX ,Authors: Ramesh, D; Joji, A; Vijayakumar, BG; Sethumadhavan, A; Mani, M; Kannan, T. The CAS is 99-93-4. Through research, I have a further understanding and discovery of 4′-Hydroxyacetophenone
Indole chalcones were designed and synthesized as a promising set of compounds against H(37)Rv strain of Mycobacterium tuberculosis. Within this library of compounds, (E)-1-(furan-3-yl)-3-(1H-indol-3-yl)prop-2-en-1-one (18), (E)-3-(1H-indol-3-yl)-1-(thiophen-2-yl)prop-2-en-1-one (20) and (E)-2-((1H-indol-2-yl)methylene)cyclopentan-1-one (24) displayed high anti-tubercular activity at 50 mu g/ml with MIC values of 210, 197 and 236 mu M respectively. The in-silico studies revealed that compound 18 exhibit binding modes similar to FAS-II inhibitors like INH or Thiolactomycin against KasA protein. Cytotoxicity assay results suggest that the compounds 18, 20 and 24 are non-cytotoxic to human megakaryocytes and murine B cells. (C) 2020 Elsevier Masson SAS. All rights reserved.
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Reference:
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