• Archives of Pharmacal Research
• /
• 제17권5호
• /
• pp.298-303
• /
• 1994

4-Arylazo-1H-pyrazol-3, 5-idimines 1a-c reacted with bromomalononitrile (2) to yield the corresponding imidazo[1, 2-b]pyrazoles 3a-c. The latter reacted with some active methylene compounds and with .alpha.-cinnamonitriles to afford the corresponding pyrazoloimidazopyridines 6, 8, 9 and 15, respectively. Compounds 3 reacted with each of formic acid, formamide, trichlo-roacetonitrile and with guanidine to yield the corresponding pyrazoloimidazopyrimidines 16-19 respectively.

• Bulletin of the Korean Chemical Society
• /
• 제31권11호
• /
• pp.3304-3308
• /
• 2010

Condensation of 4-amino-5-mercapto-3-($\alpha$-naphthyl)-s-triazole (1) with cyanogen bromide gives 6-amino-3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazole (2) which on condensation with chloranil yields 3,9-di-($\alpha$-naphthyl)-6,14-dioxo-bis-(s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]cyclohexane]-5a,6a-diene) (3). 3-($\alpha$-naphthyl)-s-triazolo[3,4-b]-1,3,4-thiadiazolo[3,2-b]imidazo[4,5-b]quinoxaline (4) is obtained by a similar condensation of (2) with 2,3-dichloroquinoxaline. The reaction of (2) with $\alpha$-haloketones followed by bromination affords 7-aryl-3-($\alpha$-naphthyl)-imidazo[2,1-b]-1,3,4-thiadiazolo[2,3-c]-s-triazoles (5) and their 6-bromo analogues 6 respectively. The structures of all newly synthesized compounds were established on the basis of elemental analyses, IR, $^1H$-NMR. The antibacterial and antifungal activities of all newly synthesized compounds have also been evaluated.

• Natural Product Sciences
• /
• 제25권3호
• /
• pp.268-274
• /
• 2019

Morus alba L., known as white mulberry, is a medicinal plant belongs to family Moraceae. It has long been used commonly in Ayurvedic for the treatment of lung-heat, cough, asthma, hematemesis, dropsy and hypertension. In the present study, seven prenylated flavonoids, along with four benzofuran compounds were isolated by means of repeated column chromatography. The structures of the known compounds were identified as kuwanon G (1), kuwanon E (2), kuwanon T (3), morusin (4), sanggenon A (5), sanggenon M (6), sanggenol A (7), moracin R (8), mulberofuran G (9), mulberofuran A (10) and mulberofuran B (11), by comparing their spectroscopic data with those reported in the literature. For these isolates, containing trace compounds, the inhibitory activity against IL-6 production in $TNF-{\alpha}$ stimulated MG-63 cells was examined. All isolated compounds (1 - 11) showed excellent inhibitory activity against IL-6 production in $TNF-{\alpha}$ stimulated MG-63 cells. Especially this study is first time to report that sanggenon A (5), sanggenon M (6), sanggenol A (7), mulberofuran G (9), mulberofuran A (10) and mulberofuran B (11) showed the inhibitory activity of IL-6 production. Our study suggested the possibility of anti-inflammatory regulation by compounds (1 - 11) isolated from M. alba.

• Journal of Magnetics
• /
• 제1권2호
• /
• pp.64-68
• /
• 1996

Compared with the conventional magnetostriction in Ni alloys which are in the order of several tens ppm (Parts Per Million =10-6), RFe$_2$(R = rare earth element) Laves Phase intermetallic compounds show large saturation magnetostriction in the range of a few thousands ppm. However, the large external magnetic field necessary to obtain saturatio magnetostriction has due to large magnetocrystalline anisotropy energy restrained the applicationof magnetostriction materials in RFe$_2$intermetallic compounds. As a result of its solution, the largest published value of effective giant magnetostriction in a low external magnetic field (less than a few hundred Oe) is reported in this paper by means of amorphisation of RFe$_2$intermetallic compounds with the addition of boron, as a half metal. For the amorphous (SmFe$_2$)0.97 B0.03 alloys, the effective magnetostriction of -545 and -610 $\times$ 10-6 is obtained at 400 and 1,000 Ie, respectively. Moreover, the effective magnetostriction of 590 and 630$\times$10-6 in the amorphous (TbFe$_2$)0.98 B0.02 alloys is also found at 400 and 1,000 Oe, respectively. This result will provide a clue to understanding the effect of half metal on anomalous increase of the effective giant magnetostriction and attract the great attention for magnetostriction applications.

• Journal of Pharmaceutical Investigation
• /
• 제17권2호
• /
• pp.61-65
• /
• 1987

4-Pivaloyloxy, 4-benzenesulfonyloxy and 4-p-toluenesulfonyloxy compounds of piroxicam (2a, 2b and 2c) and isoxicam(4a, 4b and 4c) were synthesized in fairly good yield. Antiinflammatory and ulcerogenic effects of the 6 compounds were determined. Antiinflammatory effect of 2a was comparable to that of piroxicam and ulcerogenic effect of 2a was less than that of piroxicam.

• 약학회지
• /
• 제7권2_3호
• /
• pp.58-66
• /
• 1963

Alkyl-phenylthionocarbamates already have been investigated as anthelmintics. Especially ethyl-phenylthionocarbamate is noted for its anthelmintic action. Author studied methods for synthesizing Alkyl-phenylthionocarbamates, Alkyl-p-phenetyl thionocarbamates, Alkyl-cyclohexylthionocarbamates, 5 kinds for each. For alkyl radical $-CH_{3}$, $-C_{2}H_{5}$, -n-propyl, -isobuthyl, -n-buthyl, being chosen. Compounds VIII, X, XIII, XIV, and XV are new compounds. At the sametime author prepared 4 kinds of Arylthionocarbamates, among which XVII, and XIX being new compounds. (Table I) The anthelmintic action of these thionocarbamates has been examined through kymographic records indicating the action of neuromuscular preparation of Eisenia foetida Savigny in the various concentration fo above compounds: -Trendelenburg method. Santonine as the criterion of the estimation. (Table. II) 1. Compounds I-X could be prepared by method A or method B. method A in sealed tube brought on better yield and purity. 2. Compounds XI-XV couldn't be prepared by method A but by method B. 3. Arylthionocarbamates XVI, XVII, XVIII, and XIX couldn't be prepared by method A or method B but by method C. 4. Analyzed N. contained in all compounds. Analyzed C.H. and N. contained in unknown compounds, VIII, X, XIII, XIV, XV, XVII, and XIX. 5. Examination of anthelmintic action has been done under the advice of Prof. J.S.Oh medical college, Seoul Nat. University. 6. Compounds VI-X showed little action. 7. Compounds XVI-XIX showed almost no action. 8. Compounds XI-XV showed stronger action than compounds I-V, which was reported already as a usable anthelmintics. 9. Compounds XI, XII, XIII and XIV showed strongest actions, stronger than santonine as recorded on kymographion of the Trendelenburg method. Provided that, the toxity of these compounds found mild enough for human system, these compounds will serve as anthelmintics of greater powers than compounds I-V. 10. In Alkylthionocarbamates, R'NH-radical more influence on the anthelmintic action than ester radical(-OR).

• Bulletin of the Korean Chemical Society
• /
• 제31권10호
• /
• pp.2854-2860
• /
• 2010

Synthesis of a new series of pyrimidinyl-imidazo[2,1-b]thiazole derivatives is described. Their antiproliferative activity against A375 human melanoma cell line was tested and the effect of substituents on the pyrimidinyl ring side chain was investigated. The biological results indicated that most of the newly synthesized compounds showed moderate activity against A375, compared with Sorafenib. Among all of these derivatives, the cyclic sulfamide derivatives IIIa, IIIb, and IIIe showed the most potent antiproliferative activity against A375 human melanoma cell line. The IC50 values of compounds IIIa,b were in nanomolar scale. In addition, compound IIIe ($IC_{50}=1.9\;{\mu}M$) also demonstrated more potent antiproliferative activity compared with Sorafenib ($IC_{50}=5.6\;{\mu}M$).

• Bulletin of the Korean Chemical Society
• /
• 제21권6호
• /
• pp.613-617
• /
• 2000

p-(2-Vinyloxyethoxy)benzylidenemalononitrile (4a), methyl p-(2-vinyloxyethoxy)benzylidenecyanoacetate (4b), 3,5-dimethoxy-4-(2'-vinyloxyethoxy)benzylidenemalononitrile (5a), methyl 3,5-dimethoxy-4-(2'-vinyloxy-ethoxy) benzylidenecyanoacetate (5 b), o-(2 -vinyloxyethoxy)benzylidenemalononitrile (6a), methyl o-(2-viny-Ioxyethoxy) benzylidenecyanoacetate (6b), 1,3-di-(2',2'-dicyanovinyl)-5-methyl-2-(2'-vinyloxyetioxy)benzene (7a), l,3-di-(2'-carbomethoxy-2'-cyanovinyl)-5-methyl-2-(2'-vinyloxyethoxy)benzene (7b), 2,3,4-tri-(2'-viny-Ioxyethoxy) benzylidenemalononitrile (8a), methyl 2,3,4-tri-(2'-vinyloxyethoxy)benzylidenecyanoacetate (8b), 2,4,6-tri-(2'-vinyloxyethoxy)benzylidenemalononitrile (9a), and methyl 2,4,6-tri-(2'-vinyloxyethoxy)benzyl-idenecyanoacetate(9b) were prepared by the condensation of the corresponding benzaldehyde 1-3 with malononitrile or methyl cyanoacetate, respectively. Vinyl ether monomers 4, 6, and 8 polymerized readily with radical initiators to yield crosslinked polymers 10, 12, and 14. However, compounds 5, 7, and 9 were inert to radical initiators due to the steric hindrance. The resulting polymers 10, 12, and 14 were not soluble in common solvents showing a thermal stability up to $300^{\circ}C$.

• Bulletin of the Korean Chemical Society
• /
• 제31권8호
• /
• pp.2341-2344
• /
• 2010

A convenient synthesis of substituted [1,2,4]-triazolo [1',2':1,2]pyrimido[6,5-b]-quinoline 4(a-i) from substituted 2-chloroquinoline-3-carbaldehyde 1(a-i) and 4H-1,2,4-triazol-3-amine 2 by using $SiO_2/K_2CO_3$ under microwave irradiation. This method affords the [1,2,4]-Triazolo [1',2':1,2]pyrimido[6,5-b]-quinoline 4(a-i) under the influence of microwave irradiation in solvent-free conditions within short span (12 - 20 min), & gaves excellent yields (89 - 95%). All the synthesized compounds were further screened for their antibacterial activities. Some of our compounds showed excellent antibacterial activities against control drugs.

• Archives of Pharmacal Research
• /
• 제29권12호
• /
• pp.1119-1124
• /
• 2006

The methanol extract from the aerial parts of Dictamnus albus was active in inhibiting monoamine oxidase (MAO) from the mouse brain. Activity-guided fractionation led to the isolation of four known coumarins, 7-(6'R-hydroxy-3', 7'-dimethyl-2'E, 7'-octadienyloxy) coumarin (1), auraptene (2), umbelliferone (3), and xanthotoxin (4), as active compounds along with an inactive alkaloid, skimmianine (5). Compounds 1 and 2 inhibited MAO activity in a concentration-dependent manner with $IC_{50}$ values of 0.7 and $1.7\;{\mu}M$, respectively. Compounds 1 and 2 showed a slight and potently selective inhibitory effect against MAO-B ($IC_{50}\;0.5\;and\;0.6\;{\mu}M,\;respectively$) compared to MAO-A ($IC_{50}\;1.3\;and\;34.6\;{\mu}M,\;respectively$). According to kinetic analyses derived by Lineweaver-Burk reciprocal plots, compounds 1 and 2 exhibited a competitive inhibition to MAO-B.