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Bazı 5-Kloro-2-benzoksazolinon Tiyosemikarbazit, 1,3,4-Tiyadiazol ve 1,2,4-Triazol-5-tiyon Türevleri Üzerinde Çalışmalar
No full textIn this study, nineteen new compounds which have 1-[2-(5-chloro-2-benzoxazolinone-3-yl)acetyl]-4-substitutedthiosemicarbazide, 3-[(5-chloro-2-benzoxazolinone-3-yl)methyl]-4-substituted-1H-1,2,4-triazole-5(4H)-thione, 2-substitutedamino-5-[(5-chloro-2-benzoxazolinone-3-yl)methyl]-1,3,4-thiadiazole and 3-[(5-chloro-2-benzoxazolinone-3-yl)methyl]-4-substituted-5-methylthio-1H-1,2,4-triazole structures were synthesized and screened for their antimicrobial activities. Starting compound, 2-(5-chloro-2-benzoxazolinone-3-yl)acetylhydrazine was obtained by the reaction of 5-chloro-2-benzoxazolinone with ethyl bromoacetate followed by hydrazine hydrate. This compound was reacted with methyl, ethyl, allyl, cyclohexyl and phenyl isothiocyanates to obtained 1-[2-(5-chloro-2-benzoxazolinone-3-yl)acetyl]-4-substituted thiosemicarbazides (Compounds 1-5). Compounds 1-5 were cyclized into 3-[(5-chloro-2-benzoxazolinone-3-yl)methyl]-4-substituted-1H-1,2,4-triazole-5(4H)-thiones (Compounds 6-10) and 2-substitutedamino-5-[(5-chloro-2-benzoxazolinone-3-yl)methyl]-1,3,4-thiadiazole (Compounds 15-19) in alkaline and acidic medium respectively. 3-[(5-Chloro-2-benzoxazolinone-3-yl)methyl]-4-substituted-5-methylthio-1H-1,2,4-triazoles (Compounds 11-14) were prepared by reaction of compounds 6-10 with methyl iodide in alkali medium. The physical properties of the synthesized compounds were determined. Their structures have been elucidated by spectral methods (IR, 1H-NMR, 13C-NMR, ESI-MS) and elemental analyses. Their antimicrobial activities were investigated by microdilution method against some bacteria such as Enterococcus faecalis, Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa and some fungi such as Candida albicans, C. krusei and C. parapsilosis. The synthesized compounds do not show strong antimicrobial activity but it has been found that antifungal activities are higher than their antibacterial activities.İÇİNDEKİLER
ONAY SAYFASI iii
YAYIMLAMA VE FİKRİ MÜLKİYET HAKLARI BEYANI iv
ETİK BEYAN SAYFASI v
TEŞEKKÜR vi
ÖZET vii
ABSTRACT viii
İÇİNDEKİLER ix
SİMGELER VE KISALTMALAR xi
ŞEKİLLER xii
TABLOLAR xxiv
1. GİRİŞ 1
2. GENEL BİLGİLER 4
2.1. 2-Benzoksazolinonlar 4
2.1.1. Sentez Yöntemleri 4
2.1.2. Kimyasal Özellikleri 9
2.1.3. Spektral Özellikleri 14
2.1.4. Biyolojik Özellikleri 17
2.2. Tiyosemikarbazitler 22
2.2.1. Sentez Yöntemleri 23
2.2.2. Kimyasal Özellikleri 24
2.2.3. Spektral Özellikleri 29
2.2.4.Biyolojik Özellikleri 31
2.3. 1,2,4-Triazol-5-tiyon ve 5-Alkiltiyo-1,2,4-Triazoller 34
2.3.1. Sentez Yöntemleri 35
2.3.2. Kimyasal Özellikleri 46
2.3.3. Spektral Özellikleri 51
2.3.4. Biyolojik Özellikleri 55
2.4. 1,3,4-Tiyadiazoller 75
2.4.1. Sentez Yöntemleri 75
2.4.2. Kimyasal Özellikleri 80
2.4.3. Spektral Özellikleri 84
2.4.4. Biyolojik Özellikleri 85
2.5. Antibakteriyel-Antifungal Aktivite Tayin Yöntemleri 98
2.5.1. Dilüsyon Yöntemi 98
2.5.2. Difüzyon Yöntemi 100
3. GEREÇ VE YÖNTEM 101
3.1. Kimyasal Çalışmalar 101
3.1.1. Materyal 101
3.1.2. Genel Sentez Yöntemleri 101
3.1.3. Analitik Yöntemler 103
3.2. Biyolojik Aktivite Çalışmaları 104
3.2.1. Materyal 104
3.2.2. Yöntem 105
3.2.3. Sonuçların Değerlendirilmesi 106
4. BULGULAR 107
4.1. Kimyasal Çalışmalar 107
4.2. Biyolojik Aktivite Çalışmaları 128
5. TARTIŞMA 130
6. SONUÇ VE ÖNERİLER 152
7. KAYNAKLAR 154
8. EKLER
EK-1: Tez çalışması ile ilgili bildiriler
9. ÖZGEÇMİŞBu çalışmada, 1-[2-(5-kloro-2-benzoksazolinon-3-il)asetil]-4-sübstitüetiyosemikarbazit, 3-[(5-kloro-2-benzoksazolinon-3-il)metil]-4-sübstitüe-1H-1,2,4-triazol-5(4H)-tiyon, 3-[(5-kloro-2-benzoksazolinon-3-il)metil]-4-sübstitüe-5-metiltiyo-4H-1,2,4-triazol, 2-sübstitüeamino-5-[(5-kloro-2-benzoksazolinon-3-il) metil]-1,3,4-tiyadiazol yapısında literatürde kayıtlı olmayan on dokuz yeni bileşiğin sentezi yapılarak bu bileşiklerin antimikrobiyal aktiviteleri incelenmiştir. Bileşiklerin sentezinde, 5-kloro-2-benzoksazolinondan hareket edilmiş ve önce etil bromoasetat, takiben hidrazin hidrat ile reaksiyona sokularak 2-(5-kloro-2-benzoksazolinon-3-il)asetilhidrazin elde edilmiştir. Bu bileşiğin metil, etil, allil, sikloheksil ve fenil izotiyosiyanat ile reaksiyonu sonucu 1-[2-(5-kloro-2-benzoksazolinon-3-il)asetil]-4-sübstitüetiyosemikarbazit türevlerine (Bileşik 1-5) ulaşılmıştır. Bileşik 1-5’in alkali ortamda siklizasyonu sonucu 3-[(5-kloro-2-benzoksazolinon-3-il)metil]-4-sübstitüe-1H-1,2,4-triazol-5(4H)-tiyon (Bileşik 6-10), asidik ortamda siklizasyonu sonucu 2-sübstitüeamino-5-[(5-kloro-2-benzoksazolinon-3-il)metil]-1,3,4-tiyadiazol türevleri (Bileşik 15-19), Bileşik 6-10’un alkali ortamda metil iyodürle reaksiyonu sonucu ise 3-[(5-kloro-2-benzoksazolinon-3-il)metil]-4-sübstitüe-5-metiltiyo-4H-1,2,4-triazoller (Bileşik 11-14) kazanılmıştır. Sentezi yapılan bileşiklerin fiziksel özellikleri belirlenmiş, yapıları IR, 1H-NMR, 13C-NMR, ESI-MS spektral yöntemleri ve eleman analizleri ile aydınlatılmış, antimikrobiyal aktiviteleri Enterococcus faecalis, Staphylococcus aureus, Escherichia coli ve Pseudomonas aeruginosa gibi bakteri, Candida albicans, C. krusei ve C. parapsilosis gibi mantarlara karşı mikrodilüsyon yöntemi kullanılarak incelenmiştir. Sentezi yapılan bileşiklerde kuvvetli antimikrobiyal etki göstermemekle beraber, antifungal etkilerinin antibakteriyel etkilerine kıyasla daha yüksek olduğu tespit edilmiştir
Studıes on Some Aryloxymethyl Thıosemıcarbazıde, 1,3,4-Thıadıazole and 1,2,4-Trıazole-5-Thıone Derıvatıves
No full textIn this study, twelve 1-(7-methoxy-2-naphthyloxyacetyl)-4-subtituted-3-thiosemicarbazide, 5-(7-methoxy-2-naphthyloxymethyl)-2-substituted
amino-1,3,4-thiadiazole and 3-(7-methoxy-2-naphthyloxymethyl)-4-substituted-
1,2,4-triazole-5-thione derivatives have been synthesized and the compounds having
2-substitutedamino-1,3,4-thiadiazole and 4-substituted-1,2,4-triazole-5-thione
structure were evaluated for inhibitory effects on COX-1 and COX-2 enzymes. The
interaction between the Compound 2b and the COX-2 enzyme was interpreted by
using “Molecular Operating Environment” MOE program.
5-(7-Methoxy-2-naphthyloxymethyl)-2-substitutedamino-1,3,4-thiadiazole
(Compounds 2a-d) and 3-(7-methoxy-2-naphthyloxymethyl)-4-substituted-1,2,4-
triazole-5-thione derivatives (Compounds 3a-d) were synthesized by cyclization of
1-(7-methoxy-2-naphthyloxyacetyl)-4-subtituted-3-thiosemicarbazides (Compounds
1a-d). Chemical structures of the compounds were elucidated by IR, 1H-NMR, 13CNMR
and mass spectra and elemental analysis.
The synthesized compounds (Compounds 2a-d and 3a-d) showed lower
inhibitory activities on COX-2 enzyme then standard compounds NS-398 and
indomethacin. 2-(7-Methoxy-2-naphthyloxymethyl)-5-ethylamino-1,3,4-thiadiazole
(Compound 2b) is more selective against COX-2, 3-(7-methoxy-2-naphthyloxy
methyl)-4-ethyl-1,2,4-triazole-5-thione and 3-(7-methoxy-2-naphthyloxymethyl)-4-
allyl-1,2,4-triazole-5-thione (Compounds 3b and 3c) are more selective against
COX-1 than rest of the compounds. As a result of the docking studies on COX-2
enzyme, it was observed that the Compound 2b is fitted and interacted with the
hydrophobic parts in the active pocket of COX-2, Val349, Tyr355, Leu359 and
Leu531.Bu çalışmada, 1-(2-(7-metoksi-2-naftiloksi)asetil)-4-sübstitüe-3-tiyosemikarbazit, 5-((7-metoksi-2-naftiloksi)metil)-2-sübstitüeamino-1,3,4-tiyadiazol
ve 3-((7-metoksi-2-naftiloksi)metil)-4-sübstitüe-1,2,4-triazol-5-tiyon yapısında 12 yeni bileşiğin sentezi yapılarak, 2-sübstitüeamino-1,3,4-tiyadiazol ve 4-sübstitüe-
1,2,4-triazol-5-tiyon yapısındaki sekiz bileşiğin COX-1 and COX-2 enzimleri
üzerindeki inhibitör etkileri incelenmiştir. Bileşiklerin COX-2 enzimi ile
etkileşmeleri “Molecular Operating Environment” (MOE) programı kullanılarak
yorumlanmıştır.
5-((7-Metoksi-2-naftiloksi)metil)-2-sübstitüeamino-1,3,4-tiyadiazol (Bileşik 2a-d)
ve 3-((7-metoksi-2-naftiloksi)metil)-4-sübstitüe-1,2,4-triazol-5-tiyon türevleri
(Bileşik 3a-d) 1-(2-(7-metoksi-2-naftiloksi)asetil)-4-sübstitüe-3-tiyosemikarbazitlerin
siklizasyonu ile elde edilmişlerdir. Sentezi yapılan bileşiklerin yapıları IR, 1H-NMR,
13C-NMR, kütle spektrumları ve elemental analiz ile aydınlatılmıştır.
Aktivitesi incelenen bileşikler (Bileşik 2a-d ve 3a-d) COX-2 enzimi üzerinde
inhibitör etki göstermekle beraber, hiçbiri standart bileşikler NS-398 ve indometazin
kadar etkili değildir. Sentez edilen türevler arasında 5-((7-Metoksi-2-
naftiloksi)metil)-2-etilamino-1,3,4-tiyadiazolün (Bileşik 2b) COX-2 enzimine, 3-((7-
metoksi-2-naftiloksi)metil)-4-etil-1,2,4-triazol-5-tiyon ve 3-((metoksi-2-naftiloksi)
metil)-4-allil-1,2,4-triazol-5-tiyonun (Bileşik 3b ve 3c) COX-1 enzimine karşı seçici
olarak en aktif bileşikler olduğu gözlenmiştir. COX-2 enzimi üzerinde yapılan
docking çalışmaları sonucunda, Bileşik 2b’nin her iki enzimde ortak olan hidrofobik
kısımlara yerleşerek enzim ile etkileştiği ancak COX-2’ye özgü ve Val349, Tyr355,
Leu359 and Leu531 tarafından oluşturulan bölgeye yerleşemedikleri gözlenmiştir
Going Beyond Counting First Authors in Author Co-citation Analysis
Get PDFThe 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
Variations on the Author
Get PDF“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
Get PDFWe 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
Dispelling the Myths Behind First-author Citation Counts
Get PDFWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
koamabayili/VECTRON-author-checklist: VECTRON author checklist
No full textWe have done our best to complete the author checklist relating to the use of animals in the hut study. Note that the objective for the hut study was to evaluate the IRS treatment applications for residual efficacy against Anopheles mosquitoes, including the local An. coluzzii mosquito population. Cows were only used to attract mosquitoes into the huts and no tests were carried out directly on the cows. The author checklist is intended for use with studies where experiments are carried out on animals, which is why we have had such difficulty in completing this for the hut study, as many of the questions do not relate to how the cows were used
Author-wise bibliometric analysis based on entropy.
No full textAuthor-wise bibliometric analysis based on entropy.</p
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