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Screening and Evaluation In Vitro

  • Robert F. Wilson
  • John F. Ryley
Part of the Handbook of Experimental Pharmacology book series (HEP, volume 96)

Abstract

In any large-scale programme aimed at drug discovery, screening procedures will be necessary in order to identify compounds of potential interest. Candidate substances for screening may include chemical compounds selected at random or according to particular structural features from an existing chemical collection, compounds designed and synthesised specifically by project chemists and broths or extracts of natural product origin. The purpose of an antifungal screen is simply to provide a yes/no answer to the question, ‘Is there sufficient interaction between this sample and fungi to warrant further investigation?’ This further investigation of compounds of potential interest is termed evaluation.

Keywords

Antifungal Agent Azole Antifungal Agar Diffusion Assay Torulopsis Glabrata Multipoint Inoculator 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. Beggs WH, Hughes CE (1987) Exploitation of the direct cell damaging action of antifungal azoles. Diag Microbiol Infect Dis 6: 1–3CrossRefGoogle Scholar
  2. Boyle FT, Ryley JF, Wilson RG (1987) In vitro-in vivo correlations with azole antifungals. In: Fromtling RA (ed) Recent trends in the discovery, development and evaluation of antifungal agents. J R Prous, Barcelona, pp S1:31–S1:41Google Scholar
  3. Clayton YM (1987) The in vitro activity of terbinafine against uncommon fungal pathogens. In: Fromtling RA (ed) Recent trends in the discovery, development and evaluation of antifungal agents. J R Prous, Barcelona, pp 433–439Google Scholar
  4. Drouhet E (1988) Standardization of antifungal susceptibility testing. An introductory overview. Proc Xth ISHAM Congress, Barcelona, pp 203–209Google Scholar
  5. Dupont B, Drouhet E (1979) In vitro synergy and antagonism of antifungal agents against yeast-like fungi. Postgrad Med J 55: 683–686PubMedCrossRefGoogle Scholar
  6. Galgiani JN (1986) Antifungal susceptibility testing: recent findings and experience. Antimicrobic Newsletter 3: 17–22CrossRefGoogle Scholar
  7. Galgiani JN (1987a) Antifungal susceptibility tests. Antimicrob Agents Chemother 31: 1867–1870PubMedGoogle Scholar
  8. Galgiani JN (1987b) The need for improved standardization in antifungal susceptibility testing. In: Fromtling RA (ed) Recent trends in the discovery, development and evaluation of antifungal agents. J R Prous, Barcelona, pp 15–24Google Scholar
  9. Guinet R, Nerson D, De Closets F, Dupouy-Camet J, Kures L, Marjollet M, Poirot JL, Ross A, Texier-Maugein J, Voile PJ (1988) Collaborative evaluation in seven laboratories of a standardized micromethod for yeast susceptibility testing. J Clin Microbiol 26: 2307–2312PubMedGoogle Scholar
  10. Minagawa H, Kitaura K, Nakamizo N (1983) Effects of pH on the activity of ketoconazole against Candida albicans. Antimicrob Agents Chemother 23: 105–107PubMedGoogle Scholar
  11. Odds FC (1982) Interactions among amphotericin B, 5-fluorocytosine, ketoconazole, and miconazole against pathogenic fungi in vitro. Antimicrob Agents Chemother 22: 763–770PubMedGoogle Scholar
  12. Odds FC (1985) Laboratory tests for the activity of imidazole and triazole antifungal agents in vitro. Semin Dermatol 4: 260–270Google Scholar
  13. Odds FC, Abbott AB (1984) Relative inhibition factors — a novel approach to the assessment of antifungal antibiotics in vitro. J Antimicrob Chemother 13: 31–43PubMedCrossRefGoogle Scholar
  14. Odds FC, Webster CE, Abbott AB (1984) Antifungal relative inhibition factors: BAY 1-9139, bifonazole, butoconazole, isoconazole, itraconazole (R 51211), oxicon- azole, Ro-14-4767/002, sulconazole, terconazole and vibunazole (BAY n-7133) compared in vitro with nine established antifungal agents. J Antimicrob Chemother 14: 105–114PubMedCrossRefGoogle Scholar
  15. Odds FC, Cockayne A, Hayward J, Abbott AB (1985) Effects of imidazoleand triazolederivative antifungal compounds on the growth and morphological development of Candida albicans hyphae. J Gen Microbiol 131: 2581–2589PubMedGoogle Scholar
  16. Odds FC, Abbott AB, Pye G, Troke PF (1986) Improved method for estimation of azole antifungal inhibitory concentrations against Candida species, based on azole/antibiotic interactions. J Med Vet Mycol 24: 305–311PubMedCrossRefGoogle Scholar
  17. Petranyi G, Meingassner JG, Mieth H (1987) Antifungal activity of the allylamine derivative terbinafine in vitro. Antimicrob Agents Chemother 31: 1365–1368PubMedGoogle Scholar
  18. Polak A, Dixon DM (1987) Antifungal activity of amorolfine (Ro 14-4767/002) in vitro and in vivo. In: Fromtling RA (ed) Recent trends in the discovery, development and evaluation of antifungal agents. J R Prous, Barcelona, pp 555–573Google Scholar
  19. Richardson K, Andrews RJ, Marriott MS, Tarbit MH, Troke PF (1986) Correlation of in vitro and in vivo activity of azole antifungals. In: Iwata K, Vanden Bossche H (eds) In vitro and in vivo evaluation of antifungal agents. Elsevier, Amsterdam, pp 147–149Google Scholar
  20. Rumler W, Heins S, Heins J (1984) Relations between the concentration and the contact-time in the antifungal activity of 5-flubrocytosine, bifonazole and BAY N 7133 to Candida albicans. Mykosen 27: 436–442PubMedGoogle Scholar
  21. Ryley JF, Rathmell WG (1984) Discovery of antifungal agents: in vitro and in vivo testing. In: Trinci APJ, Ryley JF (eds) Mode of action of antifungal agents. Cambridge University Press, Cambridge, pp 63–87 (Br My col Soc Symp No 9 )Google Scholar
  22. Ryley JF, Wilson RG, Gravestock MB, Poyser JP (1981) Experimental approaches to antifungal chemotherapy. Adv Pharmacol Chemother 18: 49–176PubMedCrossRefGoogle Scholar
  23. Ryley JF, Wilson RG, Barrett-Bee KJ (1984) Azole resistance in Candida albicans. Sabouraudia: J Med Vet Mycol 22: 53–63Google Scholar
  24. Scott EM, Gorman SP, Wright LR (1984) The effect of imidazoles on germination of arthrospores and microconidia of Trichophyton mentagrophytes. J Antimicrob Chemother 13: 101–110PubMedCrossRefGoogle Scholar
  25. Shadomy S (1987) Preclinical evaluation of antifungal agents: design of in vitro screens. In: Fromtling RA (ed) Recent trends in the discovery, development and evaluation of antifungal agents. J R Prous, Barcelona, pp S1:1–S1:10Google Scholar
  26. Shadomy S, Dixon DM, May R (1982) A comparison of bifonazole (BAY H 4502) with clotrimazole in vitro. Sabouraudia 20: 313–323PubMedCrossRefGoogle Scholar
  27. Shadomy S, Espinel-Ingroff A, Kerkering TM (1984) In-vitro studies with four new antifungal agents: BAY n 7133, bifonazole (BAY h 4502), ICI 153,066 and Ro 14-4767/002. Sabouraudia: J Med Vet Mycol 22: 7–15Google Scholar
  28. Sud IJ, Feingold DS (1981) Heterogeneity of action mechanisms among antimycotic imidazoles. Antimicrob Agents Chemother 20: 71–74PubMedGoogle Scholar
  29. Van Cutsem J, Van Gerven F, Janssen PAJ (1986) The in vitro evaluation of azoles. In: Iwata K, Vanden Bossche H (eds) In vitro and in vivo evaluation of antifungal agents. Elsevier, Amsterdam, pp 51–64Google Scholar
  30. Van Cutsem J, Van Gerven F, Janssen PAJ (1987) The in vitro and in vivo antifungal activity of itraconazole. In: Fromtling RA (ed) Recent trends in the discovery, development and evaluation of antifungal agents. J R Prous, Barcelona, pp 177–192Google Scholar
  31. Wilson RG (1985) Factors which affect the fungicidal activity of imidazoles and triazoles. IXth ISHAM Cong, Atlanta, Georgia, Abst Rl-9Google Scholar
  32. Wright LR, Scott EM, Gorman SP (1983) The sensitivity of mycelium, arthrospores and microconidia of Trichophyton mentagrophytes to imidazoles determined by in vitro tests. J Antimicrob Chemother 12: 317–327PubMedCrossRefGoogle Scholar
  33. Yamaguchi H, Hiratani T, Uchida K (1987) The in vitro activity and evaluation of bifonazole. In: Fromtling RA (ed) Recent trends in the discovery, development and evaluation of antifungal agents. J R Prous, Barcelona, pp 335–352Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1990

Authors and Affiliations

  • Robert F. Wilson
  • John F. Ryley

There are no affiliations available

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