title: Utilizing diversity-oriented synthesis in antimicrobial drug discovery.
abstract: The development of resistance to existing antimicrobials has created a threat to human health that is not being addressed through our current drug pipeline. Limitations with the use of commercial vendor libraries and natural products have created a need for new types of small molecules to be screened in antimicrobial assays. Diversity oriented synthesis (DOS) is a strategy for the efficient generation of compound collections with a high degree of structural diversity. Diversity-oriented synthesis molecules occupy the middle ground of both complexity and efficiency of synthesis between natural products and commercial libraries. In this review we focus upon the use of diversity-oriented synthesis compound collections for the discovery of new antimicrobial agents.
authors.affiliation: Therapeutics Platform, Broad Institute of MIT & Harvard, 7 Cambridge Center, Cambridge, MA 02142, USA.
authors.forename: Eamon
authors.initials: E
authors.lastname: Comer
authors.forename: Jeremy R
authors.initials: JR
authors.lastname: Duvall
authors.forename: Maurice
authors.initials: M
authors.lastname: duPont Lee
mesh_terms: D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D001688:Biological Products / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D003141:Communicable Diseases / Q000188:drug therapy; D004353:Drug Evaluation, Preclinical; D006094:Gram-Positive Bacteria / Q000187:drug effects; D057166:High-Throughput Screening Assays; D006801:Humans; D018155:Orthopoxvirus / Q000187:drug effects; D010963:Plasmodium falciparum / Q000187:drug effects; D054852:Small Molecule Libraries / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D000890:Anti-Infective Agents; D001688:Biological Products; D054852:Small Molecule Libraries
keywords: Trypanosoma cruzi; chemical complexity; diversity-oriented synthesis; drug discovery; hepatitis C virus; infectious disease; malaria; orthopoxviruses