4-Aminoquinoline-chalcone/- N -acetylpyrazoline conjugates: Synthesis and antiplasmodial evaluation

Kumar, Sumit; Saini, Anu; Gut, Jiří; Rosenthal, Philip J.; Raj, Raghu; Kumar, Vipan

doi:10.1016/j.ejmech.2017.07.041

Cited by 48 publications

(18 citation statements)

References 35 publications

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“…In Scheme 3, compounds 3(a-j) were coupled with 7-chloro-4-(prop-2-ynyloxy)quinoline complex (6) in presence of CuSO 4 $5H 2 O, sodium ascorbate, (THF : H 2 O, 1 : 2), under the reux conditions 80 C for 8 h to obtain our target compounds 7(a-j). 61 The structures of these compounds were conrmed through various analytical and spectroscopic methods: ( 1 H, 13 C NMR and mass spectra). 2.3.…”

Section: Chemical Synthesismentioning

confidence: 99%

Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development ofPlasmodium falciparumat the trophozoite stage

et al. 2019

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Section: Chemical Synthesismentioning

confidence: 99%

Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development ofPlasmodium falciparumat the trophozoite stage

et al. 2019

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“…The antiplasmodial SAR of hybrids 32 (IC 50 : 114.4 to >10,000 nM) against CQR W2 strain revealed that extension of the carbon spacer between quinoline and 1,2,3‐triazole moieties as well as introduction of methoxy into R 2 position were harmful to the activity. [ 77 ] Among them, four hybrids 32a – d (IC 50 : 114.4–175.3 nM) which were comparable with or better than chloroquine (IC 50 : 150 nM) against CQR W2 strain, also showed low cytotoxicity (IC 50 : 12.7–35.6 μM) toward HeLa cells.…”

Section: Chalcone–quinoline Hybridsmentioning

confidence: 99%

Chalcone hybrids and their antimalarial activity

Cheng

Yang

Huang

et al. 2020

Archiv der Pharmazie

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Malaria, one of the most striking, re‐emerging infectious diseases caused by the genus Plasmodium, places a huge burden on global healthcare systems. A major challenge in the control and eradication of malaria is the continuous emergence of increasingly widespread drug‐resistant malaria, creating an urgent need to develop novel antimalarial agents. Chalcone derivatives are ubiquitous in nature and have become indispensable units in medicinal chemistry applications due to their diverse biological profiles. Many chalcone derivatives demonstrate potential in vitro and in vivo antimalarial activity, so chalcone could be a useful template for the development of novel antimalarial agents. This review covers the recent development of chalcone hybrids as antimalarial agents. The critical aspects of the design and structure–activity relationship of these compounds are also discussed.

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“…Triazole-linked 4-aminoquinoline-chalcone/-N-acetylpyrazoline conjugates (67) were synthesized and evaluated for antiplasmodial activities against cultured chloroquine-resistant strain. The activities were found to be dependent on the length of the alkyl chain as well as on the presence of methoxy substituents on the chalcone rings [69].…”

Section: Miscellaneous Applications Of Chalconesmentioning

confidence: 99%

Biological Role of Chalcones in Medicinal Chemistry

Tekale¹,

Mashele²,

Pooe³

et al. 2020

Vector-Borne Diseases - Recent Developments in Epidemiology and Control

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Chalcones are promising synthons and bioactive scaffolds of great medicinal interest due to their numerous pharmacological and biological activities. They are well recognized to possess antimicrobial, anticancer, antitubercular, antioxidant, anti-inflammatory, antileishmanial, and other significant biological activities. This chapter highlights recent updates and applications of chalcones as biologically, pharmacologically, and medicinally important entities.

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4-Aminoquinoline-chalcone/- N -acetylpyrazoline conjugates: Synthesis and antiplasmodial evaluation

Cited by 48 publications

References 35 publications

Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development ofPlasmodium falciparumat the trophozoite stage

Quinoline-triazole hybrids inhibit falcipain-2 and arrest the development ofPlasmodium falciparumat the trophozoite stage

Chalcone hybrids and their antimalarial activity

Biological Role of Chalcones in Medicinal Chemistry

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