Design, synthesis, and biological evaluation of novel imidazo[1,2‐a]pyridinecarboxamides as potent anti‐tuberculosis agents

Abstract

Tuberculosis (TB) is an insidious and airborne infectious disease caused by Mycobacterium tuberculosis that mainly affects the lungs. TB is one of the top 10 leading causes of mortality worldwide from a single infectious disease (above HIV/AIDS). In 2018, the World Health Organization (WHO) estimated about 10 million people fell ill with TB worldwide while 1.5 million died as a result of TB infection (0.25 million among people living with HIV) (World Health

Antimycobacterial Activity of the Extract and Isolated Compounds From the Stem Bark of Zanthoxylum leprieurii Guill. and Perr.

“…31 Furthermore, other studies have identified the secondary amide linker as a key pharmacophore responsible for anti-TB activity. 32–34…”

“…31 Furthermore, other studies have identified the secondary amide linker as a key pharmacophore responsible for anti-TB activity. [32][33][34] It is worth noting that the secondary amide linker pharmacophore exists in the structures of rifampicin, isoniazid, and pyrazinamide, 3 of the 4 drugs used as first-line treatments for TB. In addition, amikacin and capreomycin, which are among the 4 second-line medicines for treating TB, contain this pharmacophore in their structures.…”

Design, synthesis and anti-mycobacterial evaluation of imidazo[1,2-a]pyridine analogues

“…Compound 3 was the most potent with MIC value of 0.78 μg mL −1 against MTB H37Rv strain. 16 Amongst the imidazo [1,2-a]pyridine compounds reported by Hongjian Wang et al,4 was the most active with MIC value of <0.035 μM against drug susceptible MTB H37Rv strain. 17 Apeng Wang et al reported new anti-TB agents containing the imidazo [1,2-a]pyridine skeleton.…”

“…Though second- and third-line drugs are also available for treating TB-resistant patients, they still have some significant disadvantages, such as long duration of treatment, higher cost involved for prolonged treatment, and poor drug compatibility. 4 Hence, the search for new anti-tubercular drugs with minimum side effects and better efficacy is still on.…”

Structure-Based Designing, Solvent Less Synthesis of 1,2,3,4-Tetrahydropyrimidine-5-carboxylate Derivatives: A Combined In Vitro and In Silico Screening Approach

“…DHPMs mode of action is evident from the formation of H-bonding along with nucleotides like uracil, thymine, cytosine, adenine and guanine in both DNA and RNA [ 4 ]. This class of heterocyclic synthetic compounds contains many naturally occurring therapeutic drugs like quinine, emetine, dibucaine, morphine and reserpine, as shown in Figure 1 [ 5 , 6 ].…”