Oxidosqualene cyclase inhibitors as antimicrobial agents

Jerald C. Hinshaw; Dae Yeon Suh; Philippe Garnier; Frederick S. Buckner; Richard T. Eastman; Seiichi P.T. Matsuda; Bridget M. Joubert; Isabelle Coppens; Keith A. Joiner; Salim Merali; Theodore E. Nash; Glenn D. Prestwich

doi:10.1021/jm034126t

Oxidosqualene cyclase inhibitors as antimicrobial agents

Jerald C. Hinshaw
, Dae Yeon Suh
, Philippe Garnier
, Frederick S. Buckner
, Richard T. Eastman
, Seiichi P.T. Matsuda
, Bridget M. Joubert
, Isabelle Coppens
, Keith A. Joiner
, Salim Merali
, Theodore E. Nash
, Glenn D. Prestwich

Research output: Contribution to journal › Article › peer-review

35 Scopus citations

Abstract

Small-molecule oxidosqualene cyclase (OSC) inhibitors were found to be effective in assays against cloned OSC-like enzymes from human pathogens. A combinatorial library was prepared and used to identify lead compounds that inhibit the growth of Trypanosoma cruzi, Leishmania mexicana amazonensis, and Pneumocystis carinii in culture. Selectivity for the microorganisms in preference to mammalian cells was observed.

Original language	English (US)
Pages (from-to)	4240-4243
Number of pages	4
Journal	Journal of Medicinal Chemistry
Volume	46
Issue number	20
DOIs	https://doi.org/10.1021/jm034126t
State	Published - Sep 25 2003
Externally published	Yes

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

Access to Document

10.1021/jm034126t

Cite this

@article{1620c09f38c845428a28313c752833ae,

title = "Oxidosqualene cyclase inhibitors as antimicrobial agents",

abstract = "Small-molecule oxidosqualene cyclase (OSC) inhibitors were found to be effective in assays against cloned OSC-like enzymes from human pathogens. A combinatorial library was prepared and used to identify lead compounds that inhibit the growth of Trypanosoma cruzi, Leishmania mexicana amazonensis, and Pneumocystis carinii in culture. Selectivity for the microorganisms in preference to mammalian cells was observed.",

author = "Hinshaw, \{Jerald C.\} and Suh, \{Dae Yeon\} and Philippe Garnier and Buckner, \{Frederick S.\} and Eastman, \{Richard T.\} and Matsuda, \{Seiichi P.T.\} and Joubert, \{Bridget M.\} and Isabelle Coppens and Joiner, \{Keith A.\} and Salim Merali and Nash, \{Theodore E.\} and Prestwich, \{Glenn D.\}",

year = "2003",

month = sep,

day = "25",

doi = "10.1021/jm034126t",

language = "English (US)",

volume = "46",

pages = "4240--4243",

journal = "Journal of Medicinal Chemistry",

issn = "0022-2623",

publisher = "American Chemical Society",

number = "20",

}

TY - JOUR

T1 - Oxidosqualene cyclase inhibitors as antimicrobial agents

AU - Hinshaw, Jerald C.

AU - Suh, Dae Yeon

AU - Garnier, Philippe

AU - Buckner, Frederick S.

AU - Eastman, Richard T.

AU - Matsuda, Seiichi P.T.

AU - Joubert, Bridget M.

AU - Coppens, Isabelle

AU - Joiner, Keith A.

AU - Merali, Salim

AU - Nash, Theodore E.

AU - Prestwich, Glenn D.

PY - 2003/9/25

Y1 - 2003/9/25

N2 - Small-molecule oxidosqualene cyclase (OSC) inhibitors were found to be effective in assays against cloned OSC-like enzymes from human pathogens. A combinatorial library was prepared and used to identify lead compounds that inhibit the growth of Trypanosoma cruzi, Leishmania mexicana amazonensis, and Pneumocystis carinii in culture. Selectivity for the microorganisms in preference to mammalian cells was observed.

AB - Small-molecule oxidosqualene cyclase (OSC) inhibitors were found to be effective in assays against cloned OSC-like enzymes from human pathogens. A combinatorial library was prepared and used to identify lead compounds that inhibit the growth of Trypanosoma cruzi, Leishmania mexicana amazonensis, and Pneumocystis carinii in culture. Selectivity for the microorganisms in preference to mammalian cells was observed.

UR - https://www.scopus.com/pages/publications/0141457812

UR - https://www.scopus.com/pages/publications/0141457812#tab=citedBy

U2 - 10.1021/jm034126t

DO - 10.1021/jm034126t

M3 - Article

C2 - 13678402

AN - SCOPUS:0141457812

SN - 0022-2623

VL - 46

SP - 4240

EP - 4243

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

IS - 20

ER -

Oxidosqualene cyclase inhibitors as antimicrobial agents

Abstract

ASJC Scopus subject areas

Access to Document

Other files and links

Fingerprint

Cite this