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4-dimethylamino-2-glycosylaminoquinazoline derivatives were synthesized by cyclodesulfurization of N-aryl-N'-glycosyl thioureas with dimethylcyanamide in the presence of silver triflate in good yields.
To investigate whether teratogenicity of ethylene thiourea (ETU) is due to ETU per se or to its metabolites, rat embryos cultured in vitro were exposed to 10 and 30 micrograms/ml of ETU in the presence or absence of rat liver microsomal fraction (S9mix). In the absence of S9mix, the incidence of morphological abnormalities increased dose-dependently. In the presence of S9mix, abnormal morphogenesis was almost absent in all embryos. These findings suggest that teratogenicity of ETU is due to ETU per se.
Several N-substituted-N'-[4-(4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thione -5-yl ) phenyl[thioureas were synthesized in order to examine their antibacterial and antifungal activities. The structures and purity of the synthesized compounds were confirmed by UV, IR and mass spectral data and elemental analysis. However, they were found not to possess significant antibacterial or antifungal activity.
In order to clarify the mechanisms of neoteny in the ice goby (Leucopsarion petersii), we examined effects of thyroid hormone and thiourea (TU) treatments on their neotenic characteristics and the pituitary-thyroid axis. Adult ice goby were exposed to 3, 5, 3'-triiodothyronine (T3, 0.1 ppm), TU (inhibitor of thyroid hormone synthesis, 30 ppm), or the combination of the two for 2 weeks. Observations of whole body T3 levels, thyroid follicles and TSH immunoreactive cells in the pituitary suggests the presence of a functioning thyroidal system. However, all of the neotenic features did not disappear in T3-treated fish, suggesting the absence of T3 responsiveness in peripheral tissues. These results indicate the similarity between neoteny of the ice goby and obligatory-type neoteny of urodeles.
A simple flow injection spectrophotometric method for the determination of nitrite is described. Nitrite injected into the flow system reacts with thiourea in acidic medium and the generated thiocyanate ion reacts with Fe(III) in the reagent solution to produce a highly colored product. The influences of chemical and physical parameters including reagent concentrations, sample volume injected, flow rates of the carrier and reagent solutions, reaction coil length and reaction temperature, were studied and optimum values of these parameters were established. Under the optimum conditions, the calibration curve for nitrite was linear over the concentration range 0.36 - 90 microg ml(-1) without preconcentration and over the range 3.8 - 500 ng ml(-1) with a simple online preconcentration step using an anion exchange column. The corresponding detection limits were 0.36 micro ml(-1) and 3.8 ng ml(-1), respectively. Up to 25 samples can be analyzed per hour, with an average relative standard deviation of < or = 1.2%. Interferences by various foreign ions were studied and the method was applied to the determination of nitrite in water and spiked water samples.
A new chromogenic reagent, N-o-methylphenyl-N'-(sodium p-aminobenzenesulfonate)thiourea (MSAT), has been synthesized and characterized by elemental analysis, (1)H-NMR, FT-IR and UV-Vis spectra. Based on the absorption spectrum of the colored complex of MSAT with palladium(II), a novel spectrophotometric method for the determination of palladium has been developed. In a pH 4.0 - 5.5 HAc-NaAc buffer solution, palladium(II) reacted with MSAT to form a stable yellow water-soluble complex with an apparent molar absorptivity of epsilon = 2.04 x 10(5) L mol(-1) cm(-1) at the maximum absorption of 318.0 nm. Beer's law was obeyed in the concentration range of 1.2 - 11.8 microg per 25 mL for palladium(II) with a correlation coefficient of 0.9997. The probable interfering ions and their tolerable limits have also been investigated in detail. The proposed method is simple, rapid, and sensitive, and has been applied to the determination of palladium in anode mud and ore samples with satisfactory results.
Changes of TSH-producing cells in the pituitary and thyroid expression of the growth factors, transforming growth factor alpha (TGF alpha) and epidermal growth factor receptor (EGFR), as well as cyclin D1, were investigated immunohistochemically in order to clarify their contribution to the enhancing effects of excess vitamin A (VA) on thyroidal carcinogenesis induced by thiourea (TU). Male rats were allocated to 4 groups, control, TU, VA, and TU + VA, respectively, receiving no treatment, water containing 0.2% TU, diet containing 0.1% VA, and both for 10 or 19 weeks after a single s.c. injection of DHPN (2800 mg/kg) for initiation. Immunohistochemistry using antibodies against TSH demonstrated enlargement of TSH-producing cells in the TU + VA group as compared to the TU group, supporting our conclusion that enhanced TSH stimulation is mainly responsible for promoting the effects of excess VA. Since the expression of TGF alpha, EGFR, and cyclin D1 in thyroid proliferative lesions did not exhibit any differences between the TU and TU + VA groups in the present study, these factors are unlikely to participate in VA enhancement of carcinogenesis.
In our previous investigation, which focused on two-stage carcinogenicity in the thyroid, rats were administered N-bis(2-hydroxypropyl)nitrosamine (DHPN), followed by thiourea (TU) over an experimental period of 19 weeks. Simultaneous treatment with a high level of vitamin A (VA) enhanced the induction of proliferative lesions that originated from the thyroidal follicular epithelium. To examine whether hormone synthesis in the thyroid could be inhibited by simultaneous treatment with a large amount of VA and TU, all of the rats were initially given a single subcutaneous injection of 2,800 mg DHPN/kg followed by a supply of 0% TU + 0% VA (DHPN only, control group), 0.2% TU in their drinking water (DHPN/TU group), 0.1% VA in their diet (DHPN/VA group), or 0.2% TU + 0.1% VA (DHPN/TU + VA group) during an experimental period of 4 weeks. Results obtained indicate that the iodine uptake and organification, namely iodination of tyrosine residue in thyroglobulin, of the thyroid, were significantly decreased in the DHPN/TU group compared to the DHPN control group. The variation in these values was attributable to the inhibitory effect of TU upon thyroid hormone synthesis. Results obtained from the DHPN/TU + VA and DHPN/TU groups were comparable. Therefore, the possibility that modification of hormone synthesis contributes to the enhancing effect of simultaneous treatment with a large amount of VA on thyroidal tumor induction by TU is considered to be very minimal.
1. The fate of N-methyl-N'-(hydroxy[14C]methyl)thiourea (MHT) has been studied in the male Sprague-Dawley rat. The compound is degraded to N-methylthiourea and formaldehyde. 2. N-Methylthiourea is excreted as a urinary metabolite whereas the formaldehyde is not excreted, either in the urine or the expired air, but is metabolized via formate to CO2. 3. At least 50% of an i.p. dose (100 mg/kg) of MHT is excreted unchanged and some of this undergoes hydrolysis within the urine to N-methylthiourea and formaldehyde. Production of formaldehyde leads to the formation of the urinary artefact N-(hydroxymethyl)urea. 4. Tissue-distribution studies with 14C-MHT have shown that radioactivity is selectively associated with the thyroid gland. A preliminary investigation has indicated that MHT has anti-thyroid hormone activity as it lowers the thyroxine in rat serum.
Pre-polymerized glutaraldehyde covalently linked to thiourea has been synthesized as a soluble polymer for immobilizing Ag(I) and Pt(II) and it has also been used for activating a polyacrylamide gel filtration media. The modified gel filtration media (Bio-Gel P-200) has a high capacity for Ag(I) (20 mumol/ml) and Pt(II) (8 mumol/ml) and has been shown to be stable and useful even in the presence of relatively high chloride (up to 1 M NaCl) and phosphate concentrations (0.25 M). The soluble polymer can have a Ag(I) capacity of between 2-11 mmol/g. Bio-Gel P-200 modified using glutaraldehyde/thiourea and in the Ag(I) and Pt(II) form selectively binds biotinylated BSA (b-BSA) over BSA. Using the Ag(I) form of the gel at pH 4.8 (0.05 M phosphate) only b-BSA binds and 30% can be eluted using 0.15 M NaCl, while no BSA binds to the column under these conditions. For the Pt(II) form of Bio-Gel P-200 at pH 4.8, none of the applied BSA binds to the modified resin while 40% of b-BSA does bind.
Reaction of 12 aromatic sulfonamides containing a free amino group with cyanate or thiocyanate in the presence of acid afforded the corresponding urea/thiourea derivatives which were assayed as inhibitors of three isozymes of carbonic anhydrase (CA), i.e., CA I, II and IV. Oxidation of the obtained thioureas with iodine in acidic medium afforded symmetrical 2,5-bis(substituted-phenyl)-1,3,4-thiadiazole derivatives possessing sulfonamido groups on the aromatic ring, via a new synthesis of the heterocyclic moiety. Good inhibition of all these three CA isozymes was observed with the new compounds, but a novel finding was that the ureas/thioureas reported here had an increased affinity for the slow isozyme CA I, which generally is less sensitive to inhibition by sulfonamides when compared to the rapid isozymes CA II and IV. The disubstituted-1,3,4-thiadiazoles on the other hand were better inhibitors of CA II than CA IV and especially CA I, similarly to the large majority of aromatic/heterocyclic sulfonamides. Some of the new compounds could constitute good lead molecules for developing more selective CA I inhibitors.
A simple, mild and synthetically useful method for the desulfurization of cyclic thioureas and related compounds, existing as thiol-thione tautomeric mixtures, by hydrogen peroxide in acetic acid is proposed. The effect of substituting different solvents for the acetic acid was investigated.
(1S,2S)-1,3-Diacetoxy-1-(4-nitrophenyl)-2-propyl isothiocyanate ((S,S)-DANI) was recently introduced as a new chiral derivatizing agent for the enantioseparation of amino compounds. In the present study, diastereomeric derivatives of racemic amino acids were formed with (S,S)-DANI. The thioureas produced were distinguished by means of infrared spectroscopy, theoretical calculations and high-performance liquid chromatography. The differences observed between the corresponding diastereomers by the independent methods are considered to prove the applicability of the new reagent in the field of enantiomer separation.
The thiourea treated mongooses display an increase in the number and size of the calcitonin cells. These cells sometimes are seen accompanied with desquamated epithelial cells within the colloid. The thyroid follicular cells also record an increase in their height.
The synthesis of the new radioprotective compounds ATB (I, 2-allylthioureidobenzoic acid), PTB (II, 2-phenylthioureidobenzoic acid), A-2-PTU (III, N-allyl-N'-2-pyridylthiourea), and P-2-PTU (IV, N-phenyl-N'-2-pyridylthiourea) and their influence on biological and genetic effects of gamma rays was studied. In result of investigations it must be noted that PTB displayed radioprotective effect as a result of which more plants in M1 germination and survive in M2 of the induced mutations is increased. The cytological analysis reveals that the studied substance (PTB) decreases chromosome aberration in meristem cells of pea roots almost twice as a result of postirradiation treatment. The effect of A-2-PTU in the experiments with peas greatly depends on the dose of irradiation, i.e., on the degree of damaging of the processes of cell restoration and the possibility of their partial restoration after the treatment with the protector. The results obtained suggest that chemical compounds of N,N'-disubstituted thiourea group (A-2-PTU and P-2-PTU) exert strong radioprotective effect in the experiments with peas. This is of great importance to modern radiobiology and radiation mutagenesis and also to protect hereditary structures against radiation.
Some new 5,7-disubstituted pyrido[2,3-d]pyrimidine derivatives have been synthesized by the condensation of 2-amino-3-cyano-4,6-disubstituted pyridine with carbon disulfide, thiourea, urea and formamide. The structure of these products are supported by their IR and 1H-NMR spectra as well as by elemental analysis. The compounds have been tested for their antibacterial activity against E. coli and S. aureus.
The inclusion interaction of beta-cyclodextrin and sym-diphenyl-thiourea and sym-diphenyl-urea was studied by UV spectra. The stoichiometry ratio for the formation of the inclusion complexes was determined by Hildebrand-Benesi equation linear analysis and molar ratio method. The standard molar Gibbs energies, enthalpies, and entropies were derived for the inclusion process by Ks at different temperatrues. The result showed that the host:guest ratio of inclusion complex between the two diphenyl compounds and beta-CD is 2 : 1, the stability constant (Ks) of 2 : 1 inclusion complexes was higher than that of 1 : 1 inclusion complexes due to cooperative binding in the close two hydrophobic cyclodextrin cavities, and the association of the guest molecule with beta-CD was favored by enthalpy changes, proving that the Van der Waals interaction and the dipole-dipole interaction were main binding forces of cyclodextrin inclusion complex.
The effect of thiourea (applied topically, in different concentrations, to the eggs and all the nymphal instars, and to adults also by feeding) on the red cotton-bug Dysdercus similis was studied. The eggs were severely affected (i.e. mortality was high), while the nymphal instars showed an adverse effect on ecdysis and adults which emerged from the treated last nymphal instar were characterized by high mortality, abnormal behaviour and reduced fecundity and viability. They were also smaller, weaker and morphologically abnormal compared with the controls and were differently coloured. They were likewise unable to reproduce, owing to atrophy of the gonads. The ovaries contained a large number of immature, pathological oocytes with degenerating follicular epithelium, which was thin with a regular outline in the early stages, but later became multilayered, with pyknotic nuclei, and displayed active destruction of glycoproteins and lipoproteins. Fibrogenesis and thickening of the tunica propria were clearly discernible. Although treated females were kept together with untreated males, the two showed no signs of being attracted to one another and displayed no mating behaviour, although some females showed a very low degree of ovulation. Only a few survived the Ist nymphal instar and none survived up to adult emergence, despite being kept under normal laboratory conditions.