共查询到20条相似文献,搜索用时 15 毫秒
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M Kajino K Mizuno H Tawada Y Shibouta K Nishikawa K Meguro 《Chemical & pharmaceutical bulletin》1991,39(11):2888-2895
New 2H-1,4-benzothiazin-3(4H)-one derivatives possessing (4-phenyl-1-piperazinyl)alkyl moieties at the 2-position were synthesized and tested for calcium antagonistic and calmodulin antagonistic activities. Antihypertensive effects in spontaneously hypertensive rats were also evaluated. In general, these compounds were rather weak calcium channel blockers, although, in contrast, many of them had moderate to potent calmodulin antagonistic activity, and 2-[3-(4-(4-fluorophenyl)-1-piperazinyl]propyl]-2H-1,4-benzothiazin -3 (4H)-one derivatives 45, 74 and 75 showed potent antihypertensive effects. 相似文献
3.
Salvatore Cabiddu Costantino Floris Stefana Melis Francesca Sotgiu Giovanni Cerioni 《Journal of heterocyclic chemistry》1986,23(6):1815-1820
Benzocondensed six-membered heterocyclic rings containing two heteroatoms have been synthesized by a generally applicable method starting from disubstituted benzene compounds and methyl 4-chlorobutynoate ( 1 ) or methyl 4-bromobutenoate ( 2 ). The reactions with 1 yield a mixture of endo and exo (E or Z) isomers. The 13C nmr spectroscopy was used to assign the structure of the synthesized compounds. 相似文献
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Cyril Párkányi Abdou O. Abdelhamid Ahmad S. Shawali 《Journal of heterocyclic chemistry》1984,21(2):521-524
Arylazo derivatives of quinoxaline (1,4-benzodiazine), 1,4-benzothiazine, and 1,4-benzoxazine have been prepared by condensation of hydrazidoyl halides with o-phenylenediamine, o-aminothiophenol, and o-aminophenol, respectively (Table I). This method seems to be more general than the approach using coupling of reactive diazonium salts with, e.g., 277–1,4-benzothiazine. Both the spectral data and the results of HMO calculations of bonding energies of the azo compounds obtained in this study indicate that they exist predominantly in the hydrazone tautomeric form. 相似文献
6.
The review considers recent advances in using diethanolamine (DEA) in the synthesis of amides, polymerization reactions, and synthesis of heterocycles, crown ethers, Mannich bases, and ionic liquids. Biological activity of DEA and its derivatives is also reviewed. 相似文献
7.
B. Steiner M. Koóš M. Matulová B. Proksa 《Monatshefte für Chemie / Chemical Monthly》1993,124(4):425-430
Summary 2-Aminothiophenol (1) reacts with 3-chloro-2,4-pentanedione (2) in the presence of pyridine to form 2-acetyl-3-methyl-4H-1,4-benzothiazine (3) in high yields. Reaction of3 with hydrazine gives 4-(2-aminophenylthio)-3,5-dimethylpyrazole (5). Condensation of3 with 4-nitrobenzaldehyde yields the corresponding Schiff base7. Hydroxylamine with benzothiazine3 affords 3,9a-dimethyl-3a, 9a-dihydro-9H-isoxazolo[4,5-b][1,4]benzothiazine (8).
Synthese von 2-Acetyl-3-methyl-4H-1, 4-benzothiazin und seinen Derivaten
Zusammenfassung 2-Aminothiophenol (1) reagiert mit 3-Chlor-2,4-pentandion (2) in Anwesenheit von Pyridin unter Bildung von 2-Acetyl-3-methyl-4H-1,4-benzothiazin (3) in sehr hoher Ausbeute. Benzothiazin3 kondensiert mit Hydrazin zu 4-(2-Aminophenylthio)-3,5-dimethylpyrazol (5), dessen Aminogruppe reagiert mit 4-Nitrobenzaldehyd zu einer Schiffschen Base (7), die spektroskopisch charakterisiert wurde. Benzothiazin3 mit Hydroxylamin ergibt 3,9a-Dimethyl-3a,9a-dihydro-9H-isoxazolo[4,5-b][1,4]benzothiazin (8). Die Stereochemie der letztgenannten Verbindung wurde ermittelt.相似文献
8.
2-Aminobenzenethiol was condensed with alkyl α-chlorophenylhydrazonoglyoxylates yielding alkyl 2-(2-aminophenylthio)-2-arylhydrazonoglyoxylates which were cyclized to the corresponding 2-arylhydrazono-2,3-dihydro-4H-1,4-benzothiazin-3-ones. Starting from α-chloro-α-arylhydrazonoacetones the corresponding 2-arylhydrazono-3-methylbenzo-1,4-benzothiazines were formed. 相似文献
9.
F. A. Yassin 《Chemistry of Heterocyclic Compounds》2009,45(1):35-41
The reaction of 2-chloro-4,6-dimethylpyridine-3-carbonitrile with hydrazine hydrate, hydroxylamine, and anthranilic acid afforded
the corresponding pyrazolo, isoxazolo, and pyridoquinazoline derivatives. Alkylation of 2-mercapto-4,6-dimethylpyridine-3-carbonitrile
with ethyl chloroacetate or phenacyl bromide followed by cyclization in NaOH gave thienopyridine derivatives. Diazotization
of ethyl 3-amino-4,6-dimethylthiеno[2,3-b]pyridine-2-carboxylate followed by the reaction with thiourea, guanidine carbonate,
and hydroxylamine hydrochloride gave the corresponding thienopyridine derivatives. The biological activity of some new compounds
has been discussed.
Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 1, pp. 43–51, Januar, 2009. 相似文献
10.
H Tawada Y Sugiyama H Ikeda Y Yamamoto K Meguro 《Chemical & pharmaceutical bulletin》1990,38(5):1238-1245
N-Acetic acid derivatives (I) of 2-substituted 1,4-benzoxazines and benzothiazines were designed and synthesized for evaluation as new aldose reductase inhibitors. In general, 3-thioxo derivatives were more potent inhibitors of aldose reductase from human palcenta in vitro than the corresponding 3-oxo derivatives. While many compounds (I) were not very effective in inhibiting sorbitol accumulation in the rat sciatic nerve in vivo, the 3-thioxo compounds bearing an isopropyl group at the 2-position showed highly potent activity in the in vivo assay. Compound 46 (AD-5467) was selected from this series as a candidate for further development. 相似文献
11.
Jnos Szab Ernest Bani-Akoto Gyrgy Dombi Gbor Bernth Lajos Fodor PL Sohr 《Journal of heterocyclic chemistry》1992,29(6):1513-1517
The ring-closure reactions of N-(3,4-dimethoxyphenylthiomethyl)-2-nitrobenzamide derivatives 5a,b with phosphoryl chloride gave 4-(2-nitrophenyl)-2H1,3-benzothiazine derivatives 7a,b , which on reduction yielded 4-(2′-aminophenyl)-3,4-dihydro-2H-1,3-benzothiazines 8a,b. Reaction of these compounds with phosgene led to a new heterocyclic ring system, 6H,8H-quinazolino[3,4-c][1,3]benzothiazine derivatives 9a,b. The structures of the title compounds were proved via their ir and nmr (1H, 13C) spectra. 相似文献
12.
Nada Kheira Sebbar Mohamed El Mehdi Mekhzoum El Mokhtar Essassi Abdelfettah Zerzouf Ahmed Talbaoui Youssef Bakri Mohamed Saadi Lahcen El Ammari 《Research on Chemical Intermediates》2016,42(9):6845-6862
In order to develop relatively small molecules as pharmacologically active molecules, novel 1,4-benzothiazine derivatives with triazole and oxazolidinone were synthesized. In this study, a series of 1,2,3-triazolylmethyl-1,4-benzothiazine derivatives were developed by exploiting a click chemistry reaction using a CuI-catalyzed Huisgen [3 + 2] cycloaddition. Starting from 2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one, a number of 1,4-benzothiazine derivatives were also synthesized using different alkylating agents to give a 4-(substituted)-2-(substituted)-3,4-dihydro-2H-1,4-benzothiazi-3-one in good yields. The crystal and molecular structure of compound oxazolidin-2-one in basic benzothiazine was established by single-crystal X-ray diffraction. The newly synthesized products were subjected to in vitro biological evaluation. The result indicated that the compounds show convincing antibacterial activities against different microorganisms. All structures of the synthesized compounds were elucidated on the basis of spectral analyses and chemical reactions. 相似文献
13.
This review deals with the synthesis, reactions and biological activity of pyrazoloquinazoline derivatives. Some of these reactions have been used successfully to the production of biologically importance compounds. The main purpose of this review is to present a survey of the literature on the chemistry of pyrazoloquinazolines and provides useful applications for these compounds. 相似文献
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This review describes the synthesis and reactions of naproxen derivatives and highlights the effects of compounds containing the naproxen moiety in important biological applications. 相似文献
15.
A. K. Mansour Mohga M. Eid R. A. Hassan A. Haemers S. R. Pattyn D. A. Vanden Berghe L. Van Hoof 《Journal of heterocyclic chemistry》1988,25(1):279-283
6-Substituted benzyl-4-phenyl-3-thioxo-2,3,4,5-tetrahydro-1,2,4-triazin-5-ones 3a-d were prepared and converted into their corresponding 3-methylthio derivatives 4a-d . Reaction of compounds 4a-d with hydrazine hydrate gave the corresponding 4-amino-3-anilino-4,5-dihydro-1,2,4-triazin-5-ones 5a-d . 6-Substituted benzyl-4-phenyl-2,3,4,5-tetrahydro-1,2,4-triazin-3,5-diones 9a-c were synthesized and allowed to react with hydrazine hydrate to give the corresponding 6-substituted benzyl-4-amino-2,3,4,5-tetrahydro-1,2,4-triazin-3,5-diones 10a-c . The biological evaluation of some of these triazines is described. All compounds were screened for antiviral, antibacterial, antimycobacterial, antifungal and antiyeast activity. No important biological activity was found. 相似文献
16.
Andrey P. Mityuk Oleksandr P. Dacenko Pavel K. Mykhailiuk Dmitriy M. Volochnyuk 《Tetrahedron letters》2010,51(13):1790-12599
A series of bridged 1,4-diazepanes (i.e., diazabicyclo[n.3.2]alkanes, n = 3-5) selectively protected at one of the nitrogen atoms was prepared, for possible application in drug design, via Schmidt rearrangement of the corresponding ketones. 相似文献
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This review covers the total asymmetric synthesis and biological evaluation of derivatives of the marine natural products known as the apratoxins. 相似文献
18.
磺酰胺类化合物是继磺酰脲与咪唑啉酮除草剂之后开发的乙酰乳酸合成酶 (ALS)抑制剂的另一重要领域 ,已筛选出一些高活性的新品种[1~ 3] 。为寻找新的性能优良的活性物质 ,进一步研究活性与结构的关系 ,本文设计将磺酰胺类和酰胺类除草剂的基本骨架用一个亚甲基 CH2 连结起来 ,相当于在磺酰脲桥链中间插入了一个亚甲基 ,共合成了 1 6个新的邻烷氧基羰基苯磺酰胺衍生物( 2a~ 2p) ,并初步测试了它们的生物活性。1 实验部分1 1 仪器和试剂JEOLFX 90Q型、BRUKERAC P2 0 0型核磁共振仪 ,TMS为内标 ;Shimad… 相似文献
19.
Reaction of dithioacid (ArCS2CH2CO2H, Ar = phenyl, 2‐furyl or 2‐thienyl) with nBu2SnO gives monomeric (ArCS2CH2CO2)2Sn(Bun)2 in a 2:1 molar ratio, and dimeric {[(ArCS2CH2CO2)Sn(Bun)2]2O}2 in a 1:1 molar ratio, respectively, which have been characterized by IR, NMR (1H, 13C and 119Sn) spectra and elemental analyses. X‐ray crystal structure analyses indicate that the compound [(C4H3S)CS2CH2CO2]2Sn(Bun)2 is monomeric with the tin atom occupying a skew‐trapezoidal bipyramidal geometry. In addition, this compound forms a three‐dimensional structure through the weak intermolecular S…S and Sn…O interactions. Compound {[((C4H3S)CS2CH2CO2)Sn(Bun)2]2O}2 is a centrosymmetric dimer with a cyclic Sn2O2 unit, in which the coordination modes of the two crystallographically unique carboxylic ligands are different. One acts as monodentate ligand by the carboxylate oxygen atom, the other bridges two tin atoms via only one carboxylate oxygen atom. Furthermore, each tin atom in this compound locates a distorted trigonal bipyramidal geometry. Biological activities of these organotin compounds show that they have hardly acaricidal activity, but display certain activities on fungi. In mononuclear tin compounds, the inhibition percentage of [(C4H3S)CS2CH2CO2]2Sn(Bun)2 in vitro for Alternaria solani and Physolospora piricola is 57.1% and 43.9%, respectively, while in dimers {[((C4H3O)CS2CH2CO2)Sn(Bun)2]2O}2 shows high inhibition percentage for Gibbereila zeae (52.6%) and Physolospora piricola (50.0%), respectively. Copyright © 2006 John Wiley & Sons, Ltd. 相似文献
20.
Pyrrolidine-2,3-diones are of continuing interest as intermediates in the synthesis of heterocycles related to pyrrolidine alkaloids, medicinally relevant compounds, and in the development of antibiotics and drugs. The present review deals with the most important literature on the synthesis and reactions of pyrrolidine-2,3-diones and the related biologically important compounds. 相似文献