Sulfonylguanidine Derivatives as Potential Antimelanoma Agents

Sulfonylguanidines are interesting bioactive compounds with a broad range of applications in the treatment of different pathologies. 2-Aminobenzazole-based structures are well employed in the development of new anticancer drugs. Two series of novel N-benzazol-2-yl-N′-sulfonyl guanidine derivatives were synthesized with the sulfonylguanidine in either an extra- or intracyclic frame. They were evaluated for their antiproliferative activity against malignant melanoma tumor cells, thus allowing structure-activity relationships to be defined. Additionally, NCI-60 screening was performed for the best analogue to study its efficiency against a panel of other cancer cell lines. The stability profile of this promising compound was then validated. During the synthetic process, an unexpected new deamidination of the sulfonylguanidine towards sulfonamide function was also identified.     

Fate of trace organics during rapid infiltration of primary wastewater at Fort Devens, Massachusetts

Transport and fate of trace organics were studied during rapid infiltration of primary wastewater at a land application facility in Fort Devens, Massachusetts. A preliminary sampling trip was made to compare trace organic concentrations in the infiltrating wastewater and in ground water samples from three monitoring wells around the site. Trace organic concentrations were reduced by the rapid infiltration process. However, significant concentrations of specific compounds could be detected in ground water down-gradient of the site.Therefore, a field study was undertaken to determine the primary region where trace organics were removed in the system. Teflon monitoring wells were installed at a depth of 1.2 m in one of the basins at the site prior to flooding. Flooding was initiated and samples of the raw wastewater, the wastewater entering the basin, the infiltrate at 1.2-m depth and the ground water down-gradient of the site were analyzed for six compounds selected for the study.Results from replicate samples during the 6-day flooding period demonstrated that most of the removal for the six compounds occurred in the top meter of the soil, although concentrations of each compound increased substantially in the basin infiltrate from two of the sample points after the fourth day of flooding. No removal of p-dichlorobenzene, p-(I,1,3,3-tetramethylbutyl)phenol and 2-(methylthio)benzothiazole was apparent in the aquifer itself, as indicated by relatively high concentrations of these compounds in the contaminated monitoring well down-gradient of the site.These data indicate that trace organic concentrations in primary effluent can be reduced by rapid infiltration and that most of the removal occurs in the top meter of the soil during the early phase of the flooding cycle. This removal capability can rapidly diminish, however, and result in ground water contamination by trace organics above background levels.     

GD-423杀菌灭藻剂在循环冷却水系统中的应用

GD-423是以TCMTB为主成分的新型杀菌灭藻剂,该杀菌剂对循环冷却水中的铁细菌、亚硝化菌,真菌特别有效。使用结果表明：GD-423具有杀生速度快,杀菌、灭藻及剥离粘泥效果好的特点,值得推广。     

Tribological properties and hydrolysis stability study of benzothiazole borate derivative

A novel borate ester derivative containing mercaptobenzothiazol and ethanolamine group (BMB) was synthesised and characterised. Its tribological properties in RSO were evaluated using a four‐ball tribometer, and its action mechanisms were investigated by scanning electron microscopy and X‐ray photoelectron spectroscopy. Its hydrolysis stability was investigated by open observation method and half‐time method, and its mechanism was discussed through Gaussian calculation. Results show that BMB possesses excellent extreme pressure, better anti‐wear performances and excellent hydrolysis stability for lone electron of nitrogen atoms forming a coordination effect with B atom. The boundary film, which contains organic nitrogen and inorganic salt, such as BN, Fe₂(SO₄)₃ and Fe‐O‐B, contributed to improve the tribological properties of RSO. Copyright © 2013 John Wiley & Sons, Ltd.     

Synthesis of N-(2 amino benzothiazole) methacylamide monomer and its copolymers for antimicrobial coating application by RAFT polymerization

Monomer with thiazole moiety was synthesized and copolymerized with butyl acrylate and methyl methacrylate by reversible addition fragmentation chain transfer emulsion polymerization. The chain transfer agent was synthesized using N-ethyl piperazine, carbon disulfide, and ethyl 2-bromoisobutyrate. The wt% of monomer was varied from 3, 5, 7, 9, and 12 respectively. A antimicrobial activities of monomer and its copolymers were screened against E. coli, B. subtilis, C. albicans, and Aspergillus niger microorganisms. The synthesized monomer and chain transfer agent were characterized by ¹H NMR, FTIR, and mass spectral analysis, whereas emulsion copolymers were characterized for their molecular weight, particle size, and FTIR analysis.     

2-肼基-4-甲基苯并噻唑的合成

研究了合成 2肼基 4甲基苯并噻唑的工艺 ,获得了可靠的工艺条件 ,放大实验结果表明产品的得率达 90 %。     

2-巯基苯并噻唑氧化合成苯并噻唑

以2-巯基苯并噻唑为原料,用双氧水进行氧化合成苯并噻唑,从反应原料的含量、反应温度、氢氧化钠含量、酸化时间4个方面优化了合成工艺。结果表明,优化反应条件为:50 mmol双氧水滴加到溶解有25 mmol 2-巯基苯并噻唑的100 mL浓度为0.25 mol/L氢氧化钠溶液中进行氧化,双氧水的滴加时间为30～40 min;反应温度为60～65℃;酸化时间为50～60 min,苯并噻唑收率为85%。     

1-苯并噻唑基-3,5-二苯基吡唑啉衍生物的合成与荧光性

设计和合成了7个新型苯并噻唑基-吡唑啉类化合物，通过元素分析和红外光谱检测，确定了化合物的结构，荧光检测结果表明它们的荧光强度为36．1-69.2，荧光强度的大小与衍生物中的取代基有关，溴和甲氧基取代衍生物具有较高的荧光性。     

含1,2,3-三唑的新型硫脲和氨基硫脲的合成

利用2-苯基-1，2，3-三唑-4-甲酰基异硫氰酸酯与2-氨基取代苯并噻唑和2-肼基取代苯并噻唑的加成反应合成了一系列二取代硫脲和氨基硫脲衍生物。研究了合成反应的条件。目标化合物经元素分析、IR和1^HNMI进行了结构确证。     

2-硫氰基甲基硫代苯并噻唑在工业水处理中的应用

作者介绍了2－硫氰基甲基硫代苯并噻唑（TCMTB）在工业水处理中用作杀菌灭藻剂的研究概况,并对其开发应用提出了一些建议。