Copyright (c) 2013 AJC
This work is licensed under a Creative Commons Attribution 4.0 International License.
Synthesis and Antifungal Activity of Some Thiazole Derivatives
Corresponding Author(s) : Geng-Liang Yang
Asian Journal of Chemistry,
Vol. 25 No. 4 (2013): Vol 25 Issue 4
Abstract
A series of some thiazole derivatives were designed and synthesized. The structure of newly synthesized compounds was characterized by HRMS, 1H NMR and 13C NMR. The synthesized compounds were evaluated against ten species of fungi in vitro by agar cup plate and micro-titration methods, respectively. The results of antifungal screening reveal that among all the compounds screened three compounds showed moderate antifungal activity. The MIC value of 3 h against two fungal strains C. neoformans and C. albicas is 8 μg mL-1 respectively. The MIC value of 3i against two fungal strains C. neoformans and T. mentagrophytes is 8 μg mL-1 and 16 μg mL-1, respectively and 3a against T. mentagrophytes is 16 μg mL-1, the MIC of others are all beyond 32 μg mL-1.
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- M. Wang, L.F. Wang, Y.Z. Li, Q.X. Li, Z.D. Xu and D.M. Qu, Transition Met. Chem., 26, 307 (2001).
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M. Wang, L.F. Wang, Y.Z. Li, Q.X. Li, Z.D. Xu and D.M. Qu, Transition Met. Chem., 26, 307 (2001).
K. Tsuji and H. Ishikawa, Bioorg. Med. Chem. Lett., 4, 1601 (1994).
K.J. Wilson, C.R. Illig, N. Subasinghe, J.B. Hoffman, M.J. Rudolph, R. Soll, C.J. Molloy, R. Bone, D. Green, T. Randall, M. Zhang, F.A. Lewandowski, Z. Zhou, C. Sharp, D. Maguire, B. Grasberger, R.L. DesJarlais and J. Spurlino, Bioorg. Med. Chem. Lett., 11, 915 (2001).
F. Haviv, J.D. Ratajczyk, R.W. DeNet, F.A. Kerdesky, R.L. Walters, S.P. Schmidt, J.H. Holms, P.R. Young and G.W. Carter, J. Med. Chem., 31, 1719 (1988).
W.C. Patt, H.W. Hamilton, M.D. Taylor, M.J. Ryan, D.G. Taylor Jr., C.J. Connolly, A.M. Doherty, S.R. Klutchko and I. Sircar, J. Med. Chem. 35, 2562 (1992).
F.W. Bell, A.S. Cantrell, M. Hoegberg, S.R. Jaskunas, N.G. Johansson, C.L. Jordan, M.D. Kinnick, P. Lind and J.M. Morin, J. Med. Chem., 38, 4929 (1995).
(a) X.H. Gu, X.Z. Wan and B. Jiang, Bioorg. Med. Chem. Lett., 9, 569 (1999); (b) B. Jiang and X.H. Gu, Bioorg. Med. Chem., 8, 363 (2000).
(a) Y. Kumar, R. Green, K.Z. Borysko, D.S. Wise, L.L. Wotring and L.B. Townsend, J. Med. Chem., 36, 3843 (1993); (b) Y. Kumar, R. Green, D.S. Wise, L.L. Wotring and L.B. Townsend, J. Med. Chem., 36, 3849 (1993).
H. Nakazumi, T. Ueyama and T. Kitao, J. Heterocycl. Chem., 1, 193 (1984).
T.A. Nakib, V. Bezjak and M.J. Meegan, Eur. J. Med. Chem., 5, 455 (1990).
S. Bondock and M.A. Metwally, J. Sulfur Chem., 29, 623 (2008).
P. Karegoudar, M.S. Karthikeyan, D.J. Prasad, M. Mahalinga, B.S. Holla and N.S. Kumari, Eur. J. Med. Chem., 43, 261 (2008).
M. Schmidt, J. Ungvári, J. Glöde, B. Dobnerc and A. Langner, Bioorg. Med. Chem., 15, 2283 (2007).
S. Wagle, A.V. Adhikari and N.S. Kumari, Phosphorus Sulfur Silicon Rel. Elem., 183, 1285 (2008).
X.F. Zhu and D.Q. Shi, Phosphorus Sulfur Silicon Rel. Elem., 183, 2020 (2008).