A facile access to novel steroidal 17-2′-(1′,3′,4′)-oxadiazoles,and an evaluation of their cytotoxic activities in vitro

Novel types of 17-exo-heterocycles in the Δ⁵ androstene series carrying an 1,3,4-oxadiazole moiety were efficiently synthesized via aldehyde N-acylhydrazone intermediates, obtained from the microwave-assisted condensation of 3β-hydroxy- or 3β-acetoxyandrost-5-ene-17β-carbaldehyde with different acylhydrazides. The subsequent phenyl iodonium diacetate-induced oxidative cyclization proceeded under mild conditions. The synthesized compounds were subjected to in vitro pharmacological studies to investigate their antiproliferative activities on four malignant adherent cell lines (HeLa, MCF7, A2780 and A431), and exhibited the highest potency against HeLa cells, some of them revealing action comparable to that of the reference agent cisplatin.     

Microwave assisted synthesis of naphthopyrans catalysed by silica supported fluoroboric acid as a new class of non purine xanthine oxidase inhibitors

A series of naphthopyrans was synthesized employing silica supported fluoroboric acid under solvent free conditions in a microwave reactor. The catalytic influence of HBF₄–SiO₂ was investigated in detail to optimize the reaction conditions. The synthesised compounds were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure–activity relationship analyses have also been presented. Among the synthesised compounds, NP-17, NP-19, NP-20, NP-23, NP-24, NP-25 and NP-26 were the active inhibitors with an IC₅₀ ranging from 4 to 17 μM. Compound NP-19 with a thiophenyl ring at position 1 emerged as the most potent xanthine oxidase inhibitor (IC₅₀ = 4 μM) in comparison to allopurinol (IC₅₀ = 11.10 μM) and febuxostat (IC₅₀ = 0.025 μM). The basis of significant inhibition of xanthine oxidase by NP-19 was rationalized by its molecular docking at MTE binding site of xanthine oxidase.     

InCl3 as a powerful catalyst for the acetylation of carbohydrate alcohols under microwave irradiation

Indium(III) chloride catalyzed microwave assisted acetylation of different carbohydrates is an efficient synthesis of per-O-acetyl derivatives and provides the products in good to excellent yields.     

Salt-assisted acid hydrolysis of chitosan to oligomers under microwave irradiation

The effect of inorganic salts such as sodium chloride on the hydrolysis of chitosan in a microwave field was investigated. While it is known that microwave heating is a convenient way to obtain a wide range of products of different molecular weights only by changing the reaction time and/or the radiation power, the addition of some inorganic salts was shown to effectively accelerate the degradation of chitosan under microwave irradiation. The molecular weight of the degraded chitosan obtained by microwave irradiation was considerably lower than that obtained by traditional heating. Moreover, the molecular weight of degraded chitosan obtained by microwave irradiation assisted under the conditions of added salt was considerably lower than that obtained by microwave irradiation without added salt. Furthermore, the effect of ionic strength of the added salts was not linked with the change of molecular weight. FTIR spectral analyses demonstrated that a significantly shorter time was required to obtain a satisfactory molecular weight by the microwave irradiation-assisted inorganic salt method than by microwave irradiation without inorganic salts and conventional technology.     

Piperazine-azole-fluoroquinolone hybrids: Conventional and microwave irradiated synthesis,biological activity screening and molecular docking studies

A series of new 1,2,4-triazole and 1,3,4-oxadiazole derivatives was obtained via several steps sequential reactions of phenyl piperazine. Then, these compounds were converted to the corresponding fluoroquinolone hybrids via one pot three component Mannich reaction. All the reactions were examined under conventional and microwave mediated conditions, and optimum conditions were determined. The effect of different solvents and microwave power on microwave prompted reactions was investigated as well. All the newly synthesized compounds were characterized by FTIR, ¹H NMR, ¹³C NMR and EI MS spectral techniques. The antimicrobial activity, DNA gyrase and Topoisomerase IV inhibition potentials were performed. The results obtained showed that fluoroquinolone hybrids possess good antimicrobial activity. Moreover, Fluoroquinolone-azole-piperazine hybrids synthesized in the present study displayed excellent DNA gyrase inhibition. To unveil the interaction mode of compounds to receptor, a molecular docking study was performed. With an average least binding energy of −9.5 kcal/mol, all compounds were found to have remarkable inhibitory potentials against DNA gyrase (E. coli).     

Rapid microwave-assisted synthesis and characterization of cellulose-hydroxyapatite nanocomposites in N,N-dimethylacetamide solvent

Preparation of nanocomposites was carried out using microcrystalline cellulose, CaCl₂, and NaH₂PO₄ in N,N-dimethylacetamide (DMAc) solvent by a microwave-assisted method at 150 °C. XRD results showed that the nanocomposites consisted of cellulose and hydroxyapatite (HA). The cellulose existed as a matrix in the nanocomposites. SEM and TEM analysis showed that HA nanorods were homogeneously dispersed in the cellulose matrix. The effects of the microwave heating time on the products were investigated. This method has advantages of being simple, rapid, low-cost, and environmentally friendly.     

Microwave driven wood liquefaction with glycols

Wood liquefaction with glycols using p-toluenesulfonic acid as the catalyst was carried out under microwave heating. With rapid heating and temperatures in the 190–210 °C range complete liquefaction was achieved in 7 min. Liquefaction efficiency was dependent on the choice of glycol. Simple glycols such as ethylene glycol and propylene glycol were more effective than higher analogues. The use of glycerol in mixtures with glycols showed a synergistic effect. Size exclusion chromatography was used to follow the gradual emergence of liquefaction products in solution as well as the recondensation products that start forming early in the reaction and precipitate from solution when molar masses of approx. 1 × 10⁴ g/mol are reached.     

The Microwave Syndrome: A Preliminary Study in Spain

A health survey was carried out in Murcia, Spain, in the vicinity of a Cellular Phone Base Station working in DCS‐1800 MHz. This survey contained health items related to “microwave sickness” or “RF syndrome.” The microwave power density was measured at the respondents' homes. Statistical analysis showed significant correlation between the declared severity of the symptoms and the measured power density. The separation of respondents into two different exposure groups also showed an increase of the declared severity in the group with the higher exposure.     

超声造影引导下行微波消融术治疗肝癌的临床效果分析*

摘要目的：评估超声造影(CEUS)引导下微波消融(MWA)治疗肝癌的有效性及应用价值。方法：108 例肝癌患者,共147个病灶经 MWA治疗。根据患者在做常规超声检查时,是否有扫查不清晰的结节或其他影像学检查提示可能存在多发结节等,分成CEUS 族和对照组。CEUS组41 名患者,年龄(57.9± 7.8）岁,共57 个病灶,平均直径（2.4± 1.5）cm,经超声造影引导下行微波消融治疗。 对照组67 名患者,年龄（55.5± 8.9）岁,共90 个病灶,平均直径（2.6± 1.7）cm,常规超声引导下同种条件行微波消融治疗。治疗后 对两组患者进行6～12 个月随访。结果：CEUS组的57 个病灶均清晰显示其位置、数目、大小、边界、形态,完全消融的结节为55 个,未完全消融的结节为2个。对照组67 名患者的90 个病灶,完全消融的病灶78 个;未完全消融的结节12 个。CEUS组完全消 融率高于病例对照组(96.49 %VS 86.67 %;P< 0.05）。随访6～12 个月后发现,CEUS 组完全消融率高于病例对照组(P< 0.05）,差 异有统计学意义。结论：CEUS能更好的显示病灶的位置、数目、大小,更精确显示病灶边界、范围,造影引导下MWA 是一种有效 提高完全消融效率的方法,具有较大应用价值。