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Research Laboratories Information System
Research Laboratories Information System
Farmasötik Kimya Araştırma Laboratuvarı
Farmasötik Kimya Araştırma Laboratuvarı
Anabilim Dalımız Araştırma Laboratuvarında organik maddelerin sentez, saflaştırma, yapı tayini ve kalitatif- kantitatif analizleri yapılmaktadır.
İstanbul Üniversitesi, Eczacılık Fakültesi, A-Blok, 34116 Beyazıt, İstanbul
Toplam kullanılan BAP Kaynağı: 395.000,00 TL
Anabilim Dalımız Araştırma Laboratuvarında organik maddelerin sentez, saflaştırma, yapı tayini ve kalitatif- kantitatif analizleri yapılmaktadır.
Anabilim
Dalı?mızda ntimikobakteriyel, antiviral, antikanser, antifungal, karbonik
anhidraz inhibitörü, antiimflamatuar bileşiklerin tasarımı, sentezi, saflaştırılması
ve yapı tayinleri ile, kalitatif-
kantitatif analizleri yapılmaktadır.
İstanbul Üniversitesi, Eczacılık Fakültesi, A-Blok, 34116 Beyazıt, İstanbul
Toplam kullanılan BAP Kaynağı: 395.000,00 TL
Pharmaceutical Chemistry Research Laboratory
The research laboratories in our department engage in the synthesis, purification, structural identification, and quantitative/qualitative analyses of organic compounds.
Istanbul University, Faculty of Pharmacy, Block B, 34116-Beyazit, Istanbul
Total resource (BAP): 395.000,00 TL
The research laboratories in our department engage in the synthesis, purification, structural identification, and quantitative/qualitative analyses of organic compounds.
Our department engages in the design, synthesis,
purification, characterization, and qualitative/quantitative analyses of
compounds that exhibit antibacterial, antiviral, anticancer, antifungal,
carbonic anhydrase inhibitory and anti-inflammatory properties.
Istanbul University, Faculty of Pharmacy, Block B, 34116-Beyazit, Istanbul
Total resource (BAP): 395.000,00 TL
| Görev | Ünvan | Ad | Soyad | Dahili Telefon | AVES Link | |
|---|---|---|---|---|---|---|
| Müdür | YARDIMCI DOÇENT | SERHAN | TÜRKYILMAZ | 13458 | CV |
Cihaz Adı : UV Kabin
Marka : CAMAG
Model : UV CABINET 4
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : BAP
Alım Tarihi : 31/12/2019Cihaz Adı : Distile su ve Ultra saf su Cihazı
Marka : Elga
Model : Chorus II
Teknik Özellik : 253.3.6/20/14248 (SAF SU) 253.3.6/20/14250 (TANK)
Miktar : 1
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2019Cihaz Adı : Flash Kromatografi Cihazı
Marka : Teledyne
Model : Combiflash E/Z Prep
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2015Cihaz Adı : Flash Kromatografi Cihazı
Marka : BUCHI
Model : Pure C-810 Flash
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : BAP
Alım Tarihi : 31/12/2017Cihaz Adı : NMR Cihazı
Marka : Oxford
Model : Pulsar
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2016Cihaz Adı : LC-MS
Marka : Agilent
Model : Infinity II
Teknik Özellik : 253.3.6/20/35492 (MS) 253.3.6/20/40610 (HPLC-DAD)
Miktar : 1
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2019Cihaz Adı : Rotavapor
Marka : Heidolph
Model : Heidolph
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2019Cihaz Adı : Rotavapor
Marka : BUCHI
Model : R300
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : BAP
Alım Tarihi : 31/12/2017Cihaz Adı : Etüv
Marka : MEMMERT
Model : MEMMERT
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2019Cihaz Adı : Su Banyoları
Marka : GFL
Model : GFL
Teknik Özellik : -
Miktar : 2
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2017Cihaz Adı : Ultrasonik Banyo
Marka : Bandelin
Model : Sonorex
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : BAP
Alım Tarihi : 31/12/2017Cihaz Adı : Isıtcılı Manyetik Karıştırıcı
Marka : HEIDOLPH
Model : HEIDOLPH
Teknik Özellik : -
Miktar : 4
Cihaz Kaynağı : TÜBİTAK
Alım Tarihi : 31/12/2017Cihaz Adı : Daldırmalı Soğutucu
Marka : JULOBO
Model : FT902
Teknik Özellik : Reaksiyon ortamını -70oC ye kadar soğutabilir
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : UV-VIS Spektrofotometre
Marka : SHIMADZU
Model : UV-mini 1240
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : UV-VIS Spektrofotometre
Marka : SHIMADZU
Model : LC-10ADvp
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : Vakum Etüvü
Marka : MEMMERT
Model : UM 500
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : UV-VIS Spektrofotometre
Marka : SHIMADZU
Model : UV-1601
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : Erime Derecesi Tayin Cihazı
Marka : BUCHI
Model : Melting Point B-540
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : Rotary Evaporatör
Marka : IKA-WERKE
Model : HB4 Basic
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : Kromatotron Cihazı
Marka : Chromatotron
Model : -
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : Rotary Evaporatör
Marka : BUCHI
Model : -
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : Mikrodalga Sentez Sistemi
Marka : Milestone Start S
Model : Microwave Labstation for Synthesis
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : DiğerCihaz Adı : Infrared Spektrofotometre
Marka : SHIMADZU
Model : IR Affınıty-1 Model Fourier Transform
Teknik Özellik : -
Miktar : 1
Cihaz Kaynağı : Diğer
- Makale & Yayın (10)
- Sanayi İşbirliği (0)
- Patent (0)
- Dış Kaynaklı Çalışma (0)
- Faydalı Model (0)
- Ticarileşme (0)
- Proje (8)
- Adı : A Class of Sulfonamides with Strong Inhibitory Action Against The Carbonic Anhydrase From Trypanosoma Cruzi
Açıklama : Trypanosoma cruzi, the causative agent of Chagas disease, encodes for an ?-carbonic anhydrase (CA, EC 4.2.1.1) possessing high catalytic activity (TcCA) which was recently characterized (Pan et al. J. Med. Chem. 2013, 56, 1761-1771). A new class of sulfonamides possessing low nanomolar/subnanomolar TcCA inhibitory activity is described here. Aromatic/heterocyclic sulfonamides incorporating halogeno/methoxyphenacetamido tails inhibited TcCA with KIs in the range of 0.5-12.5 nM, being less effective against the human off-target isoforms hCA I and II. A homology model of TcCA helped us to rationalize the excellent inhibition profile of these compounds against the protozoan enzyme, a putative new antitrypanosoma drug target. These compounds were ineffective antitrypanosomal agents in vivo due to penetrability problems of these highly polar molecules that possess sulfonamide moieties.
Ekip : Güzel Ö., Akdemir A. , Pan P. , Vermelho A.B. , Parkkila S., Scozzafava A. , Capasso C., Supuran C.T. - Adı : Synthesis and Evaluation of Functionalized Indoles as Antimycobacterial and Anticancer Agents
Açıklama : A new series of 5-fluoro-N(2)-(cyclohexylidene)-3-phenyl-1H-indole-2-carbohydrazides (6a-6e) and their cyclization products 5-fluoro-N-(3-oxo-1-thia-4-azaspiro [4.5]dec-4-yl)-3-phenyl-1H-indole-2-carboxamides (7a-7e, 8a-8e) have been synthesized and evaluated for in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using the Microplate Alamar Blue Assay (MABA). Compounds showed moderate to good inhibitory activity at 6.25 ?g/mL. Among them, 7b, 7d, 8b, and 8d were the most potent analogs with an inhibition range of 91-95 %. Additionally, compounds 6a, 7a, 7e, 8a, and 8e were subjected to the National Cancer Institute's (NCI) in vitro disease-oriented antitumor screening to be evaluated for antitumor activity. 8e, the most potent compound examined, displayed broad spectrum antiproliferative activity with particular selectivity against four leukemia cell lines (CCRF-CEM, HL-60 (TB), K-562, and RPMI-8226) with log (10) GI (50) values between -5.68 and -6.09.
Ekip : Cihan Üstündağ G., Çapan G - Adı : Microwave Assisted Synthesis and Anti-Influenza Virus Activity of 1-Adamantyl Substituted N-(1-Thia-4-Azaspiro[4.5] Decan-4-Yl)Carboxamide Derivatives
Açıklama : A microwave-assisted three-component one-pot cyclocondensation method was applied for the synthesis of novel N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide compounds carrying an adamantyl moiety. The structures of the compounds were confirmed by spectral and elemental analysis. All compounds were evaluated for antiviral activity against influenza A (H1N1 and H3N2) and influenza B virus in MDCK cell cultures. The compounds displayed a confined structure-activity relationship. The N-(2,8-dimethyl-3-oxo-1-thia-4-azaspiro[4.5]dec-4-yl)adamantane-1-carboxamide 3b was the most potent inhibitor [antiviral EC(50): 1.4 ?M against influenza A/H3N2 virus]. Its strong inhibitory effect in a virus hemolysis assay supports that 3b acts as an influenza virus fusion inhibitor by preventing the conformational change of the influenza virus hemagglutinin at low pH.
Ekip : Göktaş F., Vanderlinden E., Naesens L. , Cesur N., Cesur Z. - Adı : Novel Inhibitors of Influenza Virus Fusion: Structure-Activity Relationship And Interaction with the Viral Hemagglutinin
Açıklama : A new class of N-(1-thia-4-azaspiro[4.5]decan-4-yl)carboxamide inhibitors of influenza virus hemagglutinin (HA)-mediated membrane fusion that has a narrow and defined structure-activity relationship was identified. In Madin-Darby canine kidney (MDCK) cells infected with different strains of human influenza virus A/H3N2, the lead compound, 4c, displayed a 50% effective concentration of 3 to 23 muM and an antiviral selectivity index of 10. No activity was observed for A/H1N1, A/H5N1, A/H7N2, and B viruses. The activity of 4c was reduced considerably when added 30 min or later postinfection, indicating that 4c inhibits an early step in virus replication. 4c and its congeners inhibited influenza A/H3N2 virus-induced erythrocyte hemolysis at low pH. 4c-resistant virus mutants, selected in MDCK cells, contained either a single D112N change in the HA2 subunit of the viral HA or a combination of three substitutions, i.e., R220S (in HA1) and E57K (in HA2) and an A-T substitution at position 43 or 96 of HA2. The mutants showed efficiency for receptor binding and replication similar to that of wild-type virus yet displayed an increased pH of erythrocyte hemolysis. In polykaryon assays with cells expressing single-mutant HA proteins, the E57K, A96T, and D112N mutations resulted in 4c resistance, and the HA proteins containing R220S, A96T, and D112N mutations displayed an increased fusion pH. Molecular modeling identified a binding cavity for 4c involving arginine-54 and glutamic acid-57 in the HA2 subunit. Our studies with the new fusion inhibitor 4c confirm the importance of this HA region in the development of influenza virus fusion inhibitors.
Ekip : Vanderlinden E., Göktaş F., Cesur Z., Froeyen M., Reed M.L., Russell C.J., Cesur N., Naesens L - Adı : Synthesis of New Spiroindolinones Incorporating a Benzothiazole Moiety As Antioxidant Agents
Açıklama : 3H-Spiro[1,3-benzothiazole-2,3'-indol]-2'(1'H)-ones 3a-c and 4a-e were synthesized from treating the 5-substituted 1H-indole-2,3-diones with 2-aminothiophenol in ethanol. The structures were confirmed by elemental analyses, spectrometry (IR, (1)H NMR, (13)C NMR, HSQC-2D and LCMS-APCI) and single crystal X-ray analysis. The new compounds were screened for their antioxidant activities such as the Fe(3+)/ascorbate system induced inhibition of lipid peroxidation (LP) in liposomes, trolox equivalent antioxidant capacity (TEAC), scavenging effect on diphenylpicryl hydrazine (DPPH*), and reducing power. These compounds showed potent scavenging activities against DPPH* and 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (ABTS*(+)) radicals, reducing powers, and strong inhibitory capacity on lipid peroxidation. Compound 4a incorporating methyl both at R(1) and R(2) was found to be the most potent antioxidant described in this study. Compounds 3b and 4b were selected as representative compounds by the National Cancer Institute for screening against anticancer activity and these compounds were found to be cytotoxic against CNS cancer cell line SNB-75 in the primary screen.
Ekip : Karali N., Güzel Ö., Özsoy N., Özbey S., Salman A. - Adı : Synthesis and Antimicrobial Activity Evaluation of New 1,2,4-Triazoles and 1,3,4-Thiadiazoles Bearing Imidazo[2,1-b]Thiazole Moiety
Açıklama : A series of 4-alkyl/aryl-2,4-dihydro-5-((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)methyl)-3H-1,2,4-triazole-3-thiones (3a-i) and 2-alkyl/arylamino-5-((6-(4-bromophenyl)imidazo[2,1-b]thiazol-3-yl)methyl)-1,3,4-thiadiazoles (4a-c) were synthesized starting from 6-(4-bromophenyl)imidazo[2,1-b]thiazole-3-acetic acid hydrazide. The newly synthesized compounds were characterized by IR, (1)H NMR, mass and elemental analysis. All compounds were tested for antibacterial and antifungal activities. The antimicrobial activities of the compounds were assessed by the microbroth dilution technique. The compounds were also evaluated for antituberculosis activity against Mycobacterium tuberculosis H37Rv (ATCC 27294). The preliminary results revealed that some of the compounds exhibited promising antimicrobial activities.
Ekip : Ulusoy Güzeldemirci N., Küçükbasmacı Ö. - Adı : Synthesis and Structure-Antituberculosis Activity Relationship of 1H-Indol-2,3-Dione Derivatives
Açıklama : New series of 5-fluoro-1H-indole-2,3-dione-3-thiosemicarbazones 2a-k and 5-fluoro-1-morpholino/piperidinomethyl-1H-indole-2,3-dione-3-thiosemicarbazones 3a-r were synthesized. The structures of the synthesized compounds were confirmed by spectral data, elemental and single crystal X-ray diffraction analysis. The new 5-fluoro-1H-indole-2,3-dione derivatives, along with previously reported 5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones 2l-v, 1-morpholino/piperidinomethyl-5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones 4a-l, and 5-nitro-1H-indole-2,3-dione-3-[(4-oxo-1,3-thiazolidin-2-ylidene)hydrazones] 5a-s, were evaluated for in vitro antituberculosis activity against Mycobacterium tuberculosis H37Rv. Among the tested compounds, 5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones (2p, 2r, and 2s) and its 1-morpholinomethyl derivatives (4a, 4e, 4g, and 4i) exhibited significant inhibitory activity in the primary screen. The antituberculosis activity of molecules with diverse skeletons was investigated by means of the Electronic-Topological Method (ETM). Ten pharmacophores and ten anti-pharmacophores that have been found by this form the basis of the system capable of predicting the structures of potentially active compounds. The forecasting ability of the system has been tested on structures that differ from those synthesized. The probability of correct identification for active compounds was found as equal to 93% in average. To obtain the algorithmic base for the activity prediction, Artificial Neural Networks were used after the ETM (the so-called combined ETM-ANN method). As the result, only 9 pharmacophores and anti-pharmacophores were chosen as the most important ones for the activity. By this, ANNs classified correctly 94.4%, or 67 compounds from 71.
Ekip : Karali N., Gürsoy A., Kandemirli F., Shvets N.M., Kaynak F.B., Özbey S., Kovalishyn V.V., Dimoglo A.S. - Adı : Synthesis and Primary Cytotoxicity Evaluation of New 5-Nitroindole-2,3-Dione Derivatives
Açıklama : A new series of 5-nitro-1H-indole-2,3-dione-3-thiosemicarbazones (3a-k) obtained by condensation of 5-nitro-1H-indole-2,3-dione (1) with N-substituted-thiosemicarbazides (2a-k) were treated with morpholine or piperidine and formaldehyde to yield 1-morpholino/piperidinomethyl-5-nitroindole-2,3-dione-3-thiosemicarbazones (4a-m). The structures of all the compounds were determined by analytical and spectral (IR, 1H-NMR, EIMS) methods. Compounds 3b, 3c, 3f, 3k, 4a, 4c, 4f and 4l chosen as prototypes were evaluated in the National Cancer Institute's 3-cell line, one dose in vitro primary cytotoxicity assay. All the compounds that passed the criteria for activity in this assay were scheduled automatically for evaluation against the full panel of 60 human tumour cell lines at a minimum of five concentrations at 10-fold dilutions. Sulphorhodamine B (SRB) protein assay was used to estimate cell stability or growth. The most active compound was found to be 1-morpholinomethyl-5-nitroindole-2,3-dione-3-N-(chlorophenyl)thiosemicarbazone (4l). This compound demonstrated the most marked effects in the National Cancer Institute's 60 human tumour cell line in vitro screen on a non-small cell lung cancer cell line (HOP-62, log(10)GI(50) value <-8.00) and on leukaemia cell lines (HL-60(TB), log(10)GI(50) value -6.30; MOLT-4, log(10)GI(50) value -6.18).
Ekip : Karali N - Adı : Synthesis of Mannich bases of some 2,5-disubstituted 4-thiazolidinones and evaluation of their antimicrobial activities
Açıklama : 2,5-Disubstituted 4-thiazolidinones, synthesis, Mannich bases, antimicrobial activity.
Ekip : Kocabalkanli, A., Ates, O., Ötük, G. - Adı : New 6-Phenylimidazo[2,1-b]Thiazole Derivatives: Synthesis And Antifungal Activity
Açıklama : New benzylidene-(6-phenylimidazo[2,1-b]thiazol-3-yl)-acetic acid hydrazides, 4-alkyl-1-((6-phenylimidazo[2,1-b]thiazol-3-yl)-acetyl)-3-thiosemicarbazides, 2-aryl-3-((6-phenylimidazo[2,1-b]thiazol-3-yl)-acetamido)-4-thiazolidinones, and 3-alkyl-2-(((6-phenylimidazo[2,1-b]thiazol-3-yl)-acetyl)-hydrazono)-4-thiazolidinones were synthesized from 6-phenylimidazo[2,1-b]thiazole-3-acetic acid hydrazide and evaluated for antifungal activity against three dermatophyte strains using ketoconazole as standard. Several of them were found as effective as the standard against Trichophyton rubrum and Microsporum audounii (MIC=6??g/cm3), whereas the activity of N-benzylidene-(6-phenylimidazo[2,1-b]-thiazol-3-yl)-acetic acid hydrazide against M.
Ekip : Çapan G., Ulusoy N., Ergenç N., Kiraz M
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| Tip | Adı | Açıklama | Ekip |
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| Proje (BAP) | İmidazo[2,1-b]tiyazol türevi yeni bileşikler | BAP Arastırma Projesi, Proje No 4574, | Ulusoy, N. |
| Proje (BAP) | İmidazo[2,1-b]tiyazoller | BAP Arastırma Projesi, Proje No 18903. | Güzeldemirci, N. |
| Proje (BAP) | Heteroaromatik Bileşikler | BAP Arastırma Projesi, Proje No 37447 | Güzeldemirci, N. |
| Proje (Kalkınma Bakanlığı) | Kolşisin türevlerinin sentezi ve kaspaz enzim sistemine etkilerinin incelenmesi | İstanbul Kalkınma Ajansı Desteği ile İTAM-projesi", 2013 | Araman A., Gul, A, Erman B., Cesur Z., Cesur N., Karalı, N. Cihan Üstündağ G |
| Proje (BAP) | Kaspaz-1 ve/veya kaspaz-3 inhibitörü 1H-İndol-2,3-dion 3-(N-sülfamoilfenil) tiyosemikarbazon türevleri: Tasarım, moleküler modelleme, sentez ve biyolojik inceleme | BAP Arastırma Projesi, ÖNAP-36808, 2013 | Karalı, N., Gül, A., Erman, B., Göktaş F., Lack, N., Cihan Üstündağ G., Eraslan P. |
| Proje (TÜBİTAK) | Antimikrobiyal Özelliklere Sahip Çinko (II)-Bisdipikolilamin Koordinasyon Kompleksleri ile Bezeli Polivalan Nanopartiküler ve Moleküler Sistemlerin Geliştirilmesi ve Uygulanması. | TÜBİTAK BİDEB 2232 Programından Destekli Proje, Proje No 114C041, 2013 | Türkyılmaz, S.; Araman, A.O |
| Proje (BAP) | Bazı yeni tiyosemikarbazid ve tiyazolidinon türevi bir seri bileşiğin sentez ve yapı tayinleri | BAP Arastırma Projesi, Proje No 40810, 2013 | Güzeldemirci, N. |
| Proje (BAP) | İndol-Spirotiyazolidinon Türevi Yeni Bileşikler Üzerinde Antiviral Aktivite Çalışmaları | BAP Araştırma Projesi, Proje No 29752, 2013 | Cihan Üstündağ, C., Çapan G |
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