• Title/Summary/Keyword: alkyl compounds

Search Result 246, Processing Time 0.024 seconds

Preparation of Alkyl and Aryl-thionocarbamate and their Anthelmintic action (Alkyl 급 Aryl thionocarbamate 류의 합성과 그 구충작용에 관한 연구)

  • 국채호
    • YAKHAK HOEJI
    • /
    • v.7 no.2_3
    • /
    • 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).

  • PDF

Synthesis and Antimicrobial Activity of Some New 1-Alkyl-2-alkylthio-1,2,4-triazolobenzimidazole Derivatives

  • Mohamed, Bahaa Gamal;Hussein, Mostafa Ahmed;Abdel-Alim, Abdel-Alim Mohamed;Hashem, Mohammed
    • Archives of Pharmacal Research
    • /
    • v.29 no.1
    • /
    • pp.26-33
    • /
    • 2006
  • Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.

Electrochemical Properties of Langmuir-Blodgett(LB) Film of Alkyl Bromides (브롬화 알킬화합물 LB막의 전기화학적 특성)

  • Park, Keun-Ho;Son, Tae-Chul;Min, Chang-Hun
    • Journal of the Korean Applied Science and Technology
    • /
    • v.26 no.4
    • /
    • pp.451-456
    • /
    • 2009
  • We carried out this experiment to observe an electrochemical properties for LB films of alkyl compounds by the cyclic voltammetry. Alkyl bromides was deposited by using the Langmuir- Blodgett method on the ITO glass. We measured to an electrochemical measurement by using cyclic voltammetry with a three-electrode system(an Ag/AgCl reference electrode, a platinum wire counter electrode and LB film-coated ITO working electrode) in 0.5, 1.0, 1.5 and 2.0 N $NaClO_4$ solution. A measuring range was reduced from initial potential to -1350 mV, continuously oxidized to 1650 mV. The scan rate were 100 mV/s. As a result, an electrochemical properties of the LB films of alkyl bromides appeared irreversible process caused by only the oxidation current from the cyclic voltammogram. The diffusivity(D) effect of LB films decreased with increasing of alkyl compounds amount.

The structure and synthesis of intercalation compounds between layered basic copper acetate and alkyl sulfonates (알킬술폰이 삽입된 층상구조의 염기성 초산구리의 합성과 구조)

  • 조영식;허영덕
    • Journal of the Korean Crystal Growth and Crystal Technology
    • /
    • v.8 no.3
    • /
    • pp.431-434
    • /
    • 1998
  • Layered basic copper acetate, $Cu(OH)(CH_3COO){cdot}H_2O$ was synthesized. Intercalation compounds of alkyl sulfonates into layered basic copper acetate have been synthesized via anionic exchange. From the X-ray diffraction data and the alkyl sulfonate size, the orientation of the intercalated alkyl sulfonate into layered basic copper acetate was determined.

  • PDF

Potential Functional Role of Phenethylamine Derivatives in Inhibiting Dopamine Reuptake: Structure-Activity Relationship

  • Dooti Kundu;Anlin Zhu;Eunae Kim;Suresh Paudel;Choon-Gon Jang;Yong Sup Lee;Kyeong-Man Kim
    • Biomolecules & Therapeutics
    • /
    • v.31 no.1
    • /
    • pp.108-115
    • /
    • 2023
  • Numerous psychotropic and addictive substances possess structural features similar to those of β-phenethylamine (β-PEA). In this study, we selected 29 β-PEA derivatives and determined their structure-activity relationship (SAR) to their ability to inhibit dopamine (DA) reuptake; conducted docking simulation for two selected compounds; and identified their potential functionals. The compounds were subdivided into arylethylamines, 2-(alkyl amino)-1-arylalkan-1-one derivatives and alkyl 2-phenyl-2-(piperidin-2-yl)acetate derivatives. An aromatic group, alkyl group, and alkylamine derivative were attached to the arylethylamine and 2-(alkyl amino)-1-arylalkan-1-one derivatives. The inhibitory effect of the compounds on dopamine reuptake increased in the order of the compounds substituted with phenyl, thiophenyl, and substituted phenyl groups in the aromatic position; compounds with longer alkyl groups and smaller ring-sized compounds at the alkylamine position showed stronger inhibitory activities. Docking simulation conducted for two compounds, 9 and 28, showed that the (S)-form of compound 9 was more stable than the (R)-form, with a good fit into the binding site covered by helices 1, 3, and 6 of human dopamine transporter (hDAT). In contrast, the (R, S)-configuration of compound 28 was more stable than that of other isomers and was firmly placed in the binding pocket of DAT bound to DA. DA-induced endocytosis of dopamine D2 receptors was inhibited when they were co-expressed with DAT, which lowered extracellular DA levels, and uninhibited when they were pretreated with compound 9 or 28. In summary, this study revealed critical structural features responsible for the inhibition of DA reuptake and the functional role of DA reuptake inhibitors in regulating D2 receptor function.

Synthesis and Biological Evaluation of Novel 2-[Substituted acetly]-amino-5-alkyl]-amino-5-alkyl-1,3,4-thiadiazoles

  • Shakya, Ashok K.;Mishra, Pradeep;Patnaik, G.K.;Shukla, Rakesh;Srimal, R.C.
    • Archives of Pharmacal Research
    • /
    • v.21 no.6
    • /
    • pp.753-758
    • /
    • 1998
  • Sixteen novel 2-substituted acetyl amino-5-alkyl-1,3,4-thiadiazol were synthesized and screened for their pharmacological activities. A few of the compounds namely 11, 12 and 16 showed anti-inflammatory activities comparable to phenylbutazone. Compound 12 also showed significan non-specific spasmolytic activity. Diuretic activity of compound 15 at a dose level of 90mg/kg p.o. was two fold higher compared to 50mg/kg p.o. of furosemide. Comparable diuresis was aso produced by compounds 9, 10, and 16.

  • PDF

Comparative Molecular Similarity Indices Analysis (CoMSIA) on the Melanogenesis Inhibitory Activities of Alkyl-3,4-dihydroxy- benzoate and N-alkyl-3,4-dihydroxybenzamide Derivatives.

  • Kim, Sang-Jin;Sung, Nack-Do;Lee, Sang-Ho
    • Proceedings of the SCSK Conference
    • /
    • 2003.09a
    • /
    • pp.733-740
    • /
    • 2003
  • To find a new substance with superior melanogenesis inhibitory activity, the bioactivities of alkyl-3,4-dihydroxy-5-substituted benzoate (A) and N-alkyl-3,4-dihydroxy-5-substituted benzamide (B) derivatives as substrate of tyrosinase were measured in mouse melanoma cells. And the bioactivities analyzed using comparative molecular similarity indices analysis (CoMSIA). From the CoMSIA model, when cross-validation value (q$^2$) is 0.713 at four components, the pearson correlation coefficient ($r^2$) is 0.900. Unknown compounds were predicted, using QSAR analyzed results from the CoMSIA methods. Excellent agreement was obtained between the measured and the predicted bioactivities of unknown compounds. As the results of prediction from CoMSIA, we could conclude that the bioactivities were increased from pl$_{50}$=3.18-4.80 to above 5.17 by creation of 6-methylheptyl, n-pentylphenyl and 2-hydroxypentylphenyl group etc,.,.

  • PDF

Synthesis of Three Ring Type Compounds with Fluorine and NCS Groups as Candidates for VA mode Liquid Crystal Display

  • Heo, E.Y.;Kim, Y.B.;Kim, S.H.
    • 한국정보디스플레이학회:학술대회논문집
    • /
    • 2003.07a
    • /
    • pp.571-574
    • /
    • 2003
  • Three ring type liquid crystalline compounds having 4-alklycyclohexyl group, 1,2-difluorobenzene and phenylisothiocyanate moieties as main skeleton were designed to have negative dielectricity. However, the compounds with 2,3,2'-trifluoro-3'-isothiocyanated biphenylcyclohexane core did not exhibit the nematic liquid crystalline phase because of two conformers by interaction of isothiocyanate and adjacent fluorine atoms. Also, 4-alkyl-2,2',3'-trifluoro-3-isothiocyanated biphenylcyclohexane core was designed expecting to have uniform conformers of isothiocyanate group. In the course of developing polyimides for VA mode LCD, we synthesized alkyl-3,5-diaminobenzene efficiently with various length of alkyl chains from commercially available di-t-butyl malonate and 3,5-dinitrobenzoyl chloride as starting material.

  • PDF

The structure and synthesis of intercalation compound between a layered double hydroxide and an organic compound (유기화합물이 삽입된 층상이중수산화물의 합성과 구조)

  • 우은경;허영덕
    • Journal of the Korean Crystal Growth and Crystal Technology
    • /
    • v.8 no.1
    • /
    • pp.36-41
    • /
    • 1998
  • Intercalation compounds of alkyl sulfonates into layered double hydroxides (LDH) have been directly synthesized. From the X-ray diffraction data and the alkyl sulfonates size, the orientation of the intercalated alkyl sulfonate into the layered double hydroxide was determined. The intercalated alkyl sulfonate is arranged with molecular chain perpendicular to the hydroxide layer with an antiparallel pattern.

  • PDF

The Synthesis of Sodium Bis(alkyl decaoxyethylene) Sulfonated Succinates (Sodium Bis(alkyl decaoxyethylene) Sulfonated Succinate류의 합성)

  • Lee, Hak-Bong;Jeong, No-Hee;Nam, Ki-Dae
    • Journal of the Korean Applied Science and Technology
    • /
    • v.11 no.1
    • /
    • pp.61-70
    • /
    • 1994
  • New anionic oligomeric surfactants, sodium bis(alkyl decaoxyethylene) sulfonated succinates, had been synthesized through the addition reaction of sodium hydrogen sulfite to bis(alkyl decaoxyethylene) maleates. Bis(alkyl decaoxyethylene) maleates were obtained by esterification with maleic anhydride and long chain alkyl decaoxyethylene ethers which were also obtained by addition ethylene oxide 10 mole to straight long chain alcohol with alkyl group having from 10 to 18 carbon atoms, their structure of the synthetic compounds have been characterized with IR. $^{1}H$ NMR and elemental analysis respectively.