共查询到20条相似文献,搜索用时 15 毫秒
1.
O Muraoka S Ying K Yoshikai Y Matsuura E Yamada T Minematsu G Tanabe H Matsuda M Yoshikawa 《Chemical & pharmaceutical bulletin》2001,49(11):1503-1505
A nitrogen analogue 4 of the naturally occurring sulfonium ion salacinol (1), a potent alpha-glucosidase inhibitor isolated from the Ayruvedic medicine Salacia reticulata, was synthesized and its inhibitory activity against alpha-glucosidase tested. Substitution of the sulfur atom in 1 with a nitrogen reduced the activity considerably. The solid-state stereostructure of the related compound (5) was determined on the basis of single crystal X-ray measurement. 相似文献
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zlem AKGÜL Mümin Alper ERDOAN Dervi BRM ala KAYABAI Cumhur GÜNDÜZ Güliz ARMAAN 《Turkish Journal of Chemistry》2020,44(6):1674
In this study, a group of 4-substituted benzoyltaurinamide derivatives were designed, synthesized, and investigated for their anticancer activity against three cancer cell lines and one nontumorigenic cell line by MTT assay. Among the final compounds, methoxyphenyl derivatives 14, 15, 16 were found to be effective against all the tested cancerous cell lines with promising selectivity. The most active compounds were further evaluated to determine the molecular mechanism of their anticancer activity by using western blot assay and the Annexin V-FITC/PI test. Compound 14 (in SH-SY5Y and MDA-MB-231 cell lines) and 15 (in SH-SY5Y cell line) were found to induce intrinsic apoptotic pathway by upregulating BAX, caspase-3, and caspase-9, while downregulating Bcl-2 and Bcl-xL expression levels. According to mechanistic studies, compounds displayed their anticancer activity via three different mechanisms: a. caspase-dependent, b. caspase-independent, and c. caspase-dependent pathway that excluded caspase-9 activation. As a result, this study provides interesting data which can be used to design new taurine-based anticancer derivatives. 相似文献
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A series of new thiazoline derivatives 2-alkyl(aryl) imino-4-amino-5-ethoxycarbonyl-3-phenyl-3Hthiazoline (3) and bis(2-imino-4-amino-5-ethoxycarbonyl-3-phenyl-3H-thiazoline alkylene (4) have been synthesized by reactions of intermediate 4-amino-5-ethoxycarbonyl-2-methylthio-3-phenyl-3H-thiazolinium sulphate (2) with alkylamines or arylamine in 64%-89% yields. The structures of 3 and 4 have been confirmed by 1H NMR, EI-MS, IR spectroscopy and elemental analyses. Some compounds exhibited high or moderate herbicidal activities against the roots of rapeseed and barnyard grass at 100 mg/L. 相似文献
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Kenchappa R. Bodke Yadav D. Telkar Sandeep Sindhe M. Aruna Giridhar M. 《Russian Journal of General Chemistry》2016,86(12):2827-2836
Russian Journal of General Chemistry - A novel series of (5-substituted-1-benzofuran-2-yl)(2,4-substituted phenyl)methanones (4a–4i) have been prepared by the Knoevenagel condensation of... 相似文献
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Russian Journal of General Chemistry - Quinazolinylbenzoic acid 1 was used as a precursor for synthesis of many heterocyclic systems. Ethyl 4-[4-oxo-2-phenylquinazolin-3(4H)-yl]benzoate 2 upon... 相似文献
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Silvia Prez Berta Lasheras Carmen Oset Antonio Monge 《Journal of heterocyclic chemistry》1997,34(5):1527-1533
New indolyl-1,3,4-oxadiazole and oxadiazine derivatives were prepared as reversible monoamine oxidase inhibitors. The compound 5-(3-methylindolyl)-1,3,4-oxadiazol-2(3H)one was shown to be a good monoamine oxidase B inhibitor. 相似文献
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The reactions of N-substituted maleimides with aminouracils and derivatives of aniline were carried out. The structures of
the synthesized compounds were verified by the data from elemental analysis and by the UV, IR, and 1H NMR spectra. The physicochemical characteristics, toxicity, and biological activity of the new compounds were studied.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 828–833, June, 2007. 相似文献
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Gang Liu Chunping Liu Lin Sun Rongjun Qu Hou Chen Chunnuan Ji 《Chemistry of Heterocyclic Compounds》2007,43(10):1290-1300
A series of N-substituted 4-amino-6,7,8-trimethoxyquinazoline derivatives has been synthesized from 4-chloro-6,7,8-trimethoxyquinazoline
and aryl (or benzyl) amines using 2-propanol as a solvent. The starting material 4-chloro-6,7,8-trimethoxyquinazoline has
been synthesized from natural gallic acid by a novel route. Their structures have been verified by elemental analysis and
IR, 1H, and 13C NMR spectroscopy. The title compounds have been evaluated for their in vitro antiproliferative activities against some cancer
cells by the MTT method. Unfortunately, most of the compounds tested have exhibited a weaker anticancer activity than the
reference standard drug PD153035.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, 1521–1531, September, 2007. 相似文献
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A synthesis of all possible N-alkylated 2-n-butyl-imidazo[4,5]pyridine isomers is described as well as their structural assignment by 1H NMR spectroscopy. One of these derivatives, 2,-n-butyl-3-[2′- (1H-tetrazol-5-yl)-4-biphenylylmethyl]-3H-imidazo[4,5-b]pyridine 9 is a potent angiotensin II receptor antagonist. 相似文献
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Vartanyan S. O. Avakyan A. S. Sargsyan A. B. Kerobyan M. O. Arutyunyan S. A. Gukasyan T. G. 《Russian Journal of Organic Chemistry》2017,53(12):1905-1908
Russian Journal of Organic Chemistry - Intramolecular cyclization of 2-(2,3-dihydro-1,4-benzodioxine-2-carbonyl)hydrazine-1-carbothioamide by the action of concentrated sulfuric acid gave... 相似文献
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H. Foks D. Pancechowska-Ksepko W. Kuzmierkiewicz Z. Zwolska E. Augustynowicz-Kopec M. Janowiec 《Chemistry of Heterocyclic Compounds》2006,42(5):611-614
The reactions of o-phenylenediamine and 3,4-diaminotoluene with such acids as 3-cyclohexylpropionic, 4-phenylbutyric, 4-cyclohexylbutyric,
3,3-diphenylpropionic, and 3,4-dimethoxyphenylacetic resulted in the formation of the corresponding 2-substituted benzimidazoles.
These compounds were transformed into methane-and benzenesulfonamide derivatives. The benzimidazole derivatives obtained were
tested in vitro for their tuberculostatic activity. Compounds with good activity (MIC 6.2-25 μg/ml) have been found.
Published from Khimiya Geterotsiklicheskikh Soedinenii, No. 5, pp. 697–700, May, 2006. 相似文献
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Two methods for preparing 4-aminoquinuclidine from quinuclidine-4-carboxylic acid have been developed. Acyl and alkyl derivatives of 4-aminoquinuclidine have been synthesized. 相似文献
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Magorzata Szczesio Katarzyna Gobis Izabela Korona-Gowniak Ida Mazerant-Politowicz Dagmara Ziembicka Henryk Foks Marek Gwka Andrzej Olczak 《Acta Crystallographica. Section C, Structural Chemistry》2020,76(7):673-680
Four new picolinohydrazonamide derivatives, namely, 6‐methyl‐N′‐(morpholine‐4‐carbonothioyl)picolinohydrazonamide, C12H17N5OS, 6‐chloro‐N′‐(morpholine‐4‐carbonothioyl)picolinohydrazonamide methanol monosolvate, C11H14ClN5OS·CH3OH, 6‐chloro‐N′‐(4‐phenylpiperazine‐1‐carbonothioyl)picolinohydrazonamide, C17H19ClN6S, and 6‐chloropicolinohydrazonamide, C6H7ClN4, have been synthesized and characterized by NMR spectroscopy and single‐crystal low‐temperature X‐ray diffraction. In addition, their antibacterial and anti‐yeast activities have been determined. The first three compounds adopt the zwitterionic form in the crystal structure regardless of the presence or absence of solvent molecules in the structure. They also adopt the same symmetry, i.e. P21/c (P21/n), unlike the fourth structure which is chiral and has the space group P212121. For all the studied cases, intermolecular N—H…O and N—H…N hydrogen bonds play an essential role in the formation of the structures. 相似文献
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Mohamed A.A. Radwan Osamah Al Rugaie Waleed Al Abdulmonem Mohammad Y. Alfaifi Serag Eldin I. Elbehairi 《Arabian Journal of Chemistry》2021,14(7):103209
The current approach described the synthesis of a new series of indolylpyrrole derivatives through multicomponent reaction of α-cyano chalcones, appropriate aldehydes, and ammonium acetate in refluxed acetic acid. The chemical structures of the designed compounds were confirmed with spectroscopic data and elemental analysis and then tested for their in vitro cytotoxic activity by SRB assay method towards three cell lines involving human Prostate adenocarcinoma; metastatic cells (PC-3), human ovary adenocarcinoma (SKOV3) and human dukes' type B, colorectal adenocarcinoma (LS 174 T). Most significant activity provided with compounds 5c, 5h and, 5j against prostate cancer cells (PC-3) with IC50s of 3.30 ± 0.20, 3.60 ± 0.10, and 3.60 ± 0.90 µg/ml, respectively. In human ovarian carcinoma (SKOV3), the compounds 5a, and 5i have stronger cytotoxicity with IC50s of 1.20 ± 0.04, 1.90 ± 0.50 µg/ml, respectively than the standard doxorubicin (IC50 = 2.20 ± 0.02 µg/ml). On the other hand, only compound 5a has the ability to diminish the viability of LS174T cells in an active manner with IC50 2.80 ± 0.10 µg/ml. Consequently, this effort offers groundwork for additional examination of nominated indolylpyrroles as antiproliferative agents. 相似文献
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Summary Some N-substituted derivatives of diethyl phosphoramidate are described. They were prepared by the action of various halogen compounds on the N-sodium derivative of diethyl N-methylphosphoramidate. 相似文献
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Three pairs of N-substituted normorphine derivatives and the sulfate conjugates at the 6-position were tested for the analgesic and antagonistic activities and the development of physical dependence in mice. The compounds examined were nalorphine, nalorphine-6-sulfate (N-6-S), N-cyclopropylmethylnormorphine (CPN), N-cyclopropylmethylnormorphine-6-sulfate (C-6-S), N-dimethylallylnormorphine (DMN) and N-dimethylallylnormorphine-6-sulfate (D-6-S). The latter two pairs were newly synthesized. The analgesic activity of C-6-S and D-6-S was equipotent to that of CPN and DMN by the acetic acid writhing test on the s.c. injection, and the activity of N-6-S was about 2 times more potent than that of nalorphine. The antagonistic activity of N-6-S, C-6-S and D-6-S to morphine analgesia was higher than that of the parent compounds by the tail pinch test on i.c.v. injection. A withdrawal sign was seen in mice treated chronically with CPN, C-6-S and N-6-S by challenge with naloxone, whereas the mice treated with DMN, D-6-S and nalorphine showed no such sign. The effect of sulfation at the 6-position on the development of physical dependence was not well associated with the effect on agonistic and antagonistic activities. 相似文献
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A number of acylthioureas, 2-((4-methylphenoxy)methyl)-N-(aryl-carbamothioyl)benzamides (aryl = 3,5-dichlorophenyl, 2,3-dichlorophenyl, 3,4-dichloro-phenyl, 2,4,5-trichlorophenyl, 3,4,5-trichlorophenyl, 2-bromophenyl, 2,4-dibromophenyl, 2,5-dibromophenyl, 2-iodophenyl, 3-fluorophenyl, 2,3,4-trifluorophenyl, 2,4,5-trifluoro-phenyl, 2,4,6-trifluorophenyl) have been synthesized, characterized by elemental analysis, IR and NMR spectroscopy and tested for their interaction with bacterial cells in free and adherent state. The anti-pathogenic activity was correlated with the presence of one iodine, bromide or fluorine, and two or three chloride atoms on the N-phenyl substituent of the thiourea moiety, being significant especially on Pseudomonas aeruginosa and Staphylococcus aureus strains, known for their ability to grow in biofilms. Our results demonstrate the potential of these derivatives for further development of novel anti-microbial agents with antibiofilm properties. 相似文献