Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 43 for “"Benzimidazoles"”.
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Synthesis and profiling of antimalarial side-chain modified pyrido[1,2-a]benzimidazoles
… antimalarial chemotype, namely the pyrido[1,2-a]benzimidazoles (PBI) class of compounds. A frontrunner compound based on the PBI scaffold was previously found to possess potent antiplasmodial activity in vitro [IC₅₀(Pf NF54) = 0.11 μM; IC₅₀(Pf K1) = 0.12 μM] and promising oral efficacy (95% at …
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Synthesis, biological activity and physicochemical properties evaluation of antiplasmodial pyrimido[1,2-a]benzimidazoles
Malaria is an infectious disease which still causes high morbidity and mortality rates among the world's poorest populations, especially in tropical and sub-tropical regions. In 2020, 241 million malaria cases and 627 000 associated deaths were reported, with 94% of them on the African continent, …
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Studies on Organophosphorus Catalyzed C(SP³)–H Amination for the Synthesis of Benzimidazoles
… C(sp³)–H functionalization; (2) scope studies to benzimidazoles by in situ oxidation of the corresponding dihydrobenzimidazole; and (3) insight into the reaction mechanism through in situ spectroscopic monitoring under catalytic conditions and Hammett linear free energy relationship studies. The …
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In vitro anti-cancer effects of benzimidazoles on the canine osteosarcoma D17 cell line
… vitro effects of the clinically-used veterinary benzimidazoles [mebendazole (MBZ), fenbendazole (FBZ), and albendazole (ABZ)] on a canine OS cell line. Cell lines were evaluated for dose-dependent anti-neoplastic effects on the functions of cell proliferation, cell-cycle phase distribution, and …
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Design and Synthesis of Novel Benzimidazoles and Aminothiazoles as Small Molecule Inhibitors of CDK5/p25
… An efficient synthesis of trisubtituted benzimidazoles was developed to explore the SAR at the 1-, 4-, and 6- positions of the benzimidazole core. X-ray crystal structure verification of an intermediate confirmed selective alkylation of the N-1 position of the benzimidazole scaffold. …
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Antimalarial benzimidazoles and related structures incorporating an intramolecular hydrogen bonding motif: medicinal chemistry and mechanistic studies
… In this study, two classes of compounds, benzimidazoles and imidazopyridines, incorporating an intramolecular hydrogen bonding (IMHB) motif, were explored for their antimalarial potential. These two chemotypes were selected on account of their privileged nature due to their capacity to …
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Piperazine-based pyrido[1,2-a]benzimidazoles: synthesis and pharmacological evaluation as potential antimalarial and antischistosomal agents
… as antischistosomal agents. Pyrido[1,2-a]benzimidazoles (PBIs) demonstrate various biological and pharmacological properties such as anti-inflammatory, analgesic, antimicrobial, antiviral, and antineoplastic activities. More recently, PBI derivatives showed favourable in vitro activities …
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Synthesis and biological evaluation of trimeric 2,5-disubstituted benzimidazoles and related trinuclear ruthenium(II) organometallic complexes
Cancer remains a global epidemic, with millions affected by the Non-Communicable Disease (NCD) annually. While cisplatin and its platinum(II) derivatives remain widely used chemotherapeutic agents, the undesirable side effects associated with the use of these metallodrugs and the evolution of …
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Design and Synthesis of Benzimidazoles as CDK5 Inhibitors and Progress toward the Total Synthesis of Tubulysin D
… the design and synthesis of 1,4,6-trisubstituted benzimidazoles as CDK5 inhibitors and the progress toward the total synthesis of tubulysin D.</p><p> Tubulysin is a natural product with potential anti-cancer activity. The two gamma-amino acids in the Tuv and Tup fragments of tubulysin were …
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Physicochemical, biological and β-haematin inhibiting activity of pyrido-dibemequines, pyrido[1,2-α]benzimidazoles and their derivatives
There is an urgent need for new antimalarials following the emergence of Plasmodium falciparum strains with reduced sensitivity to the currently used artemisinin combination therapies. Classical aminoquinoline-based drugs inhibit the formation of haemozoin (HZ) thereby causing parasite death from …
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Synthesis, pharmacological and physicochemical profiling of antimalarial and antischistosomal N-aryl 3-trifluoromethyl pyrido [1,2-α] benzimidazoles
Malaria and schistosomiasis represent the two most prevalent parasitic infections with grievous repercussions on the socio-economic development of affected countries, mainly in sub-Saharan Africa and South-East Asia. Despite their ravaging effects, the treatments of these two diseases have been …
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Synthesis, structure-activity relationship and solubility improvement studies of potential antimalarial and antischistosomal pyrido[1,2-a]benzimidazoles
In 2016, 216 million malaria cases with 445,000 associated deaths were recorded according to the World Health Organization (WHO). Schistosomiasis also remains a public health issue with 207 million cases recorded globally and 280,000 deaths in the same year. Widespread emergence of parasite …
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Synthesis, pharmacological and solubility evaluation of antiplasmodial pyrido[1,2-a]benzimidazoles with cyclic and functionalized amine side chain substituents
… agents for treatment of malaria. Pyrido[1,2-a]benzimidazoles (PBIs) have previously been shown to possess potent antiplasmodial activity, but their in vivo antimalarial activity is limited by poor oral bioavailability arising from low aqueous solubility. The mechanism of action of PBI …
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Structure-activity and structure-property relationships of antimalarial pyrimido[1,2-a]benzimidazoles, imidazo[1,2-a]pyridines, and imidazo[1,2-a]pyrimidines
… and structural diversity. In 2011, pyrido[1,2-a]benzimidazoles (PBI) were reported as a promising novel antimalarial chemical series. However, one of the shortcomings of these compounds, which present a barrier to achieving optimal in vivo efficacy, is their poor aqueous solubility and suboptimal …
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Structure-activity relationship studies of 2-phenylbenzimidazoles and related organometallic complexes as antiplasmodial agents
… resistant strains in particular. In this regard, benzimidazoles have been identified as promising potential drug candidates, displaying potent antiplasmodial activity. Furthermore, benzimidazoles can be chemically transformed into metal-containing organometallic complexes that elevate generally …
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Synthesis, physicochemical and biological evaluation of N-dealkylated metabolites of antimalarial pyrido[1,2-a]benzimidazoles and related compounds containing a Mannich base side-chain
Malaria is one of the leading causes of deaths worldwide. Despite strategic implementations aimed at decreasing mortality and morbidity rates in recent decades, this plasmodial disease continues to impact public health and the economies of developing countries. Furthermore, the emergence of …
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Design and Synthesis of CDK-5 and MEK-5 Inhibitors and Synthesis towards Tubulysin Analogs
… progression of Alzheimer's disease. C6-O linked benzimidazoles and C-4 benzamide and phenylacetamide benzimidazoles based on (R)-Roscovitine, a non-selective inhibitor of CDK-5 were designed and synthesized. </p><p>MEK-5, a member of the MAPK family, phosphorylates ERK-5 permitting cells to …
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Synthesis and evaluation of selected benzimidazole derivatives as potential antimicrobial agents. An investigation into the synthesis of substituted benzimidazoles and their evaluation in vitro for antimicrobial activity.
Microbe resistence is a serious issue, especially as they have become resistant to most well known drugs. Therefore this is considered as a global problem and is now dealt with at a poitical level. Since no new classes of antimicrobial agents have been discovered in the past three deacdes, the …
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