1,720,972 research outputs found
A QSAR Analysis of Flavone Derivatives of Antimalarial Compounds Based on PM3 Semi-Empirical Method
No full textSINTESIS SENY AWA (1)-N-(4-BENZILOKSI-3-METOKSIBENZIL)-1, 10- FENANTROLINIUM KLORIDA SEBAGAI ANTI MALARIA
No full textTelah dilakukan sintesis senyawa (1)-N-(4-benziloksi-3-metoksibenzil)-1,10- fenantrolinium klorida dari 1,1O-fenantrolin monohidrat dan 4-hidroksi- -metoksibenzaldehida (vanilin) sebagai bahan dasar. Pembuatan senyawa (1)-N-(4- benziloksi-3-metoksibenzil)-1,1O-fenantrolinium klorida melalui 4 tahap reaksi yaitu: (1) reaksi benzilasi terhadap senyawa 4-hidroksi-3-metoksibenzaldehida dilakukan menggunakan katalis sodium hidroksida yang ditambahkan secara perlahan-Iahan kemudian direfluks selama 2 jam. Hasil reaksi diperoleh senyawa 4-benziloksi-3- metoksibenzaldehida berupa padatan cok!at (t.I=61-62&de
Quantitative Structure-Activity Relationship Analysis of Antimalarial Compound of Mangostin Derivatives Using Regression Linear Approach
No full textSynthesis and Antiplasmodial Activity of 2-(4-Methoxyphenyl)-4-Phenyl-1,10-Phenanthroline Derivative Compounds
No full textA unique of synthetic methods was employed to prepare 2-(4-methoxyphenyl)-4-phenyl-1,10-phenanthroline (5) derivatives from 4-methoxy-benzaldehyde (1), acetophenone (2), and 8-aminoquinoline (4) with aldol condensation and cyclization reactions. The derivatives were tested through antiplasmodial test. The synthesis of derivatives compound 5 was conducted in three steps. The 3-(4-methoxyphenyl)-1-phenylpropenone 3 was synthesized through aldol condensation of 1 and 2 which has a yield of 96.42%. The compound 5 was synthesized through cyclization of compound 4 and 3 with 84.55% yield. The derivative of compound 5 was synthesized from compound 5 using DMS and DES reagents which refluxed for 21 and 22 h, to produce (1)-N-methyl-9-(4-methoxyphenyl)-7-phenyl-1,10-phenanthrolinium sulfate (6) and (1)-N-ethyl-9-(4-methoxyphenyl)-7-phenyl-1,10-phenanthrolinium sulfate (7) with 91.42 and 86.36% yields, respectively. Results of in vitro testing of antiplasmodial activity of compound 5 derivatives (i.e., compound 6 and 7) against chloroquine-resistant P. falciparum FCR3 strain showed that compound 7 had higher antimalarial activity than compounds 5 and 6. Whereas, results of in vitro testing against chloroquine-sensitive P. falciparum D10 strain showed that compound 6 has higher antimalarial activity than compounds 5 and 7
Going Beyond Counting First Authors in Author Co-citation Analysis
Full text linkThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Sistesis Senyawa Antimalaria 3-(2-Hidrosietil)-2-Metil-1,10-Fenantrolin-4-OL dari 8-Aminoquinolin = Synthesis of Antimalarial 3-(2-Hydroxyethyl)-2-methyl-1,10-phenanthroline-4-ol from 8-Aminoquinoline
No full textIt has been conducted the synthesis of 3-(2-hydroxyethyl)-2- methyl-1,10-phenanthroline-4-ol was carried out from 8-aminoquinoline which are expected to posses antimalarial activity. The experiment perfomed consisted of two steps i.e (1) reaction of 8-aminoquinoline with 2-acetyl-butyrolactone and (2) cyclization of the resulted 341-(quinolin-8-ylamino)- ethylidene]-4,5-dihydro-furan-2-one. Identification of the products were carried out by means of infra red (IR) spectroscopy, proton nuclear magnetic resonance (1H-NMR) spectroscopy, and mass spectroscopy (MS).
The reaction of 8-aminoquinoline with 2-acetyl-butyrolactone was performed in toluene at reflux for 6 hours in the presence of p-toluensulfonic acid as catalyst. This reaction gave 3- [1-(quinolin-8-ylamino)-etiliden]-4,5-dihidro-furan-2-on in 60.6% yield. The cyclization of 341-(quinoline-8-ylamino)-ethyliden]-4,5- dihydro-furan-2-one was conducted in cloroform at reflux for 4 hours in the preserice of H2SO4 as catalyst and also tween 80 as transfer phase catalyst to give 3-(2-hydroxy-ethyl)-2-methyl-1,10- phenanthroline-4-ol in 76.2% yield.
Key words : antimalarial, 8-aminoquinoline, cyclization, 1,10- phenantroline
QSAR Analysis of Benzothiazole Derivatives of Antimalarial Compounds Based On AM1 Semi-Empirical Method
Full text linkQuantitative Structure and Activity Relationship (QSAR) analysis of 13 benzothiazoles derivatives compound as antimalarial compounds have been performed using electronic descriptor of the atomic net charges (q), dipole moment (μ), ELUMO, EHOMO and polarizability (α). The electronic structures as descriptors were calculated through HyperChem for Windows 7.0 using AM1 semi-empirical method. The descriptors were obtained through molecules modeling to get the most stable structure after geometry optimization step. The antimalarial activity (IC50) were taken from literature. The best model of QSAR model was determined by multiple linear regression approach and giving equation of QSAR: Log IC50 = 23.527 + 4.024 (qC4) + 273.416 (qC5) + 141.663 (qC6) – 0.567 (ELUMO) – 3.878 (EHOMO)– 2.096 (α). The equation was significant on the 95% level with statistical parameters: n = 13, r = 0.994, r2 = 0.987, SE = 0.094, Fcalc/Ftable = 11.212, and gave the PRESS = 0.348. Its means that there were only a relatively few deviations between the experimental and theoretical data of antimalarial activity
Variations on the Author
Full text link“Variations on the Author” discusses two of Eduardo Coutinho’s recent films (Um Dia na Vida, from 2010, and Últimas Conversas, posthumously released in 2015) and their contribution to the general question of documentary authorship. The director’s filmography is characterized by a consistent yet self-effacing form of authorial self-inscription: Coutinho often features as an interviewer that rather than express opinions propels discourses; an interviewer that is good at listening. This mode of self-inscription characterizes him as an author who is not expressive but who is nonetheless markedly present on the screen. In Um Dia na Vida, however, Coutinho is completely absent form the image, while Últimas Conversas, on the contrary, includes a confessional prologue that moves the director from the margins to the center of his films. This article examines the ways in which these works stand out in the filmography of a director who offers new insights into the notion of cinematic authorship
Appropriate Similarity Measures for Author Cocitation Analysis
Full text linkWe provide a number of new insights into the methodological discussion about author cocitation analysis. We first argue that the use of the Pearson correlation for measuring the similarity between authors’ cocitation profiles is not very satisfactory. We then discuss what kind of similarity measures may be used as an alternative to the Pearson correlation. We consider three similarity measures in particular. One is the well-known cosine. The other two similarity measures have not been used before in the bibliometric literature. Finally, we show by means of an example that our findings have a high practical relevance.information science;Pearson correlation;cosine;similarity measure;author cocitation analysis
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