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1.
Cemil İbiş Nihal Yilmaz H. Özlem Ataseven 《Phosphorus, sulfur, and silicon and the related elements》2013,188(9):1897-1906
Compounds 3a–k were obtained from the reactions of compounds 1a–k with homopiperazine (2) in CH 2 Cl 2 . Compounds 1a–b, 1d–f, and 1h–l gave compounds 5a–b, 5d–f, and 5h–l with 2-methylpiperazine (4) in dichloromethane. Compounds 7c and 9c were obtained from the reactions of compound 1c with 4-ethoxycarbonyl piperazine (6) and 4-piperidinol (8) in CH 2 Cl 2 . Compounds 1a and 1f gave compounds 11a and 11f with 4-methylpiperazine (10), and compound 13f was obtained from the reactions of compound 1f with 4-methylpiperidine (12) in CH 2 Cl 2 . 相似文献
2.
Phenacyl-malononitrile derivatives 1a,b react with dimethyl formamide dimethyl acetal (DMFDMA) in refluxing toluene to afford the enaminones 2a,b respectively. Compounds 2a and 2b react with the aromatic amines (aniline, p-toluidine, p-anisidine) in refluxing ethanol to afford the pyrroles 4a–f and with anthranilonitrile and methyl anthranilate to afford the pyrrolo[1,2-a]quinazolines 5a,b and 6a,b respectively. The pyrrole derivatives 4a–f react with hydrazine hydrate and phenyl hydrazine in refluxing ethanol to afford the pyrrolo[3,4-d] pyridazine derivatives 7a–f and 8a–f respectively. 相似文献
3.
2,3,4-三-O-乙酰基-b-D-木吡喃糖基异硫氰酸酯1与2-氨基-4/6-取代-苯并噻唑2a~2e反应, 生成糖基硫脲衍生物3a~3e, 再在伯胺存在下经氯化汞脱硫, 得到一系列新的胍基木吡喃糖苷类化合物4a~4e, 5a~5e, 6a~6e, 7a~7e, 所有新化合物的结构均经IR, 1H NMR, MS谱和元素分析证实, 所得产物均为β-构型. 生物活性测试结果表明, 化合物4c, 5b, 6b~6d, 7b等对HIV-1蛋白酶表现出了较高的抑制活性. 相似文献
4.
Rajani Kanta Behera Ajay Kumar Behera Rosy Pradhan Anita Pati Manabendra Patra 《合成通讯》2013,43(24):3729-3742
The reaction of thiobarbituric acid with different diarylidene ketones 1a–c yields the spiro compounds 2a–c. The diarylidene derivatives 3a–c are synthesized by the condensation of spiro compounds 2a–c with different aldehydes. A series of spiro heterocycles compounds 4a–l, 5a–l, 6a–l, 7a–l, 8a–l, and 9a–l are synthesized from the diarylidene compounds. The structures of the compounds are ascertained from their analytical and spectral data. Some of the compounds are screened for their biological activities. 相似文献
5.
Rasha A. M. Faty Hoda A. R. Hussein Ayman M. S. Youssef 《Phosphorus, sulfur, and silicon and the related elements》2013,188(7):1484-1490
3-Ethyl 2-amino-4-methyl-5-phenyl thiophene carboxylate 1 was used as a starting material to synthesize 2a,b via coupling with malononitrile or acetyl acetone, respectively. When heated, under reflux in sodium ethoxide solution, 2a,b give 3a,b. On the other hand, when compounds 3a,b were heated under reflux in ethanol with hydrazine hydrate, thiourea, or 1,1-phenylenediamine hydrochloride and a catalytic amount of piperidine 4a,b, 5a,b and 6a,b, were produced, respectively. The new compounds were tested for their antimicrobial activity. Compounds 2a–6b showed antibacterial activities, and 2a,2b and 4b showed antifungal activities. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. 相似文献
6.
Hai Shi Fang-Ming Liu Song-Wei Shen 《Phosphorus, sulfur, and silicon and the related elements》2013,188(2):263-270
Abstract A series of novel 3-aryl-5-(2-aryl-1,2,3-triazol-4-yl)-1-(4-aryl-2-thiazoyl)-pyrazolines 6a–6r were synthesized using 2-aryl-4-formyl-1,2,3-triazoles 1a,b as the starting materials. Thus, reacting 1a,b with 1-arylethanones 2a–2c gave 1-aryl-3-(2-aryl-1,2,3-triazol-4-yl)-2-propen-1-ones 3a–3f. The reaction of the latter with thiosemicarbazide afforded 3-aryl-5-(2-aryl-1,2,3-triazol-4-yl)-1-thiocarbamoyl-pyrazolines 4a–4f, which condensed with 2-bromo-1-arylethanones 5a–5c to afford the target compounds 6a–6r. The chemical structures of the compounds were verified by means of their IR, 1H NMR, ESI-MS spectroscopic data, and elemental analysis. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. GRAPHICAL ABSTRACT 相似文献
7.
New series of pyrazolo[3,4-b]pyridines were prepared and evaluated for antimicrobial activity toward six selected microorganisms. Compounds 2a, 3b, 3d and 3e exhibited good activity toward B. cereus. On the other hand, 2a and 3b evinced interesting activity over C. albicans, whereas 2a, 3b and 3e displayed promising activity over A. fumigatus. Antiquorum-sensing effectiveness of the new members over C. violaceum was also assessed, where compounds 2a and 3b exhibited higher activity than that of the reference compound, indole. In vitro antiproliferative assessment toward HepG2, HCT-116 and MCF-7 cancer cells evidenced that 2f has notable effectiveness on all examined cell lines, whereas 3a–c were active but to a lower extent. In vivo antitumor activity of 2f and 3a–c against EAC cells was also esteemed, where 2f and 3c showed considerable activity comparable to that of doxorubicin. Cytotoxicity screening over WI38 and WISH normal cells evinced that 2f and 3a–c are less cytotoxic than doxorubicin. Compounds 2a, 2f, 3a–c and 3e were evaluated for DNA-binding affinity and topoisomerase IIβ inhibitory activity. Analogs 2a, 2f, 3a and 3b illustrated strong DNA-binding affinity, whereas 2a, 2f and 3a exhibited interesting topoisomerase IIβ inhibitory activity. Compounds 2a and 2f were docked into topoisomerase IIβ, where 2f showed preferential binding to topoisomerase IIβ. Computational studies articulated that the new members are in compliance with Veber's standards and Lipinski’s rule. 相似文献
8.
A series of salicylidenimine functionalized p-tert-butylcalix[n]arene-core dendrimers 7a–b were synthesized in higher yields by divergent method from the corresponding ethyl p-butylcalix[n]arylacetates 2a–b (n = 6, 8). 2a–b were first treated with excess of 1,6-diaminohexane to give amide derivatives with free amine terminal groups 3a–b, which in turn reacted with salicylaldehyde in alcohol to yield the first generation of Schiff bases 4a–b. 3a–b reacted with ethyl acrylate, ammonolized with 1,6-diaminohexane and condonsated with salicylaldehyde successfully to give the second generation of Schiff bases 7a–b. The extraction and binding properties of the dentritic Schiff bases 4a–b and 7a–b for several kinds of metal ions were studied with UV–Vis spectroscopy and atomic absorption spectroscopy. In which they showed a great affinity for soft Cu2 + ions and formed 1:1 or 1:2 stoichiometric complexes. 相似文献
9.
N‐Arylaminomethyl‐3H‐1,3,4‐oxadiazole‐2‐thiones 2a,b were prepared from the corresponding N‐arylglycinoylhydrazides. A number of their thioglycoside derivatives 4–7a–c and S‐functionalized analogs 8–11a,b were synthesized by the reaction with different acetobromosugars and acyclic hydroxyalkylating agents. The antiviral activity of a number of the synthesized compounds against herpes simplex virus type 1 (HSV‐1) and hepatitis A virus (HAV) was evaluated. Compounds 5a and 5b showed promising results against HAV. 相似文献
10.
Mohamed A. A. Elneairy Sanaa M. Eldin Mohamed F. M. Attia 《Phosphorus, sulfur, and silicon and the related elements》2013,188(7):1346-1357
Pyridine-2(1H)-thione derivatives 3a,b were synthesized from the reaction of 1-(phenyl-sulfanyl)acetone (1) and cinnnamonitrile derivatives 2a,b. Compounds 3a,b reacted with different halogenated reagents 7a–f to give 2-S-alkylpyridine derivatives 8a–l, which could be, in turn, cyclized into the corresponding thieno[2,3-b]pyridine derivatives 9a–l. Compounds 9d,j reacted with acetic anhydride, formic acid, carbon disulfide, phenyl isothiocyanate, and nitrous acid to yield the corresponding pyrido[3′,2′:4,5]thieno[2,3-d]pyrimidine 12a,b, 15a,b, 17a,b, 20a,b, and pyrido[3′,2′:4,5]thieno[2,3-d][1,2,3]triazinone derivatives 22a,b, respectively. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. 相似文献
11.
Acetyl benzofurans 1a, 1b reacted with isatins 2a–2f in the presence of pyridine to give corresponding 3-[2-(1-benzofuran-2-yl)-2-oxoethyl]-3-hydroxy-1,3-dihydro-2H-indol-2-one derivatives 3a–3l. Dehydration of the latter in acidic media led to the corresponding α,β-unsaturated ketones 4a–4l. The structures of newly synthesized compounds 3a–3l and 4a–4l were established on the basis of analytical and spectral data. The synthesized compounds were screened for their antibacterial and antifungal activities. Compounds 5d, 5f, and 5h displayed excellent antimicrobial activity. The synthesized compounds were studied for docking on the enzyme, Glucosamine-6-phosphate Synthase. 相似文献
12.
2‐Phenyl‐1,1,3‐tricyano‐3‐bromopropene 1 reacts with the aromatic amines 2a–f and 6a–c to afford the N‐substituted pyrroles 4a–d, the pyrrolo[1,2‐a]quinazoline derivatives 5a, b, and the diaza‐as‐indacene derivatives 7a–c and 8a–c, presumably via elimination of hydrogen bromide followed by cyclization of the formed acyclic intermediates. All structures are confirmed by analytical and spectral data. 相似文献
13.
Dihydrobenzo[h]coumarins (5a–7a) and their 4‐methyl analogs (5b–7b) were synthesized from 1‐naphthol via two different synthetic routes. One pathway is the direct condensation of 5,8‐dihydro‐1‐naphthol (9) with malic acid or ethyl acetoacetate, affording 7,10‐dihydrobenzo[h]coumarins 7a and 7b, respectively. The other is through the oxidation of 7,8,9,10‐tetrahydrobenzo[h] coumarins (15a–b), followed by the reduction of the carbonyl group and dehydration of hydroxyl group, giving 7,8-dihydrobenzo[h]coumarins (5a, b) and 9,10-dihydrobenzo[h]coumarins (6a, b). The regio selectivities for the oxidation reactions of 15a, b were rationalized on the basis of quantum chemical calculations and further confirmed by the X‐ray crystallographic analysis of the derivatives of oxidation products. 相似文献
14.
Etify A. Bakhite Abdu E. Abdel-Rahman Elham A. Al-Taifi 《Phosphorus, sulfur, and silicon and the related elements》2013,188(3):513-520
5-Acetyl-3-amino-4-aryl-6-methylthieno[2,3-b]pyridine-2-carboxamides (1a, b) were reacted with aromatic aldehydes or with some cycloalkanones to give the corresponding tetrahydropyridothienopyrimidinone derivatives 2a–f and 4a–d . The reaction of compound 1b with urea and/or carbon disulfide has been carried out and their products were identified. Some representative compounds were screened in vitro for their antimicrobial activities. 相似文献
15.
E. M. Keshk A. A. Abu-Hashem M. M. Girges A. H. Abdel-Rahman F. A. Badria 《Phosphorus, sulfur, and silicon and the related elements》2013,188(8):1577-1593
Benzo[1,2-b:5,4-b′]difuran-2-carbohydrazides 5a, b were reacted with aryl or alkyl isothiocyanates to give the corresponding thiosemicarbazides 6a–h. Cyclization of the substituted thiosemicarbazides with sodium hydroxide led to the formation of benzo[1,2-b:5,4-b′]difuranyl-1,3,4-triazoles 7a–f. Desulfurization of thiosemicarbazides by mercuric oxide gave benzo[1,2-b:5,4-b′]difuranyl-1,3,4-oxadiazoles 8a–f. Treatment of thiosemicarbazides with ethyl bromoacetate or α-bromopropionic acid yielded benzo[1,2-b:5,4-b′]difuranyl-carbonyl-hydrazono-4-thiazolidinones 9a–f and 10a–f, respectively. Furthermore, the reaction of the thiosemicarbazides with phosphorus oxychloride gave benzo[1,2-b:5,4-b′]difuranyl-1,3,4-thiadiazoles 11a–f. Some compounds in this study were biologically evaluated for their ability to bind to DNA. 相似文献
16.
Youssef L. Aly Ashraf A. El-Shehawy Adel M. Attia Mohmed E. Sobh 《Phosphorus, sulfur, and silicon and the related elements》2013,188(7):1572-1584
Abstract 5-Anthracenylidene- and 5-(4-benzyloxy-3-methoxy)benzylidene-hydantoin and 2-thiohydantoin derivatives 3a-g were prepared by condensation of anthracene-9-carboxaldehyde and 4-benzyloxy-3-methoxybenzylaldehyde with hydantoin and 2-thiohydantoin derivatives. Compounds 3a, b, f undergo Mannich reaction with formaldehyde and morpholine to give the corresponding Mannich products 4a–c. For the synthesis of alkylmercaptohydantoin 5a–o, the potassium salt of compounds 3a, b, e, f were reacted with an alkylhalide, either methyl iodide, phenacyl bromide, ethyl bromo acetate, allyl bromide, or methallyl bromide, under stirring at room temperature to afford the alkylmercaptohydantoins 5a–o. Acid hydrolysis of compounds 5a–c afforded the corresponding arylidene-hydantoin derivatives 3c, d, g. 2-Methylmercapto-hydantoin derivatives 5a, c were reacted with some secondary amines such as morpholine or piperidine to afford 5-(4-benzyloxy-3-methoxy)benzylidene-2-morpholino- or piperidino glycocyamidine derivatives 7a, 5-anthracenylidene-2-morpholin-, or piperidino glycocyamidine derivatives 7b, c. Supplemental materials are available for this article. Go to the publisher's online edition of Phosphorus, Sulfur, and Silicon and the Related Elements to view the free supplemental file. GRAPHICAL ABSTRACT 相似文献
17.
Cemil İbiş Nihal Yılmaz 《Phosphorus, sulfur, and silicon and the related elements》2013,188(12):2543-2548
Compounds 3a–c, 4a, b, 5a–c, and 6a, c were obtained from the reactions of perchlorobutadiene (1) with 1,4-butanedithiol (2a), 1,5-pentanethiol (2b), and 2.2′-(ethlene-dioxyl)diethanethiol (2c) in ethanol in the presence of sodium hydroxide. Compounds 7a, b were obtained from the reactions of thioethers 3a, b with m-chlorperbenzoic acid in CHCl 3 . 相似文献
18.
P. Haranath V. Sreedhar Kumar C. Suresh Reddy C. Naga Raju C. Devendranath Reddy 《合成通讯》2013,43(10):1697-1708
6‐Substituted‐dibenzo[d, f][1,3,2]dioxaposphepin‐6‐oxides, sulfides, and selenides (5a–i, 6a–d, and 7a–d) were synthesized by reacting 2,2′‐biphenol (1) with phosphorus tribromide in the presence of triethylamine at 0–30°C and subsequent reaction of the monobromide (2) with different Grignard reagents (3) at room temperature. The products (4) were converted to corresponding oxides, sulfides, and selenides (5a–i, 6a–d, and 7a–d) by oxidation with H2O2 at room temperature and refluxing with sulfur and selenium respectively. The chemical structures of all the products were confirmed by analytical, IR, NMR (1H, 13C, and 31P), and mass spectral data. Most of these compounds exhibited moderate antimicrobial activity. 相似文献
19.
Twelve angular oxazole-fused coumarin derivatives were designed, synthesised and characterised by 1H NMR, 13C NMR and HRMS. The structure of compound 4a was further confirmed by X-ray single-crystal diffraction. The bioassay experiment results indicated that compounds 4f and 4l have high antifungal activity on the mycelium growth of 4 plant disease fungi. Especially, compound 4l has a stronger antifungal activity compare to the commercial fungicide, Carbendazim. The herbicidal activity experiment showed that 4a and 4b can significantly inhibit the taproot and caulis development of Chenopodium album seedling and have better activities than the commercial herbicide, Acetochlor. 相似文献
20.
Fawzy A. Attaby Sanaa M. Eldin Mohamed A. A. Elneairy Ali K. K. El-Louh 《Phosphorus, sulfur, and silicon and the related elements》2013,188(11):2205-2220
Cyanothioacetamide (f 1) reacted with α,β -unsaturated carbonyl compounds 2a–d to afford thioxohydropyridine-3-carbonitriles 5a–d, which were used as the starting materials for the preparation of several thienopyridines via their reactions with active halogen-containing compounds, e.g., 2-bromo-1-phenylethanone (7a), 2-bromo-1-p-tolyl-ethanone (7b), chloroacetone (10a), α -chloroacetylacetone (10b), and chloroacetic acid ethyl ester (13). The structure of the newly synthesized heterocyclic compounds were established based on the data of elemental analyses, IR, 1 H NMR, and mass spectra. 相似文献