Pyrrolidine bis-cyclic guanidines with antimicrobial activity against drug-resistant Gram-positive pathogens identified from a mixture-based combinatorial library

Bioorganic and Medicinal Chemistry Letters

Volumn 16, Issue 19, 2006, Pages 5073-5079

  Hensler, Mary E ^a   Bernstein, Gregory ^a   Nizet, Victor ^a   Nefzi, Adel ^b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b TORREY PINES INSTITUTE FOR MOLECULAR STUDIES   (United States)

Author keywords

American Type Culture Collection; ATCC; Bactericidal activity; Combinatorial chemistry; MBC; methicillin resistant Staphylococcus aureus; Methicillin resistant Staphylococcus aureus; MIC; minimal bactericidal concentration; minimal inhibitory concentration; MRSA; Positional scanning; positional scanning synthetic combinatorial library; PS SCL; Pyrrolidine bis cyclic guanidine library; THA; THB; Todd Hewitt agar; Todd Hewitt broth; vancomycin resistant Enterococcus; VRE

Indexed keywords

CARBOXYLIC ACID; GUANIDINE DERIVATIVE; PYRROLIDINE DERIVATIVE; VANCOMYCIN;

ANTIBIOTIC RESISTANCE; ANTIBIOTIC SENSITIVITY; ANTIMICROBIAL ACTIVITY; ARTICLE; BACTERIAL INFECTION; BACTERICIDAL ACTIVITY; BACTERIOSTASIS; BACTERIUM IDENTIFICATION; COMBINATORIAL LIBRARY; CONTROLLED STUDY; DRUG ACTIVITY; DRUG POTENCY; DRUG SCREENING; DRUG SYNTHESIS; ENTEROCOCCAL INFECTION; ENTEROCOCCUS FAECALIS; GRAM NEGATIVE BACTERIUM; GRAM POSITIVE BACTERIUM; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; MINIMUM INHIBITORY CONCENTRATION; NONHUMAN; SOLID PHASE SYNTHESIS; STAPHYLOCOCCUS INFECTION;

ANTI-BACTERIAL AGENTS; COMBINATORIAL CHEMISTRY TECHNIQUES; DRUG RESISTANCE; ENTEROCOCCUS FAECALIS; GRAM-POSITIVE BACTERIA; GUANIDINES; HUMANS; METHICILLIN; PYRROLIDINES; STAPHYLOCOCCUS AUREUS; STRUCTURE-ACTIVITY RELATIONSHIP; VANCOMYCIN;

BACTERIA (MICROORGANISMS); ENTEROCOCCUS FAECALIS; METHICILLIN RESISTANT STAPHYLOCOCCUS AUREUS; NEGIBACTERIA; POSIBACTERIA;

EID: 33747376908     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2006.07.037     Document Type: Article

References (20)

1. Miller L.G., Perdreau-Remington F., Rieg G., Mehdi S., Perlroth J., Bayer A.S., Tang A.W., Phung T.O., and Spellberg B. N. Engl. J. Med. 352 (2005) 1445
2. Koleff M.H., and Micek S.T. Curr. Opin. Infect. Dis. 19 (2006) 161
3. Appelbaum P.C. Clin. Microbiol. Infect. 12 Suppl. 2 (2006) 3
4. National Nosocomial Infections Surveillance (NNIS) System Report: data summary from January 1992 through June 2004, issued October 2004. Am. J. Infect. Control 2004, 32, 470.
5. Nefzi A., Ostresh J.M., Yu J., and Houghten R.A. J. Org. Chem. 69 (2004) 3603
6. Appel J.R., Johnson J., Narayanan V.L., and Houghten R.A. Mol. Divers. 4 (1998-1999) 91
7. Dooley C.T., and Houghten R.A. Life Sci. 52 (1993) 1509
8. Blondelle S.E., and Houghten R.A. Trends Biotechnol. 14 (1996) 60
9. Houghten R.A., Pinilla C., Appel J.R., Blondelle S.E., Dooley C.T., Eichler J., Nefzi A., and Ostresh J.M. J. Med. Chem. 42 (1999) 3743
10. Merrifield R.B. J. Am. Chem. Soc. 85 (1963) 2149
11. Merrifield R.B. Science 232 (1986) 341
12. Ostresh J.M., Schoner C.C., Hamashin V.T., Nefzi A., Meyer J.-P., and Houghten R.A. J. Org. Chem. 63 (1998) 8622
13. Nefzi A., Ostresh J.M., and Houghten R.A. Tetrahedron 55 (1999) 335
14. Pinilla C., Appel J.R., Blanc P., and Houghten R.A. Biotechniques 13 (1992) 901
15. Martin D.W., Schurr M.J., Mudd M.H., Govan J.R., Holloway B.W., and Deretic V. Proc. Natl. Acad. Sci. U.S.A. 90 (1993) 8377
16. Chandrasekaran S., and Nagarajan S. Farmaco 60 (2005) 279
17. Amir M., Aggrawal R., and Javed S.A. Oriental J. Chem. 20 (2004) 477
18. Balasankar T., and Nagarajan S. Heterocycl. Commun. 10 (2004) 451
19. Yang S.-W., Chan T.-M., Pomponi S.A., Chen G., Wright A.E., Patel M., Gullo V., Pramanik B., and Chu M. J. Antibiot. 56 (2003) 970
20. Li C., Lewis M.R., Gilbert A.B., Noel M.D., Scoville D.H., Allman G.W., and Savage P.B. Antimicrob. Agents Chemother. 43 (1999) 1347