A multicomponent reaction to design antimalarial pyridyl-indole derivatives: Synthesis, biological activities and molecular docking

Elshemy, Heba A.H.; Zaki, Mohamed A.; Mohamed, Enas I. A.; Khan, Shabana I.; Lamie, Phoebe F.

doi:10.1016/j.bioorg.2020.103673

Cited by 40 publications

(15 citation statements)

References 46 publications

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“…toward VERO cells. [71] The RI and SI values were 0.74 and >7.5, respectively, and the mechanistic study indicated that this could act on the active site of quadruple mutant P. falciparum dihydrofolate reductase enzyme. The CQR W2 strain of P. falciparum to hybrid 31…”

Section: Indole Hybridsmentioning

confidence: 94%

The antimalarial activity of indole alkaloids and hybrids

Sun

et al. 2020

Archiv der Pharmazie

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Malaria, caused by the genus Plasmodium, remains a global public health concern. It is estimated by the World Health Organization that over 40% of the world's population lives in areas at risk for malarial transmission, and around half a million people succumb to this infectious disease annually, which is related to the rapid spread of drug-resistant parasite strains. Indole derivatives, which possess broadspectrum pharmacological properties, play a crucial role in the discovery of new drugs. Many indole derivatives exhibited potential in vitro and in vivo activity against both drug-sensitive and drug-resistant malaria, suggesting that the indole moiety is a useful template for the development of novel antimalarial agents.

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Section: Indole Hybridsmentioning

confidence: 94%

The antimalarial activity of indole alkaloids and hybrids

Sun

et al. 2020

Archiv der Pharmazie

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“…Compounds 50-52 were the most active at the binding cavities of quadruple-mutant Pf DHFR-TS-active sites, indicating suitable binding associations that might be the mechanism influencing their activity as antimalarial agents. 197 Xue et al reported fosmidomycin derivatives containing the pyridine scaffold that inhibited P. falciparum DXR with K i values of 1.9-13 nM. The most potent compound (Figure 28) was elevenfold as active as fosmidomycin.…”

Section: Antimalarial Agentsmentioning

confidence: 99%

The Expanding Role of Pyridine and Dihydropyridine Scaffolds in Drug Design

Ling

Hao

Liang

et al. 2021

DDDT

191

114

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Pyridine-based ring systems are one of the most extensively used heterocycles in the field of drug design, primarily due to their profound effect on pharmacological activity, which has led to the discovery of numerous broad-spectrum therapeutic agents. In the US FDA database, there are 95 approved pharmaceuticals that stem from pyridine or dihydropyridine, including isoniazid and ethionamide (tuberculosis), delavirdine (HIV/AIDS), abiraterone acetate (prostate cancer), tacrine (Alzheimer's), ciclopirox (ringworm and athlete's foot), crizotinib (cancer), nifedipine (Raynaud's syndrome and premature birth), piroxicam (NSAID for arthritis), nilvadipine (hypertension), roflumilast (COPD), pyridostigmine (myasthenia gravis), and many more. Their remarkable therapeutic applications have encouraged researchers to prepare a larger number of biologically active compounds decorated with pyridine or dihydropyridine, expandeing the scope of finding a cure for other ailments. It is thus anticipated that myriad new pharmaceuticals containing the two heterocycles will be available in the forthcoming decade. This review examines the prospects of highly potent bioactive molecules to emphasize the advantages of using pyridine and dihydropyridine in drug design. We cover the most recent developments from 2010 to date, highlighting the ever-expanding role of both scaffolds in the field of medicinal chemistry and drug development.

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“…. Docking studies explained the interaction between compound and active site of the enzyme (quadruple mutant Plasmodium falciparum dihydrofolate reductase) [86]…”

Section: Anti-inflammatory and Analgesic Activitiesmentioning

confidence: 99%

A brief review of the biological potential of indole derivatives

2020

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Background Various bioactive aromatic compounds containing the indole nucleus showed clinical and biological applications. Indole scaffold has been found in many of the important synthetic drug molecules which gave a valuable idea for treatment and binds with high affinity to the multiple receptors helpful in developing new useful derivatives. Main text Indole derivatives possess various biological activities, i.e., antiviral, anti-inflammatory, anticancer, anti-HIV, antioxidant, antimicrobial, antitubercular, antidiabetic, antimalarial, anticholinesterase activities, etc. which created interest among researchers to synthesize a variety of indole derivatives. Conclusion From the literature, it is revealed that indole derivatives have diverse biological activities and also have an immeasurable potential to be explored for newer therapeutic possibilities.

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A multicomponent reaction to design antimalarial pyridyl-indole derivatives: Synthesis, biological activities and molecular docking

Cited by 40 publications

References 46 publications

The antimalarial activity of indole alkaloids and hybrids

The antimalarial activity of indole alkaloids and hybrids

The Expanding Role of Pyridine and Dihydropyridine Scaffolds in Drug Design

A brief review of the biological potential of indole derivatives

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