Diversity oriented synthesis for novel anti-malarials
نویسندگان
چکیده
منابع مشابه
Pseudo-Five-Component Condensation for the Diversity-Oriented Synthesis of Novel Indoles and Quinolines Containing Pseudo-Peptides (Tricarboxamides)
A novel series of indole and quinoline tricarboxamides were synthesized using simple and efficient one-pot pseudo-five-component reactions of 2-formylindole or 2-chloro-3-formyl quinolines, isocyanides, amines, and Meldrum’s acid as a CH-acid in CH2Cl2 at room temperature. This conversion has been achieved via the construction of new bonds including two C-C bonds, two ...
متن کاملDiversity-oriented synthesis as a tool for the discovery of novel biologically active small molecules.
Biologically active molecules can be identified through the screening of small-molecule libraries. Deficiencies in current compound collections are evidenced by the continuing decline in drug-discovery successes. Typically, such collections are comprised of large numbers of structurally similar compounds. A general consensus has emerged that library size is not everything; library diversity, in...
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Here, we describe the discovery of a novel antimalarial agent using phenotypic screening of Plasmodium falciparum asexual blood-stage parasites. Screening a novel compound collection created using diversity-oriented synthesis (DOS) led to the initial hit. Structure-activity relationships guided the synthesis of compounds having improved potency and water solubility, yielding a subnanomolar inhi...
متن کاملDiversity oriented synthesis of novel haloglycolipids potentially useful for crystallization of integral membrane proteins.
A series of novel haloglycolipids were synthesized based on Cu(i) catalyzed Huisgen's [3 + 2] cycloaddition reaction of diversely functionalized azides and alkynes, using a mixture of N-bromosuccinimide and Cu(i) halide as the halogen source. Since halogen atoms, like bromine and iodine, with a very high scattering power facilitate the solving of crystal structures, the title haloglycolipids co...
متن کاملThe Basics of Diversity-oriented Synthesis
In this chapter, the underlying ideas behind diversity-oriented synthesis are introduced. The relationship between diversity-oriented synthesis and combinatorial chemistry is discussed, and the rationale behind the use of diversity-oriented synthesis as a tool for the discovery of biologically active molecules is explained. Common synthetic strategies for the efficient generation of structurall...
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ژورنال
عنوان ژورنال: Systems and Synthetic Biology
سال: 2015
ISSN: 1872-5325,1872-5333
DOI: 10.1007/s11693-015-9171-0