Synthesis of halogenated 4-quinolones and evaluation of their antiplasmodial activity

The antimalarial activity of indole alkaloids and hybrids

“…[64] In the P. berghei- strains of P. falciparum. [66] The mechanistic study revealed that these hybrids were distinct from chloroquine and appeared to dissipate mitochondrial potential as an early event in their antiplasmodial action, and therefore may exert their activity by Plasmodium mitochondrial function. respectively.…”

“…respectively. [66] Indole-β-carboline hybrid 26 (IC 50 : 1.0 µM) showed considerable activity against CQR FcB1 strain of P. falciparum, and the SAR indicated that methoxy group at indole and β-carboline moieties were essential for the activity, and removal of the methoxy group led to great loss of activity. [67] The indole-ferrocene hybrids 27 (IC 50 : 12.3-90.1 µM; Figure 5) possessed broad-spectrum activity against the majority of 7 ng/ml against CQR W2 strain of Plasmodium falciparum [35] 90-670 nM against CQS 3D7 and CQR Dd2 strains of P. falciparum [39,40] 7 nM against CQS 3D7 strain of P. falciparum [42] 50 nM against CQS 3D7 strain of P. falciparum [44] 660 nM against CQS D10 strain of P. falciparum [45] 650 nM against CQS D10 strain of P. falciparum [45] (Continues) LI ET AL.…”

Recent Developments in the Synthetic Strategies of 4‐Quinolones and Its Derivatives

“…[67] Hydrogen atom transfer (HAT) reactions, especially which . DFT analysis was performed to understand the mechanism of the reaction which revealed [1,5]-hydride shift of the acetalic hydrogen towards the central carbon atom of the ketenimine motif followed by a 6p-electrocyclization to yield the desired quinolone derivatives. The substrate scope of the reaction was explored to achieve the synthesis of diversely substituted isoquinoline-1-thiones.…”

“…They are considered bioisosteres of the chromen-4-one scaffold and exist in equilibrium with its tautomeric form i. e. 4-hydroxyquinoline (figure 1). [1] They are known to possess a broad range of biological activities which includes antimicrobial, [2,3] antiviral, [4][5] antiplasmodial, [6] antioxidant, [7] anti-inflammatory, [8] anticholinesterase, [9] anticonvulsant, [10] anticancer, [11] neuroprotective, [12] genitourinary infections, [13] prostatitis, respiratory diseases, as well as skin and soft tissue infections. [14][15] In addition to the above, now they are widely explored as anti-HIV, [16] antimalarial agents, [17,18] alkaline phosphatase inhibitors, [19] antifilarial agents, [20] and antidiabetic agent, [21] for the development of novel therapeutic agents.…”

Study on the regioselectivity of the N-ethylation reaction of N-benzyl-4-oxo-1,4-dihydroquinoline-3-carboxamide

“…Nowadays, some of the most important antibiotics used in the treatment of bacterial infections are 4-oxoquinoline derivatives, namely, ciprofloxacin, levofloxacin, lomefloxacin and others [1–2]. Even though the antibacterial profile has been the most common bioactivity associated with this class of substances [1], other types of pharmacological activities have also been explored and were successfully described by researchers around the world [3–4], such as antiviral [5–6], antiplasmoidal [7–8], anticancer [9–10], and trypanocide [11] activities. 4-Oxoquinoline-3-carboxamide derivatives, more specifically, have shown to be a promising structural scaffold for pharmacological profiles [12–22].…”