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1.
Nat Prod Commun ; 10(3): 503-4, 2015 Mar.
Article in English | MEDLINE | ID: mdl-25924539

ABSTRACT

Crocetenone, a new rotenoid (1), along with five known compounds apocyanin (2), tectorigenin (3), 5,2',3'-trihydroxy-7-methoxy flavanone (4), tectoridin (5) and tectoridin glycoside (6), were isolated from the methanolic extract of the root of Iris crocea. The structure of compounds was elucidated on the basis of 1D- and 2D-NMR spectroscopic and MS analysis. Antibacterial and antioxidant activities of compounds 1-6 were evaluated. Crocetenone (1) showed a prominent antibacterial activity.


Subject(s)
Iris Plant/chemistry , Isoflavones/chemistry , Molecular Structure , Rhizome/chemistry
2.
Eur J Med Chem ; 76: 274-83, 2014 Apr 09.
Article in English | MEDLINE | ID: mdl-24589483

ABSTRACT

A series of benzfused heterocyclic derivatives such as amide conjugates of 2-(benzo[d]thiazol-2-ylthio)acetic acid with aromatic/aliphatic/cyclic secondary amines (5a-5o & 8a-8m); 1,2,3-triazole conjugates of 2-mercaptobenzothiazoles and amide conjugates of indole-3-glyoxalic acid with cyclic secondary amines (14a-14g) have been synthesized and were screened for their antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth microdilution assay method. Compounds 8b, 8f, 8g and 8l inhibited the growth of the H37Rv strain at concentrations of 8 µg/mL. These compounds (8b, 8f, 8g and 8l) have been further identified as bactericidal and are completely killing the microbes at 32-64 µg/mL concentrations. Molecular docking studies of the active compounds reveal that these compounds are targeting DprE1 and may act as DprE1 inhibitors.


Subject(s)
Antitubercular Agents/pharmacology , Benzothiazoles/pharmacology , Mycobacterium tuberculosis/drug effects , Sulfur/analysis , Benzothiazoles/chemistry , Magnetic Resonance Spectroscopy , Microbial Sensitivity Tests , Molecular Docking Simulation , Spectrometry, Mass, Electrospray Ionization
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