DESIGN AND SYNTHESIS OF SOME NOVEL FLUOROBENZIMIDAZOLES SUBSTITUTEDWITH STRUCTURAL MOTIFS PRESENT IN PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTSFOR ANTITUBERCULAR ACTIVITY

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NANDHA BANGALORE; NARGUND LAXMIVENKATESH GURACHAR; NARGUND SHACHINDRA LAXMIVENKATESH; BHAT KISHORE

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Journal Paper

Paper Information

Journal: Iranian Journal of Pharmaceutical Research Year:2017 | Volume:16 | Issue:3 Page(s): 929-942

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Title

DESIGN AND SYNTHESIS OF SOME NOVEL FLUOROBENZIMIDAZOLES SUBSTITUTEDWITH STRUCTURAL MOTIFS PRESENT IN PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTSFOR ANTITUBERCULAR ACTIVITY

Author(s)

NANDHA BANGALORE | NARGUND LAXMIVENKATESH GURACHAR | NARGUND SHACHINDRA LAXMIVENKATESH | BHAT KISHORE | Issue Writer Certificate

Keywords

FLUOROBENZIMIDAZOLE

ANTITUBERCULAR ACTIVITY

MYCOBACTERIUM TUBERCULOSIS

H37RV STRAIN

NATURAL PRODUCTS

Abstract

Keeping in view the drawbacks associated with research on anti-TB drugs based on plantextracts and the non-availability of fluorinated NATURAL PRODUCTS with ANTITUBERCULAR ACTIVITY hasprompted us to make an effort towards the synthesis and characterization of a novel series offifteen substituted FLUOROBENZIMIDAZOLEs. The newly synthesized compounds were characterizedby I. R, 1H-NMR, 13C-NMR, Mass, and elemental analysis. The synthesized compounds 4(af)and 5(b-j) have been evaluated for their in-vitro antimycobacterial activity against H37Rvstrain (ATCC 27294) by MABA method. Incorporation of methylenedioxyphenyl moiety at2-and 6-position of the benzimidazole ring furnished compounds 4d and 5i with antitubercularactivity comparable or more potent than the naturally occurring compounds with reportedANTITUBERCULAR ACTIVITY. Among the fifteen tested compounds, 4d and 5i emerged as promisinghits characterized by MIC lower than that determined for sesamin against the pathogenicH37RV STRAIN. ANTITUBERCULAR ACTIVITY results indicate that these compounds may be suitablefor further lead optimization. The cytotoxic effect of these active compounds on THP-1 cellline was assessed by MTT assay and the results suggest that these two molecules are potentialcandidates for further development as antitubercular agents.

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APA: Copy

NANDHA, BANGALORE, NARGUND, LAXMIVENKATESH GURACHAR, NARGUND, SHACHINDRA LAXMIVENKATESH, & BHAT, KISHORE. (2017). DESIGN AND SYNTHESIS OF SOME NOVEL FLUOROBENZIMIDAZOLES SUBSTITUTEDWITH STRUCTURAL MOTIFS PRESENT IN PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTSFOR ANTITUBERCULAR ACTIVITY. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 16(3), 929-942. SID. https://sid.ir/paper/288974/en

Vancouver: Copy

NANDHA BANGALORE, NARGUND LAXMIVENKATESH GURACHAR, NARGUND SHACHINDRA LAXMIVENKATESH, BHAT KISHORE. DESIGN AND SYNTHESIS OF SOME NOVEL FLUOROBENZIMIDAZOLES SUBSTITUTEDWITH STRUCTURAL MOTIFS PRESENT IN PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTSFOR ANTITUBERCULAR ACTIVITY. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2017;16(3):929-942. Available from: https://sid.ir/paper/288974/en

IEEE: Copy

BANGALORE NANDHA, LAXMIVENKATESH GURACHAR NARGUND, SHACHINDRA LAXMIVENKATESH NARGUND, and KISHORE BHAT, “DESIGN AND SYNTHESIS OF SOME NOVEL FLUOROBENZIMIDAZOLES SUBSTITUTEDWITH STRUCTURAL MOTIFS PRESENT IN PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTSFOR ANTITUBERCULAR ACTIVITY,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 16, no. 3, pp. 929–942, 2017, [Online]. Available: https://sid.ir/paper/288974/en

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