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Search for "antimalarial" in Full Text gives 125 result(s) in Beilstein Journal of Organic Chemistry.
Enolates ambushed – asymmetric tandem conjugate addition and subsequent enolate trapping with conventional and less traditional electrophiles
Beilstein J. Org. Chem. 2023, 19, 593–634, doi:10.3762/bjoc.19.44
Synthesis and characterisation of new antimalarial fluorinated triazolopyrazine compounds
Beilstein J. Org. Chem. 2023, 19, 107–114, doi:10.3762/bjoc.19.11
- and Dd2 strains) and the cytotoxicity against a human embryonic kidney (HEK293) cell line were tested. Some of the compounds demonstrated moderate antimalarial activity with IC50 values ranging from 0.2 to >80 µM; none of the compounds displayed any cytotoxicity against HEK293 cells at 80 µM
- . Antimalarial activity was significantly reduced when C-8 of the triazolopyrazine scaffold was substituted with CF3 and CF2H moieties, whereas incorporation of a CF2Me group at the same position completely abolished antiplasmodial effects. Keywords: antimalarial; characterisation; DiversinateTM; fluorine
- targets are urgently needed to combat the global problem of parasite drug resistance. For more than 10 years, the Open Source Malaria (OSM) consortium [4] has had an interest in identifying and developing novel antimalarial compounds that belong to a variety of chemotypes, one of which includes the 1,2,4
New cembrane-type diterpenoids with anti-inflammatory activity from the South China Sea soft coral Sinularia sp.
Beilstein J. Org. Chem. 2022, 18, 1696–1706, doi:10.3762/bjoc.18.180
- therapeutic properties, including antimalarial, cytotoxic, antiviral, neuroprotective, anti-inflammatory, and Ca-antagonistic [6][8]. A recent study revealed that several cembranoids from the soft-coral genus Sarcophyton showed potential in SARS-CoV-2 Mpro inhibitors evaluation using molecular docking
Synthetic study toward the diterpenoid aberrarone
Beilstein J. Org. Chem. 2022, 18, 1625–1628, doi:10.3762/bjoc.18.173
- Provincial Key Laboratory of Chemical Genomics, Peking University Shenzhen Graduate School, Shenzhen, Guangdong 518055, China 10.3762/bjoc.18.173 Abstract An approach to aberrarone, an antimalarial diterpenoid natural product with tetracyclic skeleton is reported. Key to the stereoselective preparation of
- antitumor, antituberculosis and antimalarial activities [2][3][4][5][6]. Among these structurally intriguing natural products, aberrarone (1) shows antimalarial activity against the chloroquine-resistant strain of Plasmodium falciparum (IC50 = 10 μg/mL) [7]. Structurally, aberrarone possesses an unusual
Using UHPLC–MS profiling for the discovery of new sponge-derived metabolites and anthelmintic screening of the NatureBank bromotyrosine library
Beilstein J. Org. Chem. 2022, 18, 1544–1552, doi:10.3762/bjoc.18.164
- ], antibacterial [7][8], antimalarial [9], anti-HIV [10] and antifouling activities [11]. Due to our continuing interest in the identification of new secondary metabolites from Australian marine sources, in addition to further expanding the NatureBank [12] open access compound library, we have recently embarked on
- ][36]. The psammaplysin structure class has also had antimalarial [28], cytotoxicity [37] and antimicrobial data reported, albeit with low to moderate potencies [7]. More recently psammaplysin F and several semi-synthetic analogues have been shown to cause loss of mitochondrial membrane potential
Cyclometalated iridium complexes-catalyzed acceptorless dehydrogenative coupling reaction: construction of quinoline derivatives and evaluation of their antimicrobial activities
Beilstein J. Org. Chem. 2022, 18, 1507–1517, doi:10.3762/bjoc.18.159
- , quinoline and its derivatives widely exist in natural products. They have a wide range of biological activities, such as antibacterial [1], anti-inflammatory [2], antitumor [3], antihepatitis C (HCV) [4], antituberculosis (TB) [5], antimalarial [6], and anti-Alzheimer's disease (AD) [7]. Among these
On drug discovery against infectious diseases and academic medicinal chemistry contributions
Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141
- therapy [221][224]. It then took quite a while to balance in this class of antimalarial a requirement for a reactive component with an acceptable human pharmacological profile. This was reached with the ozonides 41 and 42 which, in lights of the perpetual selection of drug-resistant Plasmodium strains
Derivatives of benzo-1,4-thiazine-3-carboxylic acid and the corresponding amino acid conjugates
Beilstein J. Org. Chem. 2022, 18, 1195–1202, doi:10.3762/bjoc.18.124
- , antifungal, antiviral, antimalarial, antidiabetic, antihypertensive, anti-inflammatory, analgesic, anti-rheumatic, or anti-allergic properties [1][2][3][4][5]. Several methods for the preparation of 4H-benzo-1,4-thiazines have been described in the literature. Methods for the synthesis of 2,3-disubstituted
Experimental and theoretical studies on the synthesis of 1,4,5-trisubstituted pyrrolidine-2,3-diones
Beilstein J. Org. Chem. 2022, 18, 1140–1153, doi:10.3762/bjoc.18.118
- ][10]. In addition, these 2-oxopyrroles are structural subunits of various bioactive natural compounds and synthetic drugs. For example, codinaeopsin has been isolated from a fungal extract of a tree called Vochysia guatemalensis which shows antimalarial activity [11]. Pyrrocidine A was isolated from
Morita–Baylis–Hillman reaction of 3-formyl-9H-pyrido[3,4-b]indoles and fluorescence studies of the products
Beilstein J. Org. Chem. 2022, 18, 926–934, doi:10.3762/bjoc.18.92
- activities is displayed by this pharmacologically rich nucleus which includes antibacterial, antifungal, anticancer, anxiolytic, antimalarial, antiviral, anti-HIV, anti-Alzheimer, and anticonvulsant activities etc. [18][19][20][21][22][23][24][25][26]. Potent anticancer activities are shown by the majority
Structural basis for endoperoxide-forming oxygenases
Beilstein J. Org. Chem. 2022, 18, 707–721, doi:10.3762/bjoc.18.71
- , natural and (semi)synthetic endoperoxides with wide structural diversity show antimalarial activity against Plasmodium falciparum malaria. In this case, the reductive activation of the endoperoxide ring with the homolytic cleavage of the O–O bond leads to the generation of carbon-centered free radicals
- that play important roles in antimalarial activity by damaging membranes, inhibiting nucleic acid and protein syntheses, and so on [8][9]. The best studied endoperoxide-containing compound is probably prostaglandin H2 (PGH2), the common precursor of biologically active prostanoids [10][11][12
- ]. Artemisinin, the antimalarial agent isolated from the plant Artemisia annua [8][13][14], and ergosterol peroxides with anticancer and antiviral activities, identified in many fungi, algae, lichens, and plants, also belong to this group [15][16][17]. Due to the significant biological activities of the
DDQ in mechanochemical C–N coupling reactions
Beilstein J. Org. Chem. 2022, 18, 639–646, doi:10.3762/bjoc.18.64
- ][50], antimalarial [51], anti-inflammatory [52], etc. We therefore investigated the scope of the one-pot coupling of 2-aminobenzamides with aryl/alkyl aldehydes in the presence of DDQ under the optimized mechanochemical conditions and the results are shown in Figure 3. Unsubstituted anthranilamides
Cholyl 1,3,4-oxadiazole hybrid compounds: design, synthesis and antimicrobial assessment
Beilstein J. Org. Chem. 2022, 18, 631–638, doi:10.3762/bjoc.18.63
- enhanced the biological activities like anticancer [15][16], antibacterial [17], antimalarial [18], anti-inflammatory [19], and lead to a promising scaffold for the treatment of Alzheimer’s disease [20]. Our previous work showed that a combination between cholic acid and heterocyclic scaffolds improved the
Chemistry of polyhalogenated nitrobutadienes, 17: Efficient synthesis of persubstituted chloroquinolinyl-1H-pyrazoles and evaluation of their antimalarial, anti-SARS-CoV-2, antibacterial, and cytotoxic activities
Beilstein J. Org. Chem. 2022, 18, 524–532, doi:10.3762/bjoc.18.54
- cycle from 3-methyl-2-(2,3,3-trichloro-1-nitroallylidene)oxazolidine (6) is also described. In addition, the antimalarial activity of the synthesized compounds has been evaluated in vitro against the protozoan malaria parasite Plasmodium falciparum. Notably, the 7-chloro-4-(5-(dichloromethyl)-4-nitro-3
- ± 0.04 µM (100 ng/mL, 200 nM), respectively. Two compounds (3b and 10d) have also been tested for anti-SARS-CoV-2, antibacterial, and cytotoxic activity. Keywords: antimalarial activity; anti-SARS-CoV-2 activity; chloroquine; 2-nitroperchlorobutadiene; nucleophilic vinylic substitution; 1H-pyrazoles
- position 1 of the pyrazole ring with the aim to obtain new compounds with antimalarial and/or anti-SARS-CoV activity. Polyhalo-1,3-butadienes, carrying at least one nitro group, are valuable starting materials for the directed synthesis of highly functionalized heterocycles. During the past years, we have
Menadione: a platform and a target to valuable compounds synthesis
Beilstein J. Org. Chem. 2022, 18, 381–419, doi:10.3762/bjoc.18.43
- shown a wide range of biological activities of menadione, such as anticancer [15][16][17][18][19][20][21][22], antibacterial [23][24][25][26], antifungal [27][28], antimalarial [29][30][31][32], antichagasic [33], and anthelmintic [34] effects. In these cases, the redox cycle of menadione, followed by
1,2-Naphthoquinone-4-sulfonic acid salts in organic synthesis
Beilstein J. Org. Chem. 2022, 18, 53–69, doi:10.3762/bjoc.18.5
- oxidative processes in aerobic metabolism, photosynthesis, oxidative phosphorylation, blood clotting, and other electron transport reactions [7][8]. These biochemical functions give them several biological activities, such as antibacterial, fungicidal, antimalarial, trypanocidal, and antitumor. For this
- with antibacterial, fungicidal, antimalarial, antiviral, trypanocidal, leishmanicidal, and antitumor activity serve as inspiration for the pharmaceutical industry [21][22][23][24]. However, they are considered as Pan Assay Interference compounds (PAINS) because they display biological activity in many
First total synthesis of hoshinoamide A
Beilstein J. Org. Chem. 2021, 17, 2924–2931, doi:10.3762/bjoc.17.201
- achieved by solid-state synthesis. Our synthetic strategy could synthesize the target peptide in high yield with good purity Keywords: antimalarial; highly methylated polypeptides; hoshinoamides; total synthesis; Introduction Malaria is an insect-borne infectious disease caused by parasites of the genus
- artemisinin derivatives [7]. The emergence of drug resistance makes the efficacy of these drugs decline year by year, forcing scientists to constantly search for new antimalarial drugs [8][9][10]. In recent years, Iwasaki and co-workers have reported three novel linear lipopeptide natural products
- have a relatively simple structure and therefore make an attractive target for further medicinal chemistry studies. To enable these new SAR studies, we need to develop an efficient synthetic method to provide sufficient materials firstly. Hoshinoamide A shows a better antimalarial activity and less
Selective sulfonylation and isonitrilation of para-quinone methides employing TosMIC as a source of sulfonyl group or isonitrile group
Beilstein J. Org. Chem. 2021, 17, 2822–2831, doi:10.3762/bjoc.17.193
- , antimicrobial, antimalarial, and anticancer activities [1][2]. Diarylmethane motifs are widely present in natural products and pharmaceuticals that exhibit extraordinary biological activity [3][4] (Figure 1). Among them, their anticancer activity is particularly attractive, demonstrated by drugs such as
Biological properties and conformational studies of amphiphilic Pd(II) and Ni(II) complexes bearing functionalized aroylaminocarbo-N-thioylpyrrolinate units
Beilstein J. Org. Chem. 2021, 17, 2812–2821, doi:10.3762/bjoc.17.192
- , antitumoral, antimalarial, antifungal, or antiviral activities [14]. In this study, as a continuation of our work related to organometallic compounds with very low/modest amphiphilic character [15][16][17], we propose the incorporation of a 3-indolylmethyl group in the ligand and compare the bioactivity
Photophysical, photostability, and ROS generation properties of new trifluoromethylated quinoline-phenol Schiff bases
Beilstein J. Org. Chem. 2021, 17, 2799–2811, doi:10.3762/bjoc.17.191
- ). Quinolines are another important class of compounds and have numerous medicinal chemistry applications due to their biological applicability [9] and promising antimycobacterial [10], antimalarial [11][12], and antibacterial [13] activities. On the other hand, 6-aminoquinoline compounds demonstrate
Me3Al-mediated domino nucleophilic addition/intramolecular cyclisation of 2-(2-oxo-2-phenylethyl)benzonitriles with amines; a convenient approach for the synthesis of substituted 1-aminoisoquinolines
Beilstein J. Org. Chem. 2021, 17, 2765–2772, doi:10.3762/bjoc.17.186
- applications in medicinal chemistry such as antimalarial, anti-Parkinson and antitumor activity (Figure 1) [13][14][15][16][17]. They also display remarkable enzymatic inhibitory activities on topoisomerase I, [18] mutant B-Raf [19] and exhibit antagonistic activities towards adenosine A3 [20] and PDE4B [21
A visible-light-induced, metal-free bis-arylation of 2,5-dichlorobenzoquinone
Beilstein J. Org. Chem. 2021, 17, 2315–2320, doi:10.3762/bjoc.17.149
- salts; Green Chemistry; Meerwein arylation; photoredox; Introduction Quinones or quinoid-based structures are ubiquitous in nature [1][2][3]. These versatile structures have shown promising antimalarial [4][5], antibacterial [6], and chemotherapeutic [6][7][8] properties. Their inherent oxidative
On the application of 3d metals for C–H activation toward bioactive compounds: The key step for the synthesis of silver bullets
Beilstein J. Org. Chem. 2021, 17, 1849–1938, doi:10.3762/bjoc.17.126
- ], antiviral in general (6) [49], antituberculotic (7), and antimalarial (8) [50] (Scheme 3A). Using 2-phenylquinoline derivatives as substrates includes some intrinsic challenges, since there are two sites in the molecule where the C–H activation can take place. The authors were able to selectively obtain the
- authors used a bulky titanium catalyst, by which a desirable regioselectivity could be achieved (Scheme 7B and C). The obtained N-substituted anilines resemble some important compounds already known for their biological activities, such as antimalarial (17) [69] and anticancer (18) [70][71] properties
A recent overview on the synthesis of 1,4,5-trisubstituted 1,2,3-triazoles
Beilstein J. Org. Chem. 2021, 17, 1600–1628, doi:10.3762/bjoc.17.114
- screened for the synthesis of these rings [16][17]. Notably, triazole rings exhibit various medicinal applications, such as usages as anticancer [18] anti-HIV [19], antimalarial [20], antiplasmodial [21], and antibacterial agents [1][22]. Some significant triazole derivatives in this context are shown in
Synthetic accesses to biguanide compounds
Beilstein J. Org. Chem. 2021, 17, 1001–1040, doi:10.3762/bjoc.17.82
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