title: Isolation, enzyme-bound structure and antibacterial activity of platencin A1 from Streptomyces platensis.
abstract: Natural products continue to serve as one of the best sources for discovery of antibacterial agents as exemplified by the recent discoveries of platensimycin and platencin. Chemical modifications as well as discovery of congeners are the main sources for gaining knowledge of structure-activity relationship of natural products. Screening for congeners in the extracts of the fermentation broths of Streptomyces platensis led to the isolation of platencin A(1), a hydroxy congener of platencin. The hydroxylation of the tricyclic enone moiety negatively affected the antibacterial activity and appears to be consistent with the hydrophobic binding pocket of the FabF. Isolation, structure, enzyme-bound structure and activity of platencin A(1) and two other congeners have been described.
authors: Merck Research Laboratories, Rahway, NJ 07065, USA. sheo_singh@merck.com
authors: Sheo B
authors: SB
authors: Singh
authors: John G
authors: JG
authors: Ondeyka
authors: Kithsiri B
authors: KB
authors: Herath
authors: Chaowei
authors: C
authors: Zhang
authors: Hiranthi
authors: H
authors: Jayasuriya
authors: Deborah L
authors: DL
authors: Zink
authors: Gopalakrishnan
authors: G
authors: Parthasarathy
authors: Joseph W
authors: JW
authors: Becker
authors: Jun
authors: J
authors: Wang
authors: Stephen M
authors: SM
authors: Soisson
mesh_terms: D000218:Adamantane / Q000031:analogs & derivatives* / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D062365:Aminobenzoates / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D000627:Aminophenols / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D000813:Anilides / Q000737:chemistry / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology; D018360:Crystallography, X-Ray; D008968:Molecular Conformation; D011083:Polycyclic Compounds / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology; D013302:Streptomyces / Q000737:chemistry*; D013329:Structure-Activity Relationship
chemical_list: D062365:Aminobenzoates; D000627:Aminophenols; D000813:Anilides; D000900:Anti-Bacterial Agents; D011083:Polycyclic Compounds; C543969:platencin A1; D000218:Adamantane; C510909:platensimycin; C520340:platencin