• Natural Product Sciences
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• 제3권2호
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• pp.89-99
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• 1997

Aminolysis, hydrazinolysis and alkylation of 4-methoxy and 4,9-dimethoxy-6-cyano-7-thione-5-methyl-7H furo [3,2-g] [1] benzopyridine (1 a-b) yielded 7N-substituted furobenzopyridine derivatives (2 a-e or the possible isomers 3 a-e and 4 a-b), (5 a,b and 6 a,b) and the ester (8 a,b). Hydrolysis of (la) with acetic acid gave the corresponding pyridone derivatives (7). Furobenzopyridinyl-7-thioacetyl hydrazide (9 a,b) have been prepared via alkylation of furobenzopyridine thione (1 a-b) with ethyl chloroacetate followed by condensation with hydrazine hydrate. Schiff base (11) was prepared by reacting (9a) with p. N,N-dimethyl aminobenzaldehyde in boiling ethanol. Treatment of (8a) with anthranilic acid gave the corresponding 7-substituted-4H-3,1-benzoxazine-4-one (10). We found that compound (11) increased bleeding, coagulating time, the total count of white blood cells, blood glucose level (cause hyperglycemia), enzymes (GOT, GPT) activities, concentration of urea and creatinine. On the other hand it decreased red blood cells number, haemoglobin content and haematocrite value.

• 약학회지
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• 제16권4호
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• pp.176-179
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• 1972

The bile secretion was accelerated generally by the administration of all derivatives tested: chemodeoxycholate, deoxycholate, cholate, dehydrocholate, 7-ketochenodeoxycholate, and 3, 7-diketochenodeoxycholate in decreasing order. Bile acids content in bile from animals administered with cholate was increased, however, other derivatives did not alter the contents of bile acids and bilirubin. In view of pharmacological point, all derivatives have hydrocholeretic action, however, only cholate exhibits typical choleretic action.

• 약학회지
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• 제37권6호
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• pp.615-620
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• 1993

The cross-coupling reaction of organo tin reagents with a variety of organic halides, catalyzed by palladium, provides a novel method for generating a carbon-carbon bond. We used this method for the antibacterial agents, and synthesis of new quinolone derivatives which have carbon-carbon bond at C-7 position of general quinolone moieties. Aryl tin, quinolone moieties, and palladium catalyst were refluxed in DMF to afford new quinolone derivatives. This palladium catalyzed coupling reactions have capacity for further synthetic elaboration.

• Bulletin of the Korean Chemical Society
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• 제35권7호
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• pp.2038-2042
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• 2014

4-(tert-Octyl)phenol derivatives bearing the D-mannitol substructure (6a, 6b, 7) were prepared from $\small{D}$-mannitol and evaluated their anticancer activity against human lung (A549) and prostate (Lncap, Du145, PC3) cancer cell lines. Among derivatives tested, the bis(tert-octyl)phenoxy compound 7 exhibited strongest proliferation inhibitory activities against human cancer cell lines tested, especially high sensitivity to human Du145 prostate cancer cells ($IC_{50}=7.3{\mu}M$).

• 통합자연과학논문집
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• 제7권3호
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• pp.159-165
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• 2014

Pyrazole, hydroxyimino, aldehyde and isoxazole derivatives exhibit a broad spectrum of biological activities such as antimicrobial, anti-inflammatory and antitumor activities. With growing application on their synthesis and bioactivity, chemists and biologists in recent years have considerable attention on the research of these derivatives. In the view of potential importance of these derivatives, we have crystallized few of the derivatives and its report has been published. The present study focuses on docking studies of these derivatives against Phospholipases $A_2$ enzyme. This enzymes has implicated as potential targets for anti-inflammatory drug design. co-crystal structure (PDB ID: 1POE) of $PLA_2$ deposited in Protein Data Bank has been retrieved for docking analysis. Docking studies using Schrodinger's GLIDE reveals that these derivatives shows better binding energy and score in the defined active site. These results may provide a guiding role to design a lead molecule which may reduce inflamation.

• Archives of Pharmacal Research
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• 제13권3호
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• pp.274-277
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• 1990

It has been found that $\alpha, \beta$-unsaturated nitrile derivatives 1-3 reached with S- methylisothiourea to give the prpone derivatives 4-6 respectively. Cyclisation of 4-6 using ethanolic hydrochloric acid afforded the pyridine derivatives 7-9 in good yields. On the other hand, the reactions of hydrazine hydrate and of phenylhydrazine with each of 7-9 gave the corresponding pyrazolopyridine derivatives 10-15. The structures of the newly synthesised derivatives were assigned on the basis of elemental analyses, IR and $^1H$-NMR spectral data studies.

• 약학회지
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• 제41권2호
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• pp.181-186
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• 1997

A series of 7-deazahypoxanthine and 7-deazaadenine derivatives[6,7.8.9.10,13] as purine antagonists was prepared. The pyrrolidine-5-one derivatives[4,11] were treated vith $(C_2H_5)_3OBF_4$ to give 3- aryl-5-ethoxy-2H-3,4-dihydropyrrole[5,12], which were converted to 7-aryl-7,8-dihydro-7(9H)-deazahy-poxanthine[6,7,8,9,10] and 7-phenyl-2-methyl-7,8- dihydro-7(9H)-deazaadenine[13].

• 약학회지
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• 제41권1호
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• pp.7-13
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• 1997

A regiospecific total synthesis on the precursor(18b) of rhodomycinones is described. The anion of 3-carbomethoxy-1(3H)-isobenzofuranone(13) was respectively condensed wi th naphthalenone (12) and butenoate(8) derivatives which were, prepared by two different synthetic routes to afford 9-ethyl-6,7-dihydroxy 7,8,9,10-tetrahydronaphthacene-5,12 dione(18b) after oxidation and reduction.

• 약학회지
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• 제41권6호
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• pp.724-729
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• 1997

New 7-Halo-4-hydroxy-2-allyl-N-3-(4-methoxy-2-carboxylic acid pyrrolidinyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide derivatives were synthesized through the condensation of 7-halo-4-hydroxy-2-allyl-1,2-benzothiazine-3-carboxylic acid methyl ester 1,1-dioxide with 4-methoxy L-proline.

• 대한화학회지
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• 제56권4호
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• pp.459-463
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• 2012

8-Formyl-4-Methyl-7-Hydroxy Coumarin Derivatives were synthesized via Penchem condensation followed by Duffs reaction. Treatment of this with N,N-di substituted cyano acetamides in the presence of piperdine afforded New 8-Formyl-4-Methyl-7-Hydroxy Coumarin Derivatives (7a-o). Their structures were characterized by IR, $^1H$ and $^{13}C$ NMR and Mass spectral and elemental analysis data.