[Et3NH][HSO4] catalyzed efficient synthesis of 5-arylidene-rhodanine conjugates and their antitubercular activity

[Et3NH][HSO4] catalyzed efficient synthesis of 5-arylidene-rhodanine conjugates and their... Keywords Ionic liquid  Antitubercular activity  Cytotoxicity  Rhodanine and Knoevenagel condensation Introduction Almost 9 million new cases of human tuberculosis (TB) are diagnosed and 1.5 million deaths are reported worldwide [1]. Mycobacterium tuberculosis (MTB)is among the most challenging bacterial infections, requiring daily combination therapy of up to 4 drugs for at least 6 months to treat uncomplicated drug-sensitive infections [2]. Nowadays, synergy with HIV and the appearance of MTB strains, which are multi-drug resistant or hyper-virulent, poses further threats [3–5]. Thus, the discovery of novel anti-TB drug targets is of increasing importance in combating this disease. In addition, M. bovis BCG vaccination is also among the most commonly administered vaccines worldwide [6]. It is usually the first vaccine administered to newborns in developing countries and is a part of the expanded programme of immunization of the World Health Organization WHO [7]. Rhodanine (2-thioxothiazolid-4-one) and their analogues have been known as privileged structures in pharmacological research which display a broad spectrum of biological activities [8]. In particular, 5-arylidene rhodanines display antifungal [9] and antibacterial properties [10, 11], are DNA polymerase k inhibitors [12, 13], and anti-inflammatory [14, 15], while ZTB24, ZTB28R and ZTB29R are antitubercular agents [16, 17]. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Research on Chemical Intermediates Springer Journals

[Et3NH][HSO4] catalyzed efficient synthesis of 5-arylidene-rhodanine conjugates and their antitubercular activity

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Publisher
Springer Journals
Copyright
Copyright © 2016 by Springer Science+Business Media Dordrecht
Subject
Chemistry; Catalysis; Physical Chemistry; Inorganic Chemistry
ISSN
0922-6168
eISSN
1568-5675
D.O.I.
10.1007/s11164-016-2484-0
Publisher site
See Article on Publisher Site

Abstract

Keywords Ionic liquid  Antitubercular activity  Cytotoxicity  Rhodanine and Knoevenagel condensation Introduction Almost 9 million new cases of human tuberculosis (TB) are diagnosed and 1.5 million deaths are reported worldwide [1]. Mycobacterium tuberculosis (MTB)is among the most challenging bacterial infections, requiring daily combination therapy of up to 4 drugs for at least 6 months to treat uncomplicated drug-sensitive infections [2]. Nowadays, synergy with HIV and the appearance of MTB strains, which are multi-drug resistant or hyper-virulent, poses further threats [3–5]. Thus, the discovery of novel anti-TB drug targets is of increasing importance in combating this disease. In addition, M. bovis BCG vaccination is also among the most commonly administered vaccines worldwide [6]. It is usually the first vaccine administered to newborns in developing countries and is a part of the expanded programme of immunization of the World Health Organization WHO [7]. Rhodanine (2-thioxothiazolid-4-one) and their analogues have been known as privileged structures in pharmacological research which display a broad spectrum of biological activities [8]. In particular, 5-arylidene rhodanines display antifungal [9] and antibacterial properties [10, 11], are DNA polymerase k inhibitors [12, 13], and anti-inflammatory [14, 15], while ZTB24, ZTB28R and ZTB29R are antitubercular agents [16, 17].

Journal

Research on Chemical IntermediatesSpringer Journals

Published: Feb 29, 2016

References

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