title: 2-Phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives as new inhibitors of bacterial cell wall biosynthesis.
abstract: Twenty-five 2-phenyl-5,6-dihydro-2H-thieno[3,2-c]pyrazol-3-ol derivatives were synthesized for evaluation as new inhibitors of bacterial cell wall biosynthesis. Many of them demonstrated good inhibitory activity against Staphylococcus aureus MurB, MurC and MurD enzymes in vitro and antimicrobial activity against gram-positive bacteria including MRSA, VRE and PRSP. However, when they were tested in the presence of 4% bovine serum albumin, the MIC values increased to greater than 128 microg/mL against PRSP. None of the compounds demonstrated activity against gram-negative bacteria at MIC <32 microg/mL.
authors.affiliation: Chemical Sciences and Infectious Diseases, Wyeth Research, Pearl River, NY 10965, USA.
authors.forename: Zhong
authors.initials: Z
authors.lastname: Li
authors.forename: Gerardo D
authors.initials: GD
authors.lastname: Francisco
authors.forename: William
authors.initials: W
authors.lastname: Hu
authors.forename: Pornpen
authors.initials: P
authors.lastname: Labthavikul
authors.forename: Peter J
authors.initials: PJ
authors.lastname: Petersen
authors.forename: Anatoly
authors.initials: A
authors.lastname: Severin
authors.forename: Guy
authors.initials: G
authors.lastname: Singh
authors.forename: Youjun
authors.initials: Y
authors.lastname: Yang
authors.forename: Beth A
authors.initials: BA
authors.lastname: Rasmussen
authors.forename: Yang-I
authors.initials: YI
authors.lastname: Lin
authors.forename: Jerauld S
authors.initials: JS
authors.lastname: Skotnicki
authors.forename: Tarek S
authors.initials: TS
authors.lastname: Mansour
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002473:Cell Wall / Q000187:drug effects / Q000378:metabolism*; D024881:Drug Resistance, Bacterial; D005798:Genes, Bacterial / Q000235:genetics; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D013211:Staphylococcus aureus / Q000187:drug effects / Q000201:enzymology / Q000378:metabolism*
chemical_list: D000900:Anti-Bacterial Agents