Solid phase synthesis and biological evaluation of 1, 3, 5 triazine derivatives

... 1,3 ,5- Triazine Derivatives 11 1.2.2 Synthesis of 1,3 ,5- Triazine Derivatives 14 1.2.2.1 Solution phase synthesis of 2,4,6-trisubtituted -1,3 ,5- triazine 14 1.2.2.2 Solid- Phase Synthesis of 1,3 ,5- Triazine ... 65 3.4 Synthesis of 1,3 ,5- triazine Analogs via Guanidium Azolides 80 3 .5 Synthesis of 1,3 ,5- traizine-2,4-diones 3-17 81 3 .5. 1 Solution -Phase synthesis of 3-17 81 3 .5. 2 Solid- Phase Synthesis of ... the synthesis of 1,3 ,5- triazine, 7476 this section will concentrate on the recent solution -phase and solid- phase syntheses of the 1,3 ,5- triazine derivatives 1.2.2.1 Solution phase synthesis of...

Part 1 total synthesis and biological evaluation of antillatoxin and fragments part II synthetic studies towards the total synthesis of cytochalasans and tuberostemonine

... PART I TOTAL SYNTHESIS AND BIOLOGICAL EVALUATION OF ANTILLATOXIN AND FRAGMENTS PART II SYNTHETIC STUDIES TOWARDS THE TOTAL SYNTHESIS OF CYTOCHALASANS AND TUBEROSTEMONINE APPENDIX ... Biological Evaluation of Antillatoxin and Fragments 1. 1 Historical Background 1. 2 Previous Synthetic Studies 1. 3 Our Retrosynthetic Analysis of Antillatoxin 11 1. 4 Results and Discussion 15 1. 5 ... 1. 5 Biological Evaluation of Antillatoxin and Fragments Using Zebrafish Embryo 30 1. 6 Conclusion 44 1. 7 Experimental 45 Part II Chapter 2: Synthetic Studies Towards the Total Synthesis of Cytochalasans...

design, synthesis, and biological evaluation of new anti-cancer nitrogen-containing combretastatins and novel cysteine protease inhibitors for the treatment of chagas

... Evaluation of New Anti-cancer Nitrogen-Containing Combretastatins and Novel Cysteine Protease Inhibitors for the Treatment of Chagas Rogelio Siles Mentor: Kevin G Pinney, Ph.D In an effort to combat ... Derivatives of Combretastatins A-1 and A-4 66 Synthesis of Cold Precursors of Radio-labeled Combretastatins CA-1 and CA-4 70 Synthesis of OXi8007 and a Nitrogen-Based Indole 75 Biological and Biochemical ... Biochemical Evaluation of Cysteine Protease Inhibitors: Novel Compounds for Chagas Disease Treatment 143 Introduction 143 Background 144 Chemotherapy of Chagas Disease 148 Chapter Seven: Materials and...

Synthesis and biological evaluation of 2 substituted benzimidazole derivatives

... time in second (Mean ± SEM) 0h 2h 3h 4h 1.56 ± 0.16 2. 16 ± 0.16 2. 0 ± 0 .25 2. 16 ± 0.16 2. 0 ± 0 .25 2. 0 ± 0 .25 1.61 ± 0.30 2. 16 ± 0.30 2. 0 ± 0 .25 2. 16 ± 0.16 2. 0 ± 0 .25 2. 16 ± 0.16 Control Std 3a 3b ... 14.38; found C 57 .29 , H 3.65, N 14.45 Synthesis and biological evaluation of 2- substituted benzimidazole derivatives 2. 2 .2. 2 (1H-Benoimidazol -2- ylmethyl)- (2, 3-dichloro-phenyl)amine (3b) Light ... MS: 26 8 [M+]; Anal calcd for C14H12N4O2 (26 8): C 62. 68, H 4.51, N 20 .88; found C 62. 74, H 4.49, N 20 .78 2. 2 .2. 10 (1H-Benzimidazol -2- ylmethyl)-(4-iodo-phenyl)-amine (3j) Colorless powder; m.p .22 1 22 3...

Part i synthesis and biological evaluation of phosphoglycolipid PGL1 analogues part II synthesis and biological evaluation of andrographolide analogues

... PART I SYNTHESIS AND BIOLOGICAL EVALUATION OF PHOSPHOGLYCOLIPID PGL1 ANALOGUES PART II SYNTHESIS AND BIOLOGICAL EVALUATION OF ANDROGRAPHOLIDE ANALOGUES HADHI WIJAYA (BSc (Hons.) NUS) A THESIS ... CONTENTS iv SUMMARY vii LIST OF TABLES ix LIST OF FIGURES xi LIST OF SCHEMES xv LIST OF ABBREVIATIONS xvii CHAPTER INTRODUCTION 1.1 Overview 1.2 Definition, Classification and sources of Natural Products ... treatment of various diseases In this thesis, the synthesis and biological evaluation of analogues of two natural products are presented In Chapter 2, the synthesis and biological evaluation of phosphoglycolipid...

Synthesis and biological evaluation of isoindigo derivatives as anti proliferative agents

... functionalized isoindigos as antiproliferative agents, the aim of this thesis was to investigate medicinal chemistry approaches towards the design and synthesis of functionalized isoindigos with ... of isoindigos without compromising biological activity 1.5 Biological properties of functionalized isoindigos 1.5.1 Mode of action of meisoindigo Meisoindigo is the most widely investigated of ... understanding of the isoindigo scaffold and 19 to provide an objective assessment of its potential as a source of potent and drug-like compounds 20 Chapter 2: Functionalized isoindigos as cyclin-dependent...

Synthesis and biological evaluation of natural products and their analogs as new cancer chemotherapeutic agents

... SYNTHESIS AND BIOLOGICAL EVALUATION OF NATURAL PRODUCTS AND THEIR ANALOGS AS NEW CANCER CHEMOTHERAPEUTIC AGENTS FANG ZHANXIONG (B.Sc.(Hons.) NUS) A THESIS SUBMITTED FOR THE DEGREE OF DOCTOR OF ... production of a large number of analogs with the basic template.56 Epothilone D has shown to be at least as cytotoxic as paclitaxel against a range of cancer cell lines and one of 15 the analogs has ... as anticancer agents due to their high selectivity against A549 cells In Chapter 3, the synthesis of lignan natural products as potential anti-tumor agents was described After the synthesis of...

Design, synthesis and biological evaluation of inhibitors of flavivirus NS2B NS3 protease

... the thesis involves the design, synthesis and biological evaluation of inhibitors of Dengue and West Nile virus NS2B- NS3 protease For the design of dengue NS2B- NS3 protease inhibitors, we were inspired ... DEN2 NS2b- NS3 protease 60 Chapter 4: Synthesis and biological evaluation of small molecule inhibitors of West Nile Virus NS2B/ NS3 Protease 4.1 63 4.1.1 Chemistry 65 4.1.2 4.2 Introduction Biological ... kD VTA↓G, Unknown NS2B 14 kD RR↓S, NS2B- NS3 Protease NS3 70 kD RR↓S, NS2B- NS3 Protease NS4A 16 kD RR↓G, NS2B- NS3 Protease NS4B 28 kD VAA↓N, Signalase NS5 103 kD RR↓G, NS2B- NS3 Protease Function/enzymatic...

Synthesis and biological investigation of pyrimido 1,2 a 1,3,5 triazine and its analogues 2

... Methionine aminopeptidase Translation, ribosomal structure and biogenesis 2ea2, 1boa, 2gg8, 2p98, 2g6p 2. 948 0.58 62 43 1-aminocyclopropane-1carboxylate deaminase Amino acid transport and metabolism ... hepatocyte growth factor activity 3f 82, 3cd8 2. 956 0 .27 23 Branched-chain-amino-acid aminotransferase, mitochondrial Amino acid transport and metabolism 1kta, 1kt8 2. 94 0 .26 24 Renin Renin is a ... Met- and Leu-enkephalins by cleavage of a Gly-Phe bond 1r1i, 1y8j 3 .29 8 0.3548 3.644 0 .22 58 17 20 21 Amino acid transport and metabolism 22 DNA polymerase I, thermostable Replication, recombination...

Synthesis and biological investigation of pyrimido,1,2 a ,1,3,5,triazine and its analogues 1

... derivatives Anti-fungal activity was stated for derivatives 10 1a against Microsporum canis and average affinity of 10 1b for serotoninergic 5-HT 1A and 5-HT2B receptors was also published by Lucry and ... cyclocondensation of biguanide and its analogues 13 2 with ethyl acetoacetate gave 12 8 -13 1 as reported by Curd and Rose92 (Scheme 39, Method A) There was a need to develop an alternative method of obtaining ... catalyzed cyclization of potassium N,N-dicyanobenzamidine 11 2 with methyl anthranilate 11 1 in methanol gave triazino[2 ,1- b]quinazolone 11 4 instead of triazino [1, 2 -a] quinazolone 11 4’ In order to confirm...

Design, synthesis and biological studies of coumarin based probes and tetrahydrolipstatin analogs 1

... NBD-sarcosine (1. 14) and 7-dimethylamino coumarin- 4-acetic acid (1. 15).9 R O R O MeO O O O H O O O O O O O O O 1. 12 R = OAc 1. 16 R = 1. 14 1. 17 R = 1. 15 O2 N 1. 13 R = OAc 1. 18 R = 1. 14 1. 19 R = 1. 15 N N ... F Eur Pat 19 98, EP08479 91 13 Paterson, M J.; Jovanovic, A Arkivoc, 2 010 , 10 , 11 -16 14 Nielsen, O.; Burchardt, O Synthesis, 19 91, 819 -8 21 15 Dey, B B J Chem Soc 19 15, 10 7, 16 06 -16 51 16 (a) Pederson, ... enantiosynthesis of THL 54 4 .11 Kumaraswamy’s synthesis of THL 56 4 .12 Synthesis of β-hydroxy aldehyde 4. 71 57 4 .13 Davies’ synthesis of THL 57 4 .14 Raghavan’ synthesis of THL 59 4 .15 Hanson’ synthesis of...

Design, synthesis and biological studies of coumarin based probes and tetrahydrolipstatin analogs

... 125.7577890 MHz DATE_d : DECNUC : off NS 39.9955 39.8279 39.7551 39.6968 39.6603 39.4927 39.3324 39.1648 38.9972 38.8514 38.7057 BF1 : 137 Oct 23 2006 NUCLEUS : off PULPROG : zgpg30 SFO1 : 125.7709936 ... Parameters *** O sg1023~1 : *** Acquisition Parameters *** O 2.19 Oct 23 2006 : off NS O : DECNUC N : 125.7577890 MHz DATE_d : 57 off PULPROG : N H BF1 NUCLEUS : N H (1) N O : PROCNO 34.0345 33.9106 O ... MHz 1.00 Hz 32768 *** 1D NMR Plot Parameters *** O N H (1) 35.0 : SF 60 50 40 30 20 10 60.62 Hz off 220 39.6968 38.8514 38.7057 38.4506 34.0345 33.9106 69.5313 69.4875 68.9774 68.9556 97.4419...

Báo cáo khoa học: Phenylalanine-independent biosynthesis of 1,3,5,8-tetrahydroxyxanthone A retrobiosynthetic NMR study with root cultures of Swertia chirata docx

... phosphoenolpyruvate unit by decarboxylation of Cambridge Isotope Laboratories (Andover, MA, USA) [U-13C9]Cinnamic acid was prepared by treatment of 13 L-[U- C9]phenylalanine with phenylalanine ammonia-lyase ... biosynthetically obtained via the shikimate pathway of aromatic amino-acid biosynthesis (Fig 1) The aromatic ring of phenylalanine reﬂects the labelling patterns of C2–C3 of phosphoenolpyruvate and of ... 1H -NMR spectra As an Fig 13C -NMR spectrum of 1,3,5,8-tetrahydroxyxanthone (A) Spectrum of a sample with natural 13C abundance; (B) spectrum of a sample from the experiment with [1-13C]glucose Asterisks...

Báo cáo khoa học: Structural and biological effects of a b2- or b3-amino acid insertion in a peptide Application to molecular recognition of substance P by the neurokinin-1 receptor ppt

... control at t ¼ for each peptide The percentage of degradation was calculated by comparing the area of the peaks of the intact peptide at t ¼ and t ¼ 60 Binding assays Binding assays were carried ... [33], the peptides containing a b-amino acid substitution in position have increased stability compared to the corresponding a- amino -acid- containing peptides Therefore it is possible to increase peptide ... acid incorporation When Phe7 or Phe8 are replaced by b2-HPhe, the corresponding analogues are weak competitors of speciﬁc NK-1 binding sites These amino acids are in the helical domain of SP which...

Báo cáo khoa học: Total chemical synthesis and NMR characterization of the glycopeptide tx5a, a heavily post-translationally modiﬁed conotoxin, reveals that the glycan structure is a-D-Gal-(1ﬁ3)-a-D-GalNAc pot

... two-dimensional NMR spectroscopy The data clearly indicated that the tx 5a glycan is in an a- D-Gal-(1fi3) -a- D-GalNAc configuration Taken together, these data demonstrate that two Conus glycopeptides ... glycosylated at position Taken together, these data identified the glycan as a- D-Gal-(1fi3 )a- D-GalNAc There are several NOEs between the glycan and the glycopeptide side-chain atoms of tx 5a, which ... b-D-Gal-(1fi3) -a- D-GalNAc containing glycopeptide, and native tx 5a were simultaneously incubated and reacted with the same vial of the enzyme b-galactosidase Native tx 5a, tx 5a hydrophilic, and tx5a...

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Từ khóa: pyrazolo 1 5 a 1 3 5 triazine derivatives as inhibitors of thymidine phosphorylase valenti p da re p rampa a montanari p carrara m cima l 1993 benzo gamma pyrone analogues of geiparvarin synthesis and biological evaluation against b16 melanoma cells anticancer drug des 8 pp 349 360 biochemical and biological evaluation of cc 1065 analogs and conjugates with polyamides verification optimization synthesis and performance evaluation of real time systems solid phase extraction and hplc analysis of anthocyanidins from fruits and vegetables pyrazolo 1 5 a 1 3 5 triazines by concurrent formation of both the 1 3 5 triazine and pyrazole rings 2 4 bis 3 5 dichloroanilinyl 6 pyrrolidinyl 1 3 5 triazine 24 r1 r2 3 5 dichloroph melamin là một bazo hữu cơ ít tan trong nước có công thức hóa học là c3h6n6 danh pháp theo iupac là 1 3 5 triazine 2 4 6 triamine pyrazolo 1 5 a 1 3 5 triazines from 1 3 5 triazine scaffold traceless solid phase synthesis of 1 7 disubstituted purines synthesis thermodynamic behavior and biological properties of metal ion specific sequestering agents for iron and the actinides a semi automated method for the determination of fluticasone propionate cci187811 in human plasma using solid phase extraction and liquid chromatography tandem mass spectrometry nmr of solid phase synthesis resins solid phase microextraction for the analysis of aromas and flavors biological and biotechnological evaluation of carbon dynamics in field experiments Báo cáo thực tập tại nhà thuốc tại Thành phố Hồ Chí Minh năm 2018 Nghiên cứu tổ hợp chất chỉ điểm sinh học vWF, VCAM 1, MCP 1, d dimer trong chẩn đoán và tiên lượng nhồi máu não cấp Biện pháp quản lý hoạt động dạy hát xoan trong trường trung học cơ sở huyện lâm thao, phú thọ Giáo án Sinh học 11 bài 13: Thực hành phát hiện diệp lục và carôtenôit Quản lý hoạt động học tập của học sinh theo hướng phát triển kỹ năng học tập hợp tác tại các trường phổ thông dân tộc bán trú huyện ba chẽ, tỉnh quảng ninh Phối hợp giữa phòng văn hóa và thông tin với phòng giáo dục và đào tạo trong việc tuyên truyền, giáo dục, vận động xây dựng nông thôn mới huyện thanh thủy, tỉnh phú thọ Phát triển mạng lưới kinh doanh nước sạch tại công ty TNHH một thành viên kinh doanh nước sạch quảng ninh Trả hồ sơ điều tra bổ sung đối với các tội xâm phạm sở hữu có tính chất chiếm đoạt theo pháp luật Tố tụng hình sự Việt Nam từ thực tiễn thành phố Hồ Chí Minh (Luận văn thạc sĩ)Nghiên cứu, xây dựng phần mềm smartscan và ứng dụng trong bảo vệ mạng máy tính chuyên dùng Định tội danh từ thực tiễn huyện Cần Giuộc, tỉnh Long An (Luận văn thạc sĩ)Sở hữu ruộng đất và kinh tế nông nghiệp châu ôn (lạng sơn) nửa đầu thế kỷ XIX Tổ chức và hoạt động của Phòng Tư pháp từ thực tiễn tỉnh Phú Thọ (Luận văn thạc sĩ)Tăng trưởng tín dụng hộ sản xuất nông nghiệp tại Ngân hàng Nông nghiệp và Phát triển nông thôn Việt Nam chi nhánh tỉnh Bắc Giang (Luận văn thạc sĩ)Tranh tụng tại phiên tòa hình sự sơ thẩm theo pháp luật tố tụng hình sự Việt Nam từ thực tiễn xét xử của các Tòa án quân sự Quân khu (Luận văn thạc sĩ)Giáo án Sinh học 11 bài 15: Tiêu hóa ở động vật Giáo án Sinh học 11 bài 14: Thực hành phát hiện hô hấp ở thực vật Chiến lược marketing tại ngân hàng Agribank chi nhánh Sài Gòn từ 2013-2015 Đổi mới quản lý tài chính trong hoạt động khoa học xã hội trường hợp viện hàn lâm khoa học xã hội việt nam HIỆU QUẢ CỦA MÔ HÌNH XỬ LÝ BÙN HOẠT TÍNH BẰNG KIỀM MÔN TRUYỀN THÔNG MARKETING TÍCH HỢP