Recent Advances in the Research of Heterocyclic Compounds as Antitubercular Agents

Yan, Mi; Ma, Shutao

doi:10.1002/cmdc.201200339

Cited by 32 publications

(17 citation statements)

References 59 publications

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“…Amino group present in 2 nd position of pyrimidine ring reacts with different aldehydes produced imine (-C=N-) was shown potent activity, alongside 4 th and 6 th substitution plays major role in anti-TB activity [22,23]. Fortunately, varieties of latest potential antitubercular candidate's medication with heterocyclic rings, that are presumably to be effective against resistant strains, have entered clinical trials in current years [24].…”

Section: Fig 1 Structures Of Marketed Antitubercular Drugs With Heterocyclic Ringmentioning

confidence: 99%

Synthesis, Characterization, Anti-Mycobacterial Evaluation and In-Silico Molecular Docking of Novel Isoxazole Clubbed Pyrimidine Derivatives

Nagaraju

Sharabu

2021

JPRI

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In the present research, we tend to ready a series of novel pyrimidine-linked isoxazole derivatives (11-20). The molecular structure and the elemental composition of these compounds were confirmed by spectroscopic studies and elemental analysis. MABA (Microplate alamar Blue Assay) assay was employed for assessing the antitubercular activity against the Mycobacterium tuberculosis H37Rv strain. Among the ten synthesized compounds, 18 and 20 showed excellent anti-tubercular activity than the reference (MIC-3.125 µg/ml) at 0.78 µg/mL. The compounds were found to possess good binding affinity than a standard against thymidylate kinase enzyme (PDB-1MRS) as evidenced by the molecular docking studies. Additionally, the bioactivity was conducted by Mol-inspiration software tool and the drug-likeness property was evaluated on Lipinski's rule of five by SCFBio online software. The lead compounds identified through these studies could be useful for the furtherance of the drug discovery process in the area of antitubercular research.

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Section: Fig 1 Structures Of Marketed Antitubercular Drugs With Heterocyclic Ringmentioning

confidence: 99%

Synthesis, Characterization, Anti-Mycobacterial Evaluation and In-Silico Molecular Docking of Novel Isoxazole Clubbed Pyrimidine Derivatives

Nagaraju

Sharabu

2021

JPRI

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“…In 2016, 10.4 million people fell ill with TB, among them 90% were adults, 65% were male, and 10% were people living with HIV . There are several reasons for the incremental prevalence of TB, and the most important two are drug‐resistant TB (DR‐TB) and HIV/TB coinfection . According to the estimation of WHO, there were 600,000 new cases with resistance to RIF and of which 490,000 had multidrug‐resistant TB (MDR‐TB) .…”

Section: Introductionmentioning

confidence: 99%

Isatin Derivatives with Potential Antitubercular Activities

Jiang

Wang

Liu

et al. 2018

Journal of Heterocyclic Chem

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Tuberculosis is a life‐threatening chronic infectious disease, which primarily affects the lungs but can spread to other vital organs. The re‐emergence and wide spread of new virulent forms of Mycobacterium tuberculosis that are resistant to some or all first and second line antitubercular agents has reached an alarming level in recent decades. Thus, it is imperative to develop more effective agents. Isatin derivatives are endowed with diverse biological properties, therefore thousands of isatin derivatives have been synthesized in hopes of discovering new candidates with potential antitubercular activities against both drug‐susceptible and drug‐resistant strains. This review summarizes the recent developments of isatin derivatives with potential antitubercular activities.

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“…In spite of the first‐line anti‐TB agents are highly effective, they are far from ideal, because the threat from TB is in continual increase, as evidenced by 10.4 million people fell ill with TB throughout the world, with 1.67 million deaths made TB the leading infectious cause of death globally in the year 2016 alone, and the number is still increasing . There are many reasons for the incremental prevalence of TB, including immigration, high population densities, nutrient deficiencies, inadequate environmental conditions, globalization, conflicts, famine, and poor patient compliance, while the most important two reasons are drug‐resistant TB (DR‐TB) and human immunodeficiency virus (HIV)/TB co‐infection . The HIV/TB co‐infection makes the patients more susceptible to reinfection with either drug‐susceptible or drug‐resistant strains, and TB has already known to be the leading cause of death among people living with HIV/acquired immunodeficiency syndrome, resulted in 370,000 deaths in 2016 .…”

Section: Introductionmentioning

confidence: 99%

Quinoline Derivatives with Potential Activity Against Multidrug‐resistant Tuberculosis

Zhou

et al. 2018

Journal of Heterocyclic Chem

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Tuberculosis (TB), which affects primarily the lungs (pulmonary TB) apart from other vital organs, is a life‐threatening chronic deadliest infectious disease caused by members of Mycobacterium tuberculosis (MTB) complex and mainly by MTB itself. The emergence of MTB new virulent forms that are resistant to some or all first‐line and second‐line anti‐TB agents, including multidrug‐resistant (MDR), extensively drug‐resistant, and totally drug‐resistant strains has further aggravated the spread of this disease and was increased up to an alarming level in the recent decades. More than ever, it is imperative to develop novel, high effective, and fast acting anti‐TB drugs to prevent the spread of TB, particularly in its hard‐to‐kill MDR‐TB, extensively drug‐resistant‐TB, and totally drug‐resistant‐TB strains. In recent years, numerous compounds have been synthesized for this purpose, but only a handful of compounds have entered human trials after the discovery of rifampicin, reflecting the inherent difficulties of developing new anti‐TB agents. Despite of bedaquiline and delamanid have received approval from many countries for treatment of MDR‐TB infected patients, both drugs are associated with serious side effects and are only recommended for those MDR‐TB patients without other treatment options. All these aforementioned facts make it an urgent need to develop novel drugs. Quinoline‐based derivatives including quinolones ex biological activities, and some of them displayed excellent in vitro and in vivo activities against MDR‐TB. This review outlines the recent developments of quinoline‐based derivatives with potential activity against MDR‐TB as well as the structure–activity relationship.

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Recent Advances in the Research of Heterocyclic Compounds as Antitubercular Agents

Cited by 32 publications

References 59 publications

Synthesis, Characterization, Anti-Mycobacterial Evaluation and In-Silico Molecular Docking of Novel Isoxazole Clubbed Pyrimidine Derivatives

Synthesis, Characterization, Anti-Mycobacterial Evaluation and In-Silico Molecular Docking of Novel Isoxazole Clubbed Pyrimidine Derivatives

Isatin Derivatives with Potential Antitubercular Activities

Quinoline Derivatives with Potential Activity Against Multidrug‐resistant Tuberculosis

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