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1.
3-(2-呋喃基)-4-芳基-1,2,4-三唑啉-5-硫酮的合成及生物活性 总被引:3,自引:0,他引:3
1-(2-呋喃甲酰基)-4-芳基氨基硫脲经过环化反应,制备了一系列新的化合 物3-(2-呋喃基)-4-芳基-1,2,4-三唑啉-5-硫酮类化合物,并通过元素分析和 IR,^1H NMR等波谱数据确证了上述化合物的结构。初步的生物活性实验表明其中 有些化合物的具有非常好的植物生长调节活性。 相似文献
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Some new 2-[5-(aryl)-[1,3,4]oxadiazole-2-ylsulfanyl]alkanoic acids were synthesized and studied for their antibacterial activity. These compounds were prepared from aromatic carboxylic acid hydrazides. Aromatic carboxylic acid hydrazides 1 on refluxing with carbon disulfide and methanolic potassium hydroxide and then on subsequent acidification with hydrochloric acid furnish 5-aryl-1,3,4-oxadiazole-2-thiones 2. 2-Chloro alkanoic acids react with 2 in alkaline media and on acidification yield the title compounds 3. These compounds were characterised by CHN analyses, IR, mass and 1H NMR spectral data. All the compounds were evaluated for their in vitro antibacterial activity against two Gram negative strains (Escherichia coli and Pseudomonas aeruginosa) and two Gram positive strains (Bacillus subtilis and Staphylococcus aureus) and their minimum inhibitory concentration (MIC) were determined. 相似文献
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A survey of literature1 revealed that s-triazolo[3,4-b]-1,3,4-thiadiazole, an interesting fused system of s-triazole and 1,3,4-thiadiazole rings, has received much attention during recent years on account of its prominent utilizations as antifungal, antiinflammatory, antiviral, analgesic and anthelmintic agents probably resulting from its planner and compact structure. Our earlier work on the synthesis of this class of heterocycles showed antibacterial, herbicidal and plant growth regulative properties2-3 for the compounds. 1,2,3-Triazole derivatives have found their wide use in medicine, agriculture and industry4-5. Incorporation of 1,2,3-triazole moiety into the 6-position of this ring system may lead to achieving compounds of better biological activities. In view of the above findings coupled with scanty reports on these condensed compounds carrying 6-heterocyclic groups, we wish to report here the condensation of 4-amino-5-mercapto-3-(4-pyridyl)-l,2,4-triazole(2) with 1-aryl-4-carboxy-5-methyl-1,2,3-triazoles(1a-j) as a part of our continuing interest in this area. 相似文献
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Acylthiourea derivatives are useful as pesticides, herbicides, fungicides and regulator for plant growth, and also as important intermediates in the organic synthesis. In recent years, phase transfer catalysis reaction technique has been widely recognized as an efficient synthetic tool and attracted much attention. In view of these observations, a series of 5-aryl-2-furoyl thioureas containing substituted pyrimidine ring were synthesized using PEG-400 as solid-liquid phase transfer catalyst under ultrasonic irradiation. All of the new compounds have been exactly determined by IR, 1H NMRand elemental analysis. 相似文献
7.
Preparation of Some Thiazolyl Hydrazone Derivatives and Evaluation of Their Antibacterial Activities
Gülhan Turan-Zitouni Ahmet Özdemir Zafer Asım Kaplancıklı Jean-Alain Fehrentz Jean Martinez Pierre Chevallet 《Phosphorus, sulfur, and silicon and the related elements》2013,188(10):2613-2623
The increasing clinical importance of drug-resistant fungal and bacterial pathogens has provided additional urgency to microbiological research and to the development of new antibacterial compounds. For this purpose, new tert-butyl [1-aryl/alkyl-2[(4-aryl-2-thiazolyl)hydrazono]ethyl]carbamate derivatives were synthesized and evaluated for antibacterial activity. The reaction of Boc-L-phenylalaninal, Boc-D-phenylalaninal, Boc-L-leucinal, and Boc-L-tryptophanal with thiosemicarbazide yielded the thiosemicarbazones, which furnished the title compounds on reaction with phenacyl bromides. The new compounds were screened for antibacterial activity. The results from the bioassay tests show that some of the compounds have notable activity against Gram-positive bacteria. 相似文献
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Certain 5-aryl-6-[tetra(O-benzoyl)-β-D-glucopyranosylimino]-4-benzylthio-2-phenylimino-5,6-dihydro-2H-1,3,5-thiadiazines have
been prepared by interaction of N-[tetra(O-benzoyl)-β-D-glucopyranosyl] isocyanodichloride and 1-aryl-5-phenyl-2-(S-benzyl)-2,4-isodithiobiurets.
The products have been characterized through the usual chemical transformations, IR, NMR and mass spectral analyses. The compounds
have been screened for their antibacterial activities against various bacteria.
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Published in Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 910–913, June, 2005. 相似文献
9.
N-芳基-N''''-(5-芳基-2-呋喃甲酰基)硫脲衍生物的合成及其生物活性的研究 总被引:14,自引:0,他引:14
于固-液相转移条件下,合成了40个未见报道的N-芳基-N'-(5-芳基-2-呋喃甲酰基)硫脲衍生物,用元素分析、UV、IR以及~1H NMR光谱确定了它们的结构.该法具有操作简便、反应条件温和、产率高等优点.初步生物活性试验表明,该类化合物对小麦幼苗生长有明显的促进作用. 相似文献
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G. Linga Goud S. Ramesh D. Ashok V. Prabhakar Reddy 《Russian Journal of General Chemistry》2016,86(6):1419-1423
A new series of 1-aryl-3-(1-aryl-1H-[1,2,3]triazol-4-yl)propenones (6a–6j) was synthesized by condensation of substituted acetophenones (5a–5c) with substituted 1-aryl-1H-[1,2,3]triazole-4-carbaldehydes (4a–4d) in the presence of potassium hydroxide under conditions of grinding and microwave irradiation. All the newly synthesized compounds were characterized by the IR, NMR, and mass spectroscopic analyses and their antibacterial activity against gram-positive and gram-negative bacterial strains was evaluated. Among the compounds synthesized, better activity was exhibited by 6a, 6c, 6f, 6g, and 6i. 相似文献
11.
Vijai N. Pathak Rahul Joshi Jaimala Sharma Neetu Gupta Vijay Mohan Rao 《Phosphorus, sulfur, and silicon and the related elements》2013,188(7):1854-1865
N1-acetyl-5-aryl-3-(substituted styryl)pyrazolines were synthesized by the cyclocondensation of 1,5-substituted diphenyl-1,4-pentadien-3-ones with hydrazine hydrate and a cyclizing agent such as acetic acid in ethanol. The title compounds were synthesized using conventional and solvent-free approaches, which involves mechano-chemical mixing, microwave-irradiation, and ultrasound-irradiation methods in the presence of a solid support. The synthesized compounds have been characterized by elemental analyses and spectral data (IR, PMR, and FAB-mass). All the synthesized compounds have been evaluated for their antibacterial and antifungal activities. Some compounds have shown promising biological activity. 相似文献
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Cephalosporin derivatives are an interesting class of β-lactam antibiotics because of their power against a large number of both Gram-positive and Gram-negative organisms. Many efforts have been made to synthesize cephalosporin by varying the substituents. Further pharmacological research indicated the inhibitory activity, broad-spectrum biological activity and β-lactamase resistance determined by the side chain at 7β position of 7-ACA and the structure of substituted group at C3 position. Actually, most of its applications in clinic are the derivatives linked with heterocyclic at C3 and 7β position of cephalosporin skeleton. Literature[1] also revealed that cephalosporin containing aminothiazoloxime at the 7β position of 7-ACA used as antibiotics with obvious applications. Moreover, some compounds bearing 1,2,3-triazole ring at the C3 position of 7-ACA have been reported to possess better antibacterial activity. For these purpose, we synthesized new cephalosporin 3a-c and 5a-c by the reaction of 7-ACA with 2-arylamino-1,3,4-thiadiazol-5-thioles, and then reacted with 1 -aryl-5-methyl-1H-1,2,3-triazol-4-formyl chloride 2 or aminothiazoloxime active ester 4,respectively. 相似文献
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Saify ZS Mushtaq N Khan KM Perveen S Shah ST Abdel-Jalil RJ Fecker M Voelter W 《Chemical & pharmaceutical bulletin》2005,53(1):64-66
A new series of 4-(4'-chlorophenyl)-4-hydroxypiperidine derivatives (2-5), substituted at nitrogen, were synthesized and tested as potential analgesic compounds as well as evaluated for their effect on hypotensive activity. Results showed that all the derivatives exhibit significant analgesic activity in male Wistar rats at a dose of 50 mg/kg of body weight after intramuscular injection, when tested by thermal stimuli (tail flick test). Pethidine was used as reference drug. Compounds 2, 3 and 5 produced reduction in blood pressure in normotensive rat. 相似文献
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Ulf Wellmar Anna-Britta Hörnfeldt Salo Gronowitz Nils Gunnar Johansson 《Chemistry of Heterocyclic Compounds》1996,32(11-12):1312-1318
A series pf 5-aryl-2′-deoxyuridines has been prepared and evaluated as antiviral agents. The following substituents have been used in position 3 of the phenyl ring: chloro, iodo, amino, azido, methylthio, and vinyl. None of the new compounds showed any significant activity when tested against human immunodeficiency virus 1 (HI V-I), herpes simplex virus 1 (HSV-I), or human cytomegalovirus (HCMV). 相似文献
15.
T. Gireesh R. R. Kamble R. K. Hunnur T. Taj M. Y. Kariduraganavar 《Chemistry of Heterocyclic Compounds》2011,47(7):877-885
The reaction of sydnone-derived 3-aryl-5-methyl-1,3,4-oxadiazol-2(3H)-ones with thiourea and α-bromoacetophenone derivatives in the presence of a catalytic amount of TiCl4 produces 2-aryl-4-(4-aryl-1,3-thiazol-2-yl)-5-methyl-2,4-dihydro-3H-1,2,4-triazol-3-ones. The title compounds were screened for their antibacterial and antifungal activity. The toxicity of
the compounds was evaluated in terms of mutagenicity, tumorigenicity, and reproductive effects. The drug-relevant properties
(ClogP, drug-likeness, and drug score) were calculated, and the structure–activity relationship was discussed. 相似文献
16.
Biginelli reaction of ethyl acetoacetate, thiourea and the appropriate aromatic aldehyde was used to produce ethyl 4-aryl-6-methyl-2-thioxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylates, that reacted with bromomalononitrile to give ethyl 3-amino-5-aryl-2-cyano-7-methyl-5H-thiazolo[3,2-a]pyrimidine-6-carboxylates rather than the isomeric 7H-thiazolo[3,2-a]pyrimidines. Thiazolopyrimidine derivatives reacted with carbon disulphide to yield ethyl 9-aryl-7-methyl-2,4-dithioxo-2,3,4,9-tetrahydro-1H-thiazolo[3,2-a:4,5-d']dipyrimidine-8-carboxylates, that reacted with phenacyl bromide to produce ethyl 8-methyl-10-(4-methoxyphenyl)-3-substituted-5-thioxo-2(un)subatituted-10H-thiazolo[3',2':1',2']pyrimido[4',5':4,5]thiazolo[3,2-a]pyrimidine-9-carboxylates. The aforementioned reactions were carried out using both conventional chemical methods and with the assistance of microwave irradaition. Comparison between both methods showed that the microwave assisted method is preferable because of the time reduction and yield improvements achieved. The new compounds were tested for their biological activity as antioxidants, antibacterial or antifungal agents. Some of the new compounds were found to have moderate to good antioxidant and antimicrobial activities. 相似文献
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2-Amino-5-(2-aryl-2H-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles 2-4 have been synthesized by the reaction of 2-aryl-2H-1,2,3-triazole-4-carboxylic acids 1 with thiosemicarbazide. Their reaction with phenacyl (p-substituted phenacyl) bromides led to formation of the respective 6-aryl-2-(2-aryl-2H-1,2,3-triazol-4-yl)imidazo[2,1-b]-1,3,4-thiadiazoles 5. Reactivity of the latter fused ring towards reaction with different electrophilic reagents afforded the corresponding 5-substituted derivatives 6-8. The structure of the above compounds was confirmed from their spectral characteristics. Some of these compounds were found to possess slight to moderate activity against the microorganisms Staphylococcus aureus, Candida albicans, Pseudomonas aeruginosa, and Escherichia coli. 相似文献
18.
Erno Mohacsi Jay P. O'Brien John F. Blount Jerry Sepinwall 《Journal of heterocyclic chemistry》1990,27(6):1623-1628
Diastereomeric cis- and trans-tetrahydro-4-aryl-3-[(dimethylamino)methyl]-2H-pyranols derived from 3-[(dimethylamino)methyl]tetrahydro-4H-pyran-4-one ( 5 ), have been prepared and their configurations were established on the basis of ir data. The biologically more potent trans isomer 3 was resolved into its optical antipodes and the absolute stereochemistry of one of the enantiomers 14 , was determined by X-ray crystallography. Some of the compounds showed analgesic activity comparable to codeine. 相似文献
19.
1,2,3-Triazole derivatives have been reported as inhibiting tumor proliferation, invasion, and metastasis[1]. The fused l,3,4-triazolo[3,4-b]-1,3,4-thiadiazoles derivatives show various biological effects such as antifungal[2], antibacterial, hypotensive and CNS depressant activities[3]. We have reported several 6-aryl-3-[5-methyl-1-(4-methylphenyl)-1,2,3-triazol-4-yl]-s-triazolo[3,4-b]-1,3,4-thiadiazoles in the previous paper[4]. The novel 6-aryl-3-[5-methyl-1-(4-methylphenyl)-1,2,3-triazol-4-yl]-s-triazolo[2,4-b]-1,3,4-thiadiazoles 6a-j have been synthesized by the condensation of 4-amino-5-mercapto-3-[5-methyl-1-(4-methylphenyl)-1,2,3-triazol-4-yl]-s-triazole 5 with various aromatic carboxylic acids in the presence of phosphorus oxychloride. The mercaptotriazole 5 was prepared from 4,the latter being prepared from 1 throng 2 and 3. The title compounds 6 were depicted in scheme 1. The structures of these compounds were established by elemental analysis, NMR, MS and IR techniques. 相似文献