title: Synthesis and biological evaluation of platensimycin analogs.
abstract: Platensimycin (1) displays antibacterial activity due to its inhibition of the elongation condensing enzyme (FabF), a novel mode of action that could potentially lead to a breakthrough in developing a new generation of antibiotics. The medicinal chemistry efforts were focused on the modification of the enone moiety of platensimycin and several analogs showed significant activity against FabF and possess antibacterial activity.
authors.affiliation: Departments of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065-0900, USA.
authors.forename: Hong C
authors.initials: HC
authors.lastname: Shen
authors.forename: Fa-Xiang
authors.initials: FX
authors.lastname: Ding
authors.forename: Sheo B
authors.initials: SB
authors.lastname: Singh
authors.forename: Gopalakrishnan
authors.initials: G
authors.lastname: Parthasarathy
authors.forename: Stephen M
authors.initials: SM
authors.lastname: Soisson
authors.forename: Sookhee N
authors.initials: SN
authors.lastname: Ha
authors.forename: Xun
authors.initials: X
authors.lastname: Chen
authors.forename: Srinivas
authors.initials: S
authors.lastname: Kodali
authors.forename: Jun
authors.initials: J
authors.lastname: Wang
authors.forename: Karen
authors.initials: K
authors.lastname: Dorso
authors.forename: James R
authors.initials: JR
authors.lastname: Tata
authors.forename: Milton L
authors.initials: ML
authors.lastname: Hammond
authors.forename: Malcolm
authors.initials: M
authors.lastname: Maccoss
authors.forename: Steven L
authors.initials: SL
authors.lastname: Colletti
mesh_terms: D015099:3-Oxoacyl-(Acyl-Carrier-Protein) Synthase / Q000037:antagonists & inhibitors* / Q000737:chemistry; D000218:Adamantane / Q000138:chemical synthesis* / Q000494:pharmacology; D062365:Aminobenzoates / Q000138:chemical synthesis* / Q000494:pharmacology; D000813:Anilides / Q000138:chemical synthesis* / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001426:Bacterial Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D018360:Crystallography, X-Ray / Q000379:methods; D015195:Drug Design; D004352:Drug Resistance, Microbial; D013293:Enterococcus faecalis / Q000378:metabolism; D020128:Inhibitory Concentration 50; D008712:Methicillin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D015394:Molecular Structure; D013302:Streptomyces / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D062365:Aminobenzoates; D000813:Anilides; D000900:Anti-Bacterial Agents; D001426:Bacterial Proteins; D015099:3-Oxoacyl-(Acyl-Carrier-Protein) Synthase; C490370:FabF protein, Enterococcus faecalis; D000218:Adamantane; C510909:platensimycin; D008712:Methicillin