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Showing 1 to 6 of 6 for “"Bioisosteres"”.
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BIOISOSTERES OF AMPA: CONFORMATIONAL ANALYSIS AND STRUCTURE ACTIVITY RELATIONSHIP
… work has focused on the synthesis of analogs and bioisosteres of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA), including lipophilic analogs using lateral metalation and electrophilic quenching and their evaluations at the system xc- transporter. Bioisosteres which are not …
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BIOISOSTERES OF AMPA: CONFORMATIONAL ANALYSIS AND STRUCTURE ACTIVITY RELATIONSHIP
… work has focused on the synthesis of analogs and bioisosteres of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA), including lipophilic analogs using lateral metalation and electrophilic quenching and their evaluations at the system xc- transporter. Bioisosteres which are not …
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Exploring the synthesis and functionalisation of methano[10]annulene
… molecules. One method to achieve this is through bioisosteres. Bioisosteres are “groups or molecules which have chemical and physical similarities producing broadly similar biological effects”. For this thesis, the proposed bioisostere of naphthalene, methano[10]annulene was investigated. …
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MMV008138 and analogs: potential novel antimalarial agents for P. falciparum
… SAR of lead compound MMV008138. Synthesized acid bioisosteres and A-ring analogs of MMV008138 were evaluated in their ability to inhibit P. falciparum parasite growth. We showed that the C3 substituent of MMV008138 has a very tight SAR, and likely interacts with a very constricted pocket within …
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PART I: SYNTHESIS OF PHENOLIC ANTIBACTERIALS AND NATURAL PRODUCTS PART II: RAPID ASSESSMENT OF HYDROGEN BONDING CAPACITY
… were obtained for a set of carboxylic acid bioisosteres. The values from the single point measurements were validated with full titrations.
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Synthesis and biological evaluation of trimeric 2,5-disubstituted benzimidazoles and related trinuclear ruthenium(II) organometallic complexes
… compounds were synthesized as non-planar bioisosteres of the 2-aryl 5-substituted benzimidazole trimeric ligands. All of the synthesized compounds were fully characterized using an array of spectroscopic (1H, 13C{1H}, 31P{1H} and 19F{1H} NMR, FT-IR spectroscopy) and analytical (mass …