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Chemical Compound Review

AC1LAQXU     10-thia-7,9- diazabicyclo[4.4.0]deca- 1,3,5...

Synonyms: SureCN205451, SureCN205452, AG-K-79621, CTK0J3994, 255-18-5, ...
 
 
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Disease relevance of Benzothiadiazine

  • However, AMPA receptor activation contributes to CA1 hippocampal neuron damage from global ischemia in rodents, raising the possibility that 7-chloro-3-methyl-3-4-dihydro-2H-1,2,4 benzothiadiazine S,S-dioxide (IDRA 21) or drugs with similar actions may worsen ischemic neuronal injury [1].
  • Benzothiadiazine diuretic agents and beta-adrenergic receptor-blocking drugs are two of the main groups of drugs used to treat mild hypertension [2].
  • Novel potential agents for human cytomegalovirus infection: synthesis and antiviral activity evaluation of benzothiadiazine dioxide acyclonucleosides [3].
  • Resistance profile of a hepatitis C virus RNA-dependent RNA polymerase benzothiadiazine inhibitor [4].
  • Photoinduced genotoxicity of benzothiadiazine diuretics was studied with regard to mutagenic and lambda prophage-inducing activities in E. coli [5].
 

High impact information on Benzothiadiazine

  • The SUR2 segment containing the 12th through 17th predicted transmembrane domains, TMD12-17, confers sensitivity to the benzopyran, cromakalim, and the pyridine, pinacidil, whereas an SUR1 segment which includes TMD6-11 and the first nucleotide-binding fold, NBF1, controls responsiveness to the benzothiadiazine, diazoxide [6].
  • In this work we report the selection of replicons resistant to inhibition by the benzothiadiazine class of NNIs [7].
  • Additionally, cross-resistance studies and synergistic inhibition of the enzyme by combinations of a benzimidazole and a benzothiadiazine indicate the existence of nonoverlapping binding sites for these two structural classes of inhibitors [7].
  • Those compounds, structurally related to previously described potassium channel openers such as the benzothiadiazine dioxide BPDZ 73, were tested as putative K(ATP) channel activators on the pancreatic endocrine tissue and on the vascular smooth muscle tissue [8].
  • Benzothiadiazine 16, although less potent at PDE 7 (IC(50) = 25 microM), also showed a trend of selectivity toward PDE 3 and PDE 4 [9].
 

Chemical compound and disease context of Benzothiadiazine

 

Biological context of Benzothiadiazine

 

Anatomical context of Benzothiadiazine

 

Gene context of Benzothiadiazine

 

Analytical, diagnostic and therapeutic context of Benzothiadiazine

References

  1. The diazoxide derivative IDRA 21 enhances ischemic hippocampal neuron injury. Yamada, K.A., Covey, D.F., Hsu, C.Y., Hu, R., Hu, Y., He, Y.Y. Ann. Neurol. (1998) [Pubmed]
  2. Diuretic agents and beta-blockers in the treatment of hypertension. Dollery, C. Hypertension (1989) [Pubmed]
  3. Novel potential agents for human cytomegalovirus infection: synthesis and antiviral activity evaluation of benzothiadiazine dioxide acyclonucleosides. Martinez, A., Esteban, A.I., Castro, A., Gil, C., Conde, S., Andrei, G., Snoeck, R., Balzarini, J., De Clercq, E. J. Med. Chem. (1999) [Pubmed]
  4. Resistance profile of a hepatitis C virus RNA-dependent RNA polymerase benzothiadiazine inhibitor. Nguyen, T.T., Gates, A.T., Gutshall, L.L., Johnston, V.K., Gu, B., Duffy, K.J., Sarisky, R.T. Antimicrob. Agents Chemother. (2003) [Pubmed]
  5. Arginine reversion and lambda induction in E. coli with benzothiadiazine diuretics irradiated with near-ultraviolet light. Fujita, H. Mutat. Res. (1985) [Pubmed]
  6. Pharmaco-topology of sulfonylurea receptors. Separate domains of the regulatory subunits of K(ATP) channel isoforms are required for selective interaction with K(+) channel openers. Babenko, A.P., Gonzalez, G., Bryan, J. J. Biol. Chem. (2000) [Pubmed]
  7. Characterization of the inhibition of hepatitis C virus RNA replication by nonnucleosides. Tomei, L., Altamura, S., Bartholomew, L., Bisbocci, M., Bailey, C., Bosserman, M., Cellucci, A., Forte, E., Incitti, I., Orsatti, L., Koch, U., De Francesco, R., Olsen, D.B., Carroll, S.S., Migliaccio, G. J. Virol. (2004) [Pubmed]
  8. Effect on K(ATP) channel activation properties and tissue selectivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides. Boverie, S., Antoine, M.H., Somers, F., Becker, B., Sebille, S., Ouedraogo, R., Counerotte, S., Pirotte, B., Lebrun, P., de Tullio, P. J. Med. Chem. (2005) [Pubmed]
  9. Benzyl derivatives of 2,1,3-benzo- and benzothieno[3,2-a]thiadiazine 2,2-dioxides: first phosphodiesterase 7 inhibitors. Martínez, A., Castro, A., Gil, C., Miralpeix, M., Segarra, V., Doménech, T., Beleta, J., Palacios, J.M., Ryder, H., Miró, X., Bonet, C., Casacuberta, J.M., Azorín, F., Piña, B., Puigdoménech, P. J. Med. Chem. (2000) [Pubmed]
  10. Inhibitors of HCV NS5B polymerase: synthesis and structure-activity relationships of N-1-benzyl and N-1-[3-methylbutyl]-4-hydroxy-1,8-naphthyridon-3-yl benzothiadiazine analogs containing substituents on the aromatic ring. Rockway, T.W., Zhang, R., Liu, D., Betebenner, D.A., McDaniel, K.F., Pratt, J.K., Beno, D., Montgomery, D., Jiang, W.W., Masse, S., Kati, W.M., Middleton, T., Molla, A., Maring, C.J., Kempf, D.J. Bioorg. Med. Chem. Lett. (2006) [Pubmed]
  11. Vasodilators in the treatment of hypertension. Kincaid-Smith, P. Med. J. Aust. (1975) [Pubmed]
  12. Suppression of human tumor cell proliferation through mitochondrial targeting. Holmuhamedov, E., Lewis, L., Bienengraeber, M., Holmuhamedova, M., Jahangir, A., Terzic, A. FASEB J. (2002) [Pubmed]
  13. Effects of the benzothiadiazine TAG on channel activation at mammalian glycine receptors. Mathers, D.A. Neurosci. Lett. (1993) [Pubmed]
  14. Effects of a new benzothiadiazine derivative, LN 5330, on insulin secretion. Blayac, J.P., Ribes, G., Buys, D., Puech, R., Loubatieres-Mariani, M.M. Archives internationales de pharmacodynamie et de thérapie. (1981) [Pubmed]
  15. Effect of LN 5330 on insulin release and calcium uptake by isolated rat islets of Langerhans. Comparison with diazoxide. Manteghetti, M., Puech, R., Ribes, G., Blayac, J.P., Loubatieres-Mariani, M.M. Archives internationales de pharmacodynamie et de thérapie. (1984) [Pubmed]
  16. Synthesis, biological evaluation and molecular modelling studies on benzothiadiazine derivatives as PDE4 selective inhibitors. Tait, A., Luppi, A., Hatzelmann, A., Fossa, P., Mosti, L. Bioorg. Med. Chem. (2005) [Pubmed]
  17. Effect of benzothiadiazine derivatives on cyclic nucleotide phosphodiesterase and on the tension of the aortic strip. Vulliemoz, Y., Verosky, M., Triner, L. Blood vessels. (1980) [Pubmed]
  18. Enantiomers of benzothiadiazine diuretics by direct chromatographic resolution of the racemic drugs. Blaschke, G., Maibaum, J. Journal of pharmaceutical sciences. (1985) [Pubmed]
  19. Semiaqueous potentiometric determinations of apparent pKa1 values for benzothiadiazines and detection of decomposition during solubility variation with pH studies. Hennig, U.G., Moskalyk, R.E., Chatten, L.G., Chan, S.F. Journal of pharmaceutical sciences. (1981) [Pubmed]
 
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