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Synthesis and Characterization of Metallated Urea Derivative of Phenyl Coumarin

to test their Anti-mycobacterial activity.

Megha Nain1, Niharika Sinha1, Atul Vashist2 and Rajesh Kumar Gupta1*
1
School of vocational studies and applied sciences, Gautam Buddha university, Greater
Noida , Uttar Pradesh 201306,India
2
Department of Infection and Immunology, THSTI, Faridabad, Haryana, India.

Abstract

Tuberculosis (TB), a highly contagious, devastating chronic disease is caused by


Mycobacterium tuberculosis (Mtb). Worldwide, Mtb is known to cause ~10.4 million new
infections and 1.8 million deaths annually. Despite the availability of various anti-
tubercular drugs, the rapid emergence of drug resistance poses major threat to the
complete control and eradication of TB. Moreover, dormancy/persistence, a hallmark of
Mtb, poses another formidable challenge for the success of any anti-tubercular drug
therapy. Therefore, it becomes imperative to develop newer compounds which can
target both active and latent tuberculosis. In recent years, scientists have been on a
mission to discover new and effective molecules for treating diseases. Among the many
molecules that have been screened, coumarin and its derivates has emerged as a
promising candidate for its potential therapeutic applications. Studies showed that
phenyl coumarin inhibit the synthesis of mycolic acid, a key component of bacterial cell
wall, in addition to this they have showed low toxicity to human cell, providing a potential
new avenue for the treatment of TB. Metal-based drugs are privileged motifs that act as
primary pharmacophores in bioactive compounds for various diseases, including
tuberculosis (TB). Metal-based drugs are privileged motifs that act as primary
pharmacophores in bioactive compounds for various diseases, including tuberculosis
(TB). In this prospective we have synthesized metal-based organometallic complexes
using phenyl coumarin urea derivatives. The compounds synthesized were
characterized by using different spectroscopic techniques i.e., IR, 1H-NMR, 13C NMR
and ESI-mass spectrometry.
References:

1.Richard E Lee et.al, The Structure Activity Relationship of Urea Derivatives as Anti
Tuberculosis, Bioorg Med Chem. 2011 September 15; 19(18): 5585–5595.

2. Gupta et al., Structure-Based Design of DevR Inhibitor Active against


Nonreplicating Mycobacterium tuberculosis, J. Med. Chem. 2009, 52, 20, 6324–6334

3. Cauê Benito Scarim et.al, Recent advances in drug discovery against Mycobacterium
tuberculosis: Metal-based complexes, European journal of medicinal chemistry 214
(2021) 113166

4. Heme Huiqing Zheng et.al , Inhibiting Mycobacterium tuberculosis DosRST Signaling


by Targeting Response Regulator DNA Binding and Sensor Kinase, Chem. Biol. 2020,
15, 52−62.

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