Synthesis and antifungal activities of novel 1,3-β-D-glucan synthase inhibitors. Part 2

Bioorganic and Medicinal Chemistry Letters

Volumn 11, Issue 10, 2001, Pages 1273-1276

  Masubuchi, Kazunao ^a   Okada, Takehiro ^a   Kohchi, Masami ^a   Murata, Takeshi ^a   Tsukazaki, Masao ^a   Kondoh, Osamu ^a   Yamazaki, Toshikazu ^a   Satoh, Yasuko ^a   Ono, Yoshinori ^a   Tsukaguchi, Toshiyuki ^a   Kobayashi, Kazuko ^a   Ono, Naomi ^a   Inoue, Tomoaki ^a   Horii, Ikuo ^a   Shimma, Nobuo ^a  

^a NIPPON ROCHE RESEARCH CENTER   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

1,3 BETA DEXTRO GLUCAN SYNTHASE INHIBITOR; ANIDULAFUNGIN; ANTIFUNGAL AGENT; CASPOFUNGIN; ENZYME INHIBITOR; FR 901469; RO 09 3655; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIFUNGAL ACTIVITY; ARTICLE; CANDIDIASIS; CHEMICAL MODIFICATION; CONTROLLED STUDY; CULTURE MEDIUM; DEUTEROMYCETES; DRUG ISOLATION; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; LIVER TOXICITY; LUNG ASPERGILLOSIS; MOUSE; NONHUMAN; SPECIES DIFFERENCE; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTIFUNGAL AGENTS; ASPERGILLOSIS, ALLERGIC BRONCHOPULMONARY; ASPERGILLUS FUMIGATUS; CANDIDA; CANDIDIASIS; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; GLUCOSYLTRANSFERASES; IMMUNOCOMPROMISED HOST; INCLUSION BODIES; INJECTIONS, INTRAVENOUS; MEMBRANE PROTEINS; MICE; MICROBIAL SENSITIVITY TESTS; MITOSPORIC FUNGI; PEPTIDES, CYCLIC; SCHIZOSACCHAROMYCES POMBE PROTEINS; TIME FACTORS;

EID: 0035927219     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(01)00178-0     Document Type: Article

References (12)

1. Willis E.A., Redinbo M.R., Perfect J.R., Poeta M.D. Emerging Therapeutic Agents. 4:2000;265.
2. The isolation and structure elucidation of compounds 1-3 will be reported elsewhere.
3. Fujie A., Iwamoto T., Muramatsu T., Okudaira T., Nitta K., Nakanishi T., Sakamoto K., Hori Y., Hino M., Hashimoto S., Okuhara M. J. Antibiot. 53:2000;912.
4. Fujie A., Iwamoto T., Muramatsu T., Okudaira T., Sato I., Furuta T., Tsurumi Y., Hori Y., Hino M., Hashimoto S., Okuhara M. J. Antibiot. 53:2000;920.
5. Barrett, D.; Tanaka, A.; Harada, K.; Ohki, H.; Kawabata, K.; Takasugi, H.; Watabe, E.; Maki, K.; Ikeda, F.; Sakane, K. Abstracts of the 19th Symposium on Medicinal Chemistry, 8th Annual Meeting of Division of Medicinal Chemistry, Abstract No. 2P-14, Nov 11-14, 1999, Tokyo, Japan.
6. Masubuchi K., Okada T., Kohchi M., Sakaitani M., Mizuguchi E., Shirai H., Aoki M., Watanabe T., Kondoh O., Yamazaki T., Satoh Y., Kobayashi K., Inoue T., Horii I., Shimma N. Bioorg. Med. Chem. Lett. 11:2001;395.
7. A histopathological examination of 1 after a 2-week treatment revealed inclusion-body formation and single cell necrosis in hepatocytes.
8. Carpino L.A., El-Faham A., Albericio F. J. Org. Chem. 60:1995;3561.
9. Irifune K., Shimoguchi K., Tateda K., Yamaguchi K., Hara K. Igaku no Ayumi. 152:1990;71.
10. For in vitro antifungal activity of MK-0991: Bartizal K., Gill C.J., Abruzzo G.K., Flattery A.M., Kong L., Scott P.M., Smith J.G., Leighton C.E., Bouffard A., Dropinski J.F., Balkovec J. Antimicrob. Agents Chemother. 41:1997;2326.
11. For in vivo antifungal activity of MK-0991 in disseminated aspergillosis: Abruzzo G.K., Flattery A.M., Gill C.J., Kong L., Smith J.G., Pikounis V.B., Balkovec J.M., Bouffard A.F., Dropinski J.F., Rosen H., Kropp H., Bartizal K. Antimicrob. Agents Chemother. 41:1997;2333.
12. Debono M., Turner W.W., LaGrandeur L., Burkhardt F.J., Nissen J.S., Nichols K.K., Rodriguez M.J., Zweifel M.J., Zeckner D.J., Gordee R.S., Tang J., Parr T.R. Jr. J. Med. Chem. 38:1995;3271.