Synthesis, antimicrobial and antioxidant activities of pyridyl substituted thiazolyl triazole derivatives

In this present study, 63 different 5-[4-methyl-2-(pyridin-3/4-yl)thiazole-5-yl]-4-substituted-3-substituted benzylthio-4H-1,2,4-triazole derivatives were synthesized, and evaluated for their in vitro antimicrobial activity against various human pathogenic microorganisms and antioxidant activity. The derivatives were synthesized in a multi-step synthesis procedure including triazole and thiazole ring closure reactions, respectively. The synthesized derivatives (A1-24; B1-39) were screened for their antibacterial, antifungal, and antioxidant activities compared to standard agents. The derivatives possessing 3-pyridyl moiety particularly exhibited relatively high antibacterial activity (MIC= < 3.09-500 µg/mL) against Gram-positive bacteria, and compounds possessing 4-pyridyl moiety showed remarkable antioxidant activity

Analysis of furans and pyridines from new generation heated tobacco product in Japan

BACKGROUND@#In recent years, heated tobacco products (HTPs), which are widely used in Japan, have been sold by various brands using additives such as flavors. It has been reported that the components of mainstream smoke are different from those of conventional cigarettes. In this study, we established an analytical method for furans and pyridines in the mainstream smoke, which are characteristic of HTPs and particularly harmful among the generated components, and investigated the amount of component to which the smokers are exposed.@*METHODS@#We established a simple analytical method for simultaneous analysis of gaseous and particulate compounds in the mainstream smoke of HTPs (IQOS, glo, ploom S) in Japan by combining a sorbent cartridge and glass fiber filter (Cambridge filter pad (CFP)). Both the sorbent cartridge and CFP were extracted using 2-propanol and analyzed via GC-MS/MS to determine the concentration of furans and pyridines generated from each HTP.@*RESULTS@#The results showed that the levels of target furans such as furfural, 2-furanmethanol, 2(5H)-furanone, and 5-methylfurfural tended to be higher in the mainstream smoke of glo than in standard cigarettes (3R4F). Pyridine, which is generated at a high level in 3R4F as a combustion component, and 4-ethenylpyridine (EP), which is a known marker of environmental tobacco smoke, were detected. Among these components, 2-furanmethanol and pyridine are classified as Group 2B (possibly carcinogenic to humans) by the International Agency for Research on Cancer (IARC). Therefore, it is possible that they will contribute to the health effects caused by use of HTPs.@*CONCLUSIONS@#Using the new collection and analytical method for furans and pyridines in the mainstream smoke of HTPs, the level of each compound to which smokers are exposed could be clarified. By comprehensively combining information on the amount of ingredients and toxicity, it will be possible to perform a more detailed calculation of the health risks of using HTPs. In addition, the components detected in this study may be the causative substances of indoor pollution through exhaled smoke and sidestream smoke; therefore, environmental research on the chemicals generated from HTPs would be warranted in future studies.

Synthesis of some novel pyrimidine, thiophene, coumarin, pyridine and pyrrole derivatives and their biological evaluation as analgesic, antipyretic and anti-inflammatory agents

Pyrimidine derivative 3 was afforded through the reaction of compound (1) with 5-ureidohydantion (2). Product 3 underwent a cyclization to produce fused pyrimidine derivative 7, although the latter product 7 was synthesized through one step via the reaction of compound (1) with 5-ureidohydantion (2) using another catalyst. Compound 3 was oriented to react with cyclic ketones 8a,b in the presence of elemental sulfur, salicylaldehyde (10), aryldiazonium chlorides 12a,b and ω-bromo-4-methoxy- acetophenone (14), which afforded, fused thiophene derivatives 9a,b, coumarin derivative 11, arylhdrazono derivatives 13a,b and 4-methoxyphenyl butenyl derivative 15, respectively. The latter product 15 was reacted with either potassium cyanide (16a) or potassium thiocyanide (16b) to form cyano and thiocyano derivatives 17a,b, respectively. Compound 17a underwent further cyclization to afford pyridopyrimidine derivative 19. Compound 15 was reacted with either hydrazine (20a) or phenylhydrazine (20b) to produce hydrazo derivatives 21a,b and these products were cyclize to produce pyrrole derivatives 23a,b. Finally, 5-ureidohydantion (2) was reacted with compounds 24a,b,c to afford pyrimidine derivatives 25a,b,c. The structures of the synthesized compounds were confirmed using IR, 1H NMR, 13C NMR and mass spectrometry techniques. Compounds 11 and 19 have promising as analgesic and antipyretic activities

Cytotoxic evaluation of certain insect growth regulators and insect sex pheromones in cho-k1 cells

The cytotoxic effects of Diflubeizuron, pyriproxifen as insect growth regulators, ZZ/ZE-7,11-hexadecadienyl acetate, Z-9- hexadecenal and Z-11-hexadecenal as insect sex pheromones were evaluated in vitro using Chinese hamster ovary [CHO-K1] cells. Total cellular protein [TCP] content and methyl tetrazolium [MTT] assays were carried out using serum free medium and medium supplemented with fetal calf serum [FCS, 10%], bovine serum albumin [BSA, 1%] and/or metabolic activation system [S9-mix]. All the tested compounds displayed cytotoxic effects that rise with time exposure. TCP assay exhibited higher sensitivity than MTT assay with all the tested compounds. In presence of the added extracellular proteins and/or metabolic activation system [S9-mix], the cytotoxic effects significantly decreased which indicate that the tested agents may be binding non-specifically with protein and extensive metabolized to less toxic metabolites

Spectral characteristics of schiff bases derived from 2,6 diamino pyridine and benzaldehyde derivatives

The spectrophotometric studies of Schiff bases were the subject of several investigations [1-5]. However, relatively little attention has been given to the spectral behaviour of more recent dianils [6], which have drawn the attention as efficient chelating compounds [7-9]. The present study deals with the uv-vis, IR, [1]H nmr and mass spectrometric investigation of a series of dianils based on 2,6-diaminopyridine, in order to elucidate their molecular structure on the spectral characteristics

Volumetric determination of piroxicam in presence of degradation product

An indirect volumetric method for the determination of piroxicam is developed. It depends on the reaction of piroxicam with a measured excess of ammonium-cerric-sulfate in sulfuric acid medium. The excess cerric is back titrated with st and ard ammonium ferrous sulfate using ferroin as indicator. The molar ratio of the reactants was determined to be one drug to four ammonium-cerric-sulfate. The method was successfully applied for the determination of piroxicam in pharmaceutical preparations. The presence of 2-aminopyridine, the degradation drug product, did not interfere with the accurate determination of piroxicam. The validity of the method was checked using the st and ard addition technique