[Dioxolanone and related compounds. II. Synthesis of 7-(2,3-dihydroxy-propyl)theophylline derivatives. (Studies on the synthesis of heterocyclic compounds. CCII)].
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Theophylline↗
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Results for “Heterocyclic Compounds”
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5-N-acetylardeemin, a novel heterocyclic compound which reverses multiple drug resistance in tumor cells. II. Isolation and elucidation of the structure of 5-N-acetylardeemin and two congeners.
A family of novel compounds has been detected and isolated following an assay for the attenuation of multiple drug resistance in tumor cells from the fermentation broth and mycelia of a strain of Aspergillus fischeri which we have designated var. brasiliensis. The structures of three components were determined employing 1-D and 2-D homonuclear and heteronuclear NMR spectroscopy and mass spectrometry. The structure of 5-N-acetylardeemin was confirmed by single crystal X-ray diffraction. These compounds are most closely structurally related to asperlicin E1).
Antibiotics, Antineoplastic↗
Condensed heterocyclic compounds: synthesis and antiinflammatory activity of novel thiazolo[3,2-alpha] pyrimidines.
In this study, thirty six new 2-benzylidene-7-methyl-3-oxo-5- phenyl-2,3-dihydro-5H-thiazolo[3,2-alpha]pyrimidine-6-carboxylic acid methyl esters were synthesized and characterized by spectral, crystallographic, and elemental analysis. The antiinflammatory activity of the compounds was tested by the carrageenan hind paw edema test. It was found that compound 6a having a 2-meth-oxyphenyl group at position 5 and a benzylidene group at position 2 was the most potent compound in this series. All the compounds that were tested for ulcer activity gave positive results.
Animals↗
Research on heterocyclic compounds. Phenyl derivatives of fused imidazole systems: antiinflammatory activity.
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Animals↗
Anticonvulsive activity of indenoimidazolidinones and related heterocyclic compounds in mice.
A series of substituted cyclic ureides and related compounds, one of them a thio analog, were synthesized by condensing ninhydrin with urea, thiourea, dimethylurea or other aromatic or bifunctional agents. When tested against seizures induced in mice by the chemoconvulsant Metrazol or against audiogenic seizures, four compounds decreased either the incidence or the severity of convulsive manifestations and protected from mortality in seizures. The effective compounds were not toxic at the administered level (150 mg/kg) and produced few observable sedative effects.
Acoustic Stimulation↗
Research on heterocyclic compounds. Antiinflammatory activity of some imidazo(1,2-c)pyrimidine derivatives.
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Animals↗
Physiologically active substances from marine sponges IV: Heterocyclic compounds.
Several guanidine compounds were synthesized by the reaction of acid chlorides of thiophene and furan with guanidines. Some of these compounds showed antibiotic and cytotoxic activities. Series of pyrrole compounds were synthesized and found to have significant antibiotic activity.
Animals↗
[Research on heterocyclic compounds. I. Heteroarylacetic acids with anti-inflammatory action].
Some new heteroarylacetic acids were prepared. Among the products so far obtained, 2-imidazo [1,2-a] pyrazineacetic acid showed an interesting antiinflammatory activity coupled with low toxicity.
Acetates↗
Synthesis and antimicrobial study of novel heterocyclic compounds from hydroxybenzophenones.
The triazolothiadiazine analogues 6a-e were obtained via a multistep synthesis sequences beginning with the hydroxybenzophenones 1a-e. Hydroxybenzophenones on reaction with ethyl chloroacetate affords ethyl (2-aroylaryloxy)acetates 2a-e which on treatment with hydrazine hydrate yields 2-(2-aroylaryloxy)acetohydrazides 3a-e. Intramolecular cyclization of 3a-e with carbon disulfide affords 5-(2-aroylaryloxy)methyl-1,3,4-oxadiazole-2-(3H)thiones 4a-e, which on treatment with hydrazine hydrate yields 4-amino-5-(2-aroyl aryloxy)methyl-1,2,4-triazole-3-(2H)thiones 5a-e. Condensation of 5a-e with alpha-halocarbonyl compound results in 3-(2-aroylaryloxy)methyl-6-phenyl-1,2,4-triazolo[3,4-b][1,3,4] thiadiazine 6a-e analogues. The compounds 4a-e, 5a-e and 6a-e were tested against variety of fungal and bacterial strains in comparison to fluconazole and chloramphenicol, respectively.
Anti-Infective Agents↗
Stereochemistry of new nitrogen containing heterocyclic compounds.; X. Supramolecular structures and stereochemical versatility of polymeric complexes.
New polymeric complexes of Cu(II), Co(II), Ni(II) and UO2(II) with 5-(2(1)-carboxyphenylazo)-8-hydroxyquinoline (LH2) have been prepared and characterized on the basis of analytical, magnetic, 1H NMR, EPR and electronic spectral studies. Tentative structures for the polymeric complexes are proposed. The important infrared (IR) bands and the main 1H NMR signals are assigned and discussed relative to the molecular structure. EPR spectrum of copper(II) complex has been studied with a view to assigning their stereochemistries. Various EPR parameters have been calculated. Each metal has six-coordinates in an octahedral environment. The ligand acts as a dibasic (bis-bidentate chelating agent coordinating through CN, N=N, COOH and OH groups by replacement of a proton from the two latter groups. Considerable interest has also been focused on the synthesis of the azo compounds and its polymeric metal complex due to its wide potential applications. The thermal decomposition behavior of the complexes is also discussed.
Electron Spin Resonance Spectroscopy↗
Antifeedant activity of some new heterocyclic compounds against the larvae of Spodoptera litura F.
The antifeedant activity of diisoflavones a synthetic products is reported for the first time against S. litura. The antifeedant activity was tested employing the non-choice test method against the 4th instar pre-starved larvae.
Animals↗
[Coreximine and related compounds. 3. The formation of coreximine isomers under Eschweiler-Clarke's conditions (studies on the syntheses of heterocyclic compounds. CLXIV.)].
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Alkaloids↗
[Indene and related compounds. V. Ring expansion of 2-nitro-1-indanone oxime with polyphosphoric acid. (Studies on the syntheses of heterocyclic compounds. 173.)].
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Chemical Phenomena↗
Bis-basic derivatives of planar heterocyclic compounds.
Four compounds derived from the furocoumarin, benzodipyrone and benzodifuran nucleus respectively, have been synthesized. They have molecular structures analogous to that of tilorone, namely an aromatic tricyclic moiety and two basic chains linked to the nucleus through ester or amido groups. Like tilorone, the new compounds efficiently from complexes with DNA, consisting in an intercalation of the planar aromatic moiety between two base pairs and an electrostatic interaction of the positively charged nitrogen atoms of the side chains with the phosphate groups of the macromolecule. When tested for their capacity to stimulate interferon production in mice, the compounds showed different activities; in particular the diethylamino ethyl ester of bis-benzodifuranic acid (III) proved to be twice as active as tilorone, assayed in the same experimental conditions for comparison purposes.
Animals↗
[Theophylline and theobromine derivatives of nitrogen heterocyclic compounds].
7-Theophylline derivatives with 4,6-dihydroxy-5-pyrimidinyl-, 3-oxopiperazinylmethyl- and 4-methyl-3,5-dioxopiperazinylmethyl substituents are described: they can be viewed as structural analogues of a nucleic base pair in the Hoogsteen arrangement; theobromine could be converted into the 1-(3,5-dioxo-4-pyrazolidinyl) derivative, similarly analogous to a base pair in the Watson-Crick arrangement.
Heterocyclic Compounds↗
Some fused heterocyclic compounds as eukaryotic topoisomerase II inhibitors.
Our previously synthesized 37 compounds, which are 2,5,6-substituted benzoxazole, benzimidazole, benzothiazole, and oxazolo(4,5-b)pyridine derivatives, were tested for their eukaryotic DNA topoisomerase II inhibitory activity in cell free system and 28 were found to inhibit the topoisomerase II at an initial concentration of 100 microg/ml. After further testing at a lower range of concentrations, 12 derivatives, which were considered as positive topoisomerase inhibitors, exhibited IC50 values between 11.4 and 46.8 microM. Etoposide was used as the standard reference drug to compare the inhibitor activity. Among these compounds, 2-phenoxymethylbenzothiazole (3f), 6-nitro-2-(2-methoxyphenyl)benzoxazole (1a), 5-methylcarboxylate-2-phenylthiomethylbenzimidazole (3c), and 6-methyl-2-(2-nitrophenyl)benzoxazole (1c) were found to be more active than the reference drug etoposide. Present results point out that, besides the very well-known bi- and ter-benzimidazoles, compounds with single bicycle fused ring systems in their structure such as benzimidazole, benzoxazole, benzothiazole, and/or oxazolopyridine derivatives also exhibit significant topoisomerase II inhibitory activity.
Animals↗
Synthesis and antihepatotoxic activity of some heterocyclic compounds containing the 1,4-dioxane ring system.
Silymarin isolated from Silybum marianum is a mixture of three isomers, silybin (1), silydianin (2) and silychristin (3). Silybin is the most active antihepatotoxic agent, and contains a 1,4-dioxane ring in addition to a flavonoid moiety. Based on the skeleton of silybin, we prepared some flavones and coumarins containing the 1,4-dioxane ring system and evaluated them for antihepatotoxic activity against carbon tetrachloride induced hepatotoxicity in albino rats. The degree of protection was determined by measuring biochemical parameters such as serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvate transaminase (SGPT), alkaline phosphatase (ALKP), total protein (TP) and total albumin (TA). The compounds namely 3',4'(1",4"-dioxino) flavone (4f), and 3',4'(2-hydroxy methyl, 1",4"-dioxino) flavone (4g) were found to exhibit a significant activity comparable to standard drug silymarin (silybon-70). Other compounds also exhibited good activity. The structure activity relationship (SAR) was also studied, and where the flavonoid analogues containing a hydroxy methyl group at position-2" in the dioxane ring exhibited superior antihepatotoxic activity in comparison to coumarin derivatives.
Animals↗
[Research on heterocyclic compounds. VIII. Heteroarylcarboxamides and-acetamides with antipyretic activity].
A series of imidazo[1,2-a]pyridine-, imidazo[2,1-b]thiazole- and imidazo[2,1-b]benzothiazole-carboxamides and -acetamides were synthesized and their antiinflammatory, analgesic, antipyretic and ulcerogenic activities were evaluated.
Acetamides↗