New Isothioureas: Synthesis and Activities
829
The complete genome sequence of Escherichia coli K-12.
Science, 277, 1453-1462 (1997).
Castano, T., Encinas, A., Perez, C., Castro, A., Campilo, N. E.,
and Gil, C., Design, synthesis, and evaluation of potential
inhibitors of nitric oxide synthase. Bioorg. Med. Chem., 16,
6193-6206 (2008).
315-322 (2003).
Jin, G. H., Lee, D. Y., Cheon, Y. J., Gim, H. J., Kim D. H., Kim,
H. D., Ryu, J. H., and Jeon, R., Synthesis of phenyliso-
thiourea derivatives as inhibitors of NO production in
LPS activated macrophages. Bioorg. Med. Chem. Lett., 19,
3088-3092 (2009).
Cedillo-Rivera, R. and Munoz, O., In vitro susceptibility of
Giardia lamblia to albendazole, mebendazole and other
chemotherapeutic agents. J. Med. Microbiol., 37, 221-224
(1992).
Kada, T., Hirano, K., and Shirasu, Y., Bacillus subtilis rec-
assay test. In de Sevres, F. E. and Hollaender, A. (Eds.).
Chemical Mutagens, vol. 6, Plenum Press, New York, pp.
149, (1980).
Cedillo-Rivera, R., Tapia-Contreras, A., Torres, J., and Munoz,
O., In vitro susceptibility of Entamoeba histolytica to
fluoroquinolones, nitrofurans and other antiamebic
agents. Arch. Med. Res., 28 (Spec. iss.), 295-297 (1997).
Clinical and Laboratory Standards Institute, Performance
standards for antimicrobial disk susceptibility tests.
Approved standard – ninth edition. CLSI document M2-
A9, Wayne, PA, USA (2006a).
Clinical and Laboratory Standards Institute, Methods for
dilution antimicrobial susceptibility tests for bacteria that
grow aerobically. Approved standard – seventh edition.
CLSI document M7-A7, Wayne, PA, USA (2006b).
del Campo, R., Criado, J. J., Gheorghe, R., Gonzalez, F. J.,
Hermosa, M. R., Sanz, F., Mazano, J. L., Monte, E., and
Rodriguez-Fernandez, E., N-benzoyl-N'-alkylthioureas and
their complexes with Ni(II), Co(III) and Pt(II) - crystal struc-
ture of 3-benzoyl-1-butyl-1-methyl-thiourea: activity against
fungi and yeast. J. Inorg. Biochem., 98, 1307-1314 (2004).
Eissa, A. A. and Moneer, A. A., Synthesis and antimicrobial
activity of novel tetrahydrobenzothienopyrimidines. Arch.
Pharm. Res., 27, 885-892 (2004).
Kaminska, B., Ellert-Miklaszewska, A., Oberbek, A.,
Wisniewski, P., Kaza, B., Makowska, M., Bretner, M., and
Kazimierczuk, Z., Efficacy and mechanism of anti-tumor
action of new potential CK2 inhibitors toward glio-
blastoma cells. Int. J. Oncol., 35, 1091-1100 (2009).
Kang, I. J., Wang, L. W., Lee, C. C., Lee, Y. C., Chao, Y. S.,
Hsu, T. A., and Chern, J. H., Design, synthesis, and anti-
HCV activity of thiourea compounds. Bioorg. Med. Chem.
Lett., 19, 1950-1955 (2009).
Khan, S. A., Singh, N., and Saleem, K., Synthesis, charac-
terization and in vitro antibacterial activity of thiourea
and urea derivatives of steroids. Eur. J. Med. Chem., 43,
2272-2277 (2008).
Li, H. Q., Lv, P. C., Yan, T., and Zhu, H. L., Urea derivatives
as anticancer agents. Anticancer Agents Med. Chem., 9,
471-480 (2009a).
Li, J., Tan, Z., Tang, S., Hewlett, I., Pang, R., He, M., He, S.,
Tian, B., Chen, K., and Yang, M., Discovery of dual inhibi-
tors targeting both HIV-1 capsid and human cyclophilin A
to inhibit the assembly and uncoating of the viral capsid.
Bioorg. Med. Chem., 17, 3177-3188 (2009b).
Garvey, E. P., Oplinger, J. A., Tanoury, G. J., Sherman, P.
A., Fowler, M., Marshall, S., Harmon, M. F., Paith, J. E.,
and Furfine, E. S., Potent and selective inhibition of human
nitric oxide synthases. Inhibition by non-amino acid iso-
thioureas. J. Biol. Chem., 269, 26669-26676 (1994).
Handy, R. L., Wallace, P., and Moore, P. K., Inhibition of
nitric oxide synthase by isothioureas: cardiovascular and
antinociceptive effects. Pharmacol. Biochem. Behav., 55,
179-184 (1996).
Ijuin, R., Umezawa, N., Nagai, S., and Higuchi, T., Evalua-
tion of 3-substituted arginine analogs as selective inhibi-
tors of human nitric oxide synthase isozymes. Bioorg.
Med. Chem. Lett., 15, 2881-2885 (2005).
Nicholson, A., Perry, J. D., James, A. L., Stanforth, S. P., De
Soyza, A., and Gould, K., Antimicrobial activity of novel S-
(benzyl) isothiourea derivatives against multiply resistant
Pseudomonas aeruginosa and Burkholderia cepacia com-
plex from patients with cystic fibrosis undergoing lung
transplant assessment. J. Heart Lung Transplant., 28,
S160 (2009).
Paesano, N., Marzocco, S., Vicidomini, C., Saturnino, C.,
Autore, G., De Martino, G., and Sbardella, G., Synthesis
and biological evaluation of 3-benzyl-1-methyl- and 1-
methyl-3-phenyl-isothioureas as potential inhibitors of
iNOS. Bioorg. Med. Chem. Lett., 15, 539-543 (2005).
Paquay, J. B., Hoen, P. A., Voss, H. P., Bast, A., Timmerman,
H., and Haenen, G. R., Nitric oxide synthase inhibition by
dimaprit and dimaprit analogues. Br. J. Pharmacol., 127,
331-334 (1999).
Iwai, N., Ebata, T., Nagura, H., Kitazume, T., Nagai, K., and
Wachi, M., Structure-activity relationship of S-benzyliso-
thiourea derivatives to induce spherical cells in Escherichia
coli
.
Biosci. Biotechnol. Biochem., 68, 2265-2269 (2004).
Perlovich, G. L., Proshin, A. N., Volkova, T. V., Kurkov, S. V.,
Grigoriev, V. V., Petrova, L. N., and Bachurin, S. O., Novel
isothiourea derivatives as potent neuroprotectors and cogni-
tion enhancers: synthesis, biological and physicochemical
properties. J. Med. Chem., 52, 1845-1852 (2009).
Rodriguez-Fernandez, E., Mazano, J. L., Benito, J. J.,
Hermosa, M. R., Monte, E., and Criado, J. J., Thiourea,
triazole and thiadiazine compounds and their metal com-
plexes as antifungal agents. J. Inorg. Biochem., 99, 1558-
Iwai, N., Nagai, K., and Wachi, M., Novel S-benzylisothiourea
compound that induces spherical cells in Escherichia coli
probably by acting on a rod-shape-determining protein(s)
other than penicillin-binding protein 2. Biosci. Biotechnol.
Biochem., 66, 2658-2662 (2002).
Jesko, H. A., Chalimoniuk, M., and Strosznajder, J. B., Acti-
vation of constitutive nitric oxide synthase(s) and absence
of inducible isoform in aged rat brain. Neurochem. Int., 42,