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A Pharmacological Appraisal of Antimalarial Plant Species
Published in Namrita Lall, Medicinal Plants for Cosmetics, Health and Diseases, 2022
Mahwahwatse J. Bapela, Precious B. Ramontja, Mcebisi J. Mabuza
Aryl-amino alcohols include quinine, mefloquine, halofantrine and lumefantrine, and their antimalarial activity seem to require the presence of an aromatic portion and an amino alcohol portion (Figure 18.2). Like the 4-aminoquinolines, aryl-amino alcohols are assumed to act primarily on the erythrocyte stage of the malaria parasite by inhibiting the formation of hemozoin (Anderson et al., 2006). 8-Aminoquinolines are derived quinoline molecules with an amine group at the 8-position of quinoline. Primaquine is the only 8-aminoquinoline used in malaria therapy, and studies have shown that it interferes with the parasite’s DNA structure and disrupts its mitochondrial membranes (Miller et al., 2013). It is also the only available drug that can prevent transmission of mature gametocytes, although it can cause intravascular hemolysis in patients with glucose-6-phosphate dehydrogenase deficiency (Sinha et al., 2014). The precise mechanisms of action of the above-mentioned quinoline-based antimalarial drugs are not yet fully understood, and are still under investigation.
Quinoline Mix
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
In studies testing the quinoline mix in groups of selected patients, prevalences of positive reactions have ranged from 1% to 18.3% (table 3.297.3). The very high percentage of 18.3 was in a study from the United Kingdom performed in the period 1988-1991 (32). The population tested consisted of patients with contact allergy to one or more corticosteroids. Co-sensitization in this group to other ingredients of topical pharmaceuticals, both active drugs and excipients, is well known and, presumably, many of these patients had used a corticosteroid-clioquinol combination product (32). High frequencies of sensitization were also found, as can be expected, in patients with leg ulcers/stasis dermatitis (6,7) and otitis externa (13,14). In most studies, no relevance data were provided, but in those that did, relevance figures were high with 60-100% (9-12,30).
Synthetic Approaches to Inhibitors of Isoprenoid Biosynthesis
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Pedro Merino, Loredana Maiuolo, Ignacio Delso, Vincenzo Algieri, Antonio De Nino, Tomas Tejero
The same researchers synthesized various quinoline derivatives (167–173) through different synthetic strategies (Fig. 2.5). Quinoline derivatives 167–173.
Synthesis, kinetic studies and in-silico investigations of novel quinolinyl-iminothiazolines as alkaline phosphatase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Muhammad Naeem Mustafa, Pervaiz Ali Channar, Muhammad Sarfraz, Aamer Saeed, Syeda Abida Ejaz, Mubashir Aziz, Fatmah Ali Alasmary, Hanadi Yaqob Alsoqair, Hussain Raza, Song Ja Kim, Asad Hamad
In the quest for safe drug therapy, researchers are striving for development of novel and specific medication for APs associated malignancies. Among various heterocyclic compounds, the quinolone and thiazolines possessed a wide range of biological and pharmacological activities including anti-cancer, anti-fungal, analgesic, antihypertensive and antibiotic activities. Specifically, quinoline has displayed an broad spectrum of biological applications such as anti-fungal, antimalarial, anticonvulsant, analgesic, anti-bacterial, cardiotonic anthelmintic, and anti-inflammatory activities19. Several pharmacologically active substances and natural products (Cinchona Alkaloids) possess quinoline nucleus20. The most famous quinoline based drug chloroquine I (Figure 1) resulted in eradication and control of malaria for the decades. This type of drugs influence parasite’s life cycle during blood stages21.
Metabolic and pharmacological profiling of Penicillium claviforme by a combination of experimental and bioinformatic approaches
Published in Annals of Medicine, 2022
Zafar Ali Shah, Khalid Khan, Zafar Iqbal, Tariq Masood, Hassan A. Hemeg, Abdur Rauf
The LC-MS chromatogram displayed peaks for all of the potential metabolites found in the mycelium of P. claviforme (Figure 1). Interestingly, the metabolites identified had previously been reported from different sources such as plants, microbes and marine organisms. Quinoline is a weak base with many pharmacological and biological activities [35]. These include analgesic, anthelmintic, cardiotonic, antifungal, anti-inflammatory, antimalarial, antibacterial and anticonvulsant activities. It is used as an intermediate in the synthesis of many products. Its higher exposure in mice has been linked to adverse effects [36]. N-(6-Oxo-6H-dibenzo[b,d]pyran-3-yl)acetamide belongs to coumarin class. A study was conducted to investigate the inhibitory action of acetamide coumarin on monoamine oxidase A in rats with serotonin using the radiometric protocol. The significant inhibitory response showed by coumarin metabolite [37]. Phalluside-1 is a glycolipid that has been isolated in large quantities from marine microorganisms. Significant antifungal activity has been shown by phallusides-1 against phytopathogenic fungi [38,39]. 3β,15β,17α-trihydroxy-pregnenone was synthesised by selective fungal specie through biotransformation. It showed promising activity against the inhibition of cholinesterase [40]. β-funaltrexamine is an alkaloid with morphinane nucleus. The inhibitory effect of morphine was blocked by β-funaltrexamine, demonstrating that it has a suppressive effect [41].
Discovery of novel quinoline-based analogues of combretastatin A-4 as tubulin polymerisation inhibitors with apoptosis inducing activity and potent anticancer effect
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2021
Tarek S. Ibrahim, Mohamed M. Hawwas, Azizah M. Malebari, Ehab S. Taher, Abdelsattar M. Omar, Thikryat Neamatallah, Zakaria K. Abdel-Samii, Martin K. Safo, Yaseen A. M. M. Elshaier
Quinoline derivatives are popular for the treatment of malaria37,38. Moreover, quinoline heterocyclic containing compounds demonstrate potent anticancer activities with different modes of actions, including inhibition of proteasome, tyrosine kinases, and tubulin polymerisation39–41. Previous studies have reported the antiproliferative activity of CA-4, isoCA-4 or chalcone compounds containing quinoline scaffold, either as ring A bioisoster, e.g. 4a23 and 4b42 or ring B bioisoster, e.g. 4c43–45 and 4d46. These compounds demonstrate the potential of the quinoline ring as a template for developing more promising tubulin polymerisation inhibitors and antiproliferative agents.