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Chemical Compound Review

Thiadiazole     thiadiazole

Synonyms: SureCN24198, SureCN973070, AG-K-07285, CHEBI:39468, KST-1B2803, ...
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Disease relevance of thiadiazole


High impact information on thiadiazole

  • A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations [2].
  • Mass spectrometric experiments on the complex between an irreversible compound belonging to the thiadiazole family and the plant enzyme identified Cys498 as the binding site of the inhibitor [6].
  • Routine screening of compounds for inhibition of collagen-induced platelet aggregation in vitro revealed 4,5-bis-(4-methoxyphenyl)-1,2,3-thiadiazole (2) was active and it represents the first example of a 1,2,3-thiadiazole with possible antithrombotic activity [7].
  • Nitrogen atoms in the thiadiazole moiety make specific hydrogen bond interactions with enzyme structural elements that are conserved across all enzymes in the matrix metalloproteinase class [8].
  • The products obtained are oxovanadium(V) compounds [VOL(L(cyclic))] (L = L(1), 1a, and L(2), 1b) that contain one molecule of ligand which undergoes metal-induced cyclization to form a thiadiazole ring [9].

Chemical compound and disease context of thiadiazole


Biological context of thiadiazole


Anatomical context of thiadiazole


Associations of thiadiazole with other chemical compounds


Gene context of thiadiazole


Analytical, diagnostic and therapeutic context of thiadiazole

  • 2. To clarify the mechanism of SCH-202676 action, we used the functional approach of [35S]GTPgammaS autoradiography with rat brain cryostat sections together with classical membrane [35S]GTPgammaS binding assays to evaluate how the thiadiazole affects G protein activity mediated by various receptors linked to the Gi-family of G proteins [22].
  • Structure-related effect of pH on the bioassay sensitivity of five thiadiazole cephalosporins (a note) [23].


  1. Thiadiazole derivatives: highly potent and specific HIV-1 reverse transcriptase inhibitors. Hanasaki, Y., Watanabe, H., Katsuura, K., Takayama, H., Shirakawa, S., Yamaguchi, K., Sakai, S., Ijichi, K., Fujiwara, M., Konno, K. J. Med. Chem. (1995) [Pubmed]
  2. A molecular basis for the selectivity of thiadiazole urea inhibitors with stromelysin-1 and gelatinase-A from generalized born molecular dynamics simulations. Rizzo, R.C., Toba, S., Kuntz, I.D. J. Med. Chem. (2004) [Pubmed]
  3. The activity of a thiadiazole on Mycobacterium leprae. Levy, L. Proc. Soc. Exp. Biol. Med. (1976) [Pubmed]
  4. Investigation of anticancer mechanism of thiadiazole-based compound in human non-small cell lung cancer A549 cells. Chou, J.Y., Lai, S.Y., Pan, S.L., Jow, G.M., Chern, J.W., Guh, J.H. Biochem. Pharmacol. (2003) [Pubmed]
  5. Thiadiazole derivatives: highly potent and selective inhibitors of human immunodeficiency virus type 1 (HIV-1) replications in vitro. Fujiwara, M., Ijichi, K., Hanasaki, Y., Ide, T., Katsuura, K., Takayama, H., Aimi, N., Shigeta, S., Konno, K., Yokota, T., Baba, M. Microbiol. Immunol. (1997) [Pubmed]
  6. Kinetic and mass spectrometric analyses of the interactions between plant acetohydroxy acid isomeroreductase and thiadiazole derivatives. Halgand, F., Vives, F., Dumas, R., Biou, V., Andersen, J., Andrieu, J.P., Cantegril, R., Gagnon, J., Douce, R., Forest, E., Job, D. Biochemistry (1998) [Pubmed]
  7. Synthesis and platelet aggregation inhibitory activity of 4,5-bis(substituted)-1,2,3-thiadiazoles. Thomas, E.W., Nishizawa, E.E., Zimmermann, D.C., Williams, D.J. J. Med. Chem. (1985) [Pubmed]
  8. Structural characterizations of nonpeptidic thiadiazole inhibitors of matrix metalloproteinases reveal the basis for stromelysin selectivity. Finzel, B.C., Baldwin, E.T., Bryant, G.L., Hess, G.F., Wilks, J.W., Trepod, C.M., Mott, J.E., Marshall, V.P., Petzold, G.L., Poorman, R.A., O'Sullivan, T.J., Schostarez, H.J., Mitchell, M.A. Protein Sci. (1998) [Pubmed]
  9. Oxovanadium(V) and cobalt(III) complexes of dithiocarbazate-based Schiff base ligands: formation of a thiadiazole ring by vanadium-induced cyclization of the coordinated ligand. Dutta, S.K., Samanta, S., Ghosh, D., Butcher, R.J., Chaudhury, M. Inorganic chemistry. (2002) [Pubmed]
  10. Characterization of human immunodeficiency virus type 1 strains resistant to the non-nucleoside reverse transcriptase inhibitor RD4-2217. Fujiwara, M., Kodama, E.N., Okamoto, M., Tokuhisa, K., Ide, T., Hanasaki, Y., Katsuura, K., Takayama, H., Aimi, N., Mitsuya, H., Shigeta, S., Konno, K., Yokota, T., Baba, M. Antivir. Chem. Chemother. (1999) [Pubmed]
  11. Effect of nanonization on absorption of 301029: ex vivo and in vivo pharmacokinetic correlations determined by liquid chromatography/mass spectrometry. Jia, L., Wong, H., Cerna, C., Weitman, S.D. Pharm. Res. (2002) [Pubmed]
  12. A fluorescence resonance energy transfer method for measuring the binding of inhibitors to stromelysin. Epps, D.E., Mitchell, M.A., Petzold, G.L., VanDrie, J.H., Poorman, R.A. Anal. Biochem. (1999) [Pubmed]
  13. Exploring 3D-QSAR of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists+. Bhattacharya, P., Leonard, J.T., Roy, K. Journal of molecular modeling (Online) (2005) [Pubmed]
  14. Anti-HIV-1 activity of thiadiazole derivatives: structure-activity relationship, reverse transcriptase inhibition, and lipophilicity. Ijichi, K., Fujiwara, M., Nagano, H., Matsumoto, Y., Hanasaki, Y., Ide, T., Katsuura, K., Takayama, H., Shirakawa, S., Aimi, N., Shigeta, S., Konno, K., Matsushima, M., Yokota, T., Baba, M. Antiviral Res. (1996) [Pubmed]
  15. Ligand design for alpha1 adrenoceptor subtype selective antagonists. Bremner, J.B., Coban, B., Griffith, R., Groenewoud, K.M., Yates, B.F. Bioorg. Med. Chem. (2000) [Pubmed]
  16. Localization of carbonic anhydrase in living osteoclasts with bodipy 558/568-modified acetazolamide, a thiadiazole carbonic anhydrase inhibitor. Brubaker, K.D., Mao, F., Gay, C.V. J. Histochem. Cytochem. (1999) [Pubmed]
  17. Cu(II)- and Hg(II)-induced modulation of the fluorescence behavior of a redox-active sensor molecule. Hennrich, G., Walther, W., Resch-Genger, U., Sonnenschein, H. Inorganic chemistry. (2001) [Pubmed]
  18. Synthesis and biological properties of new 1beta-methylcarbapenems containing heteroaromatic thioether moiety. Shin, K.J., Koo, K.D., Yoo, K.H., Kang, Y.K., Park, S.W., Kim, D.J. Bioorg. Med. Chem. Lett. (2001) [Pubmed]
  19. Exploring QSAR of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists using FA and GFA techniques. Bhattacharya, P., Leonard, J.T., Roy, K. Bioorg. Med. Chem. (2005) [Pubmed]
  20. High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor. Modica, M., Santagati, M., Santagati, A., Russo, F., Cagnotto, A., Goegan, M., Mennini, T. Bioorg. Med. Chem. Lett. (2000) [Pubmed]
  21. Synthesis of some new 2-methyl-4-(substituted benzylidene)1-phenyl-1,2,4 triazolo (3,4,-b) 1,4,5 thiadiazole as potential AChE inhibitory agents. Sen, S., Shanker, K. Bollettino chimico farmaceutico. (1996) [Pubmed]
  22. The 'allosteric modulator' SCH-202676 disrupts G protein-coupled receptor function via sulphydryl-sensitive mechanisms. Lewandowicz, A.M., Vepsäläinen, J., Laitinen, J.T. Br. J. Pharmacol. (2006) [Pubmed]
  23. Structure-related effect of pH on the bioassay sensitivity of five thiadiazole cephalosporins (a note). Uri, J.V. Acta Microbiol. Hung. (1985) [Pubmed]
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