Design, synthesis and biological evaluation of inhibitors of flavivirus NS2B NS3 protease
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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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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...
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Tài liệu Báo cáo khoa học: Design, structure and biological activity of b-turn peptides of CD2 protein for inhibition of T-cell adhesion ppt
... peptides from rat CD2 may bind to human CD58 Human -CD2 and rat -CD2 have high 3D structure similarity Comparison of 3D structures of hCD2 from CD2 CD58 complex [30] and the structure of rat CD2 [36] using ... biological activity and to study the effect of reducing the chain length of peptides on Ó FEBS 2004 Design of peptides for T-cell adhesion inhibition (Eur J Biochem 271) 2879 biological activity, ... N- and C-termini A comparison of the b-turn structure of cER with the similar region in the crystal structure of rat and human CD2 was carried out In the rat CD2 crystal structure, the b-turn structure...
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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...
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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...
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Báo cáo Y học: Synthesis, conformational analysis and biological activity of cyclic analogs of the octadecaneuropeptide ODN Design of a potent endozepine antagonist pot
... cyclic analogs of OP in order to generate possible agonists and antagonists of ODN We have determined the secondary structure of the cyclic OP analogs by two-dimensional 1H-NMR and molecular dynamic ... rat astrocytes In conclusion, we have shown that head-to-tail cyclization of the ODN agonist OP and the weak antagonist [D -Leu5]OP enhances their biological activity on rat astrocytes leading ... respectively, potent agonistic and antagonistic activities both on calcium mobilization and on polyphosphoinositide metabolism in rat astroglial cells The secondary structure of these two ODN analogs has...
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DELIVERING HEALTH EDUCATION VIA THE WEB: DESIGN AND FORMATIVE EVALUATION OF A DISCOURSE-BASED LEARNING ENVIRONMENT pot
... Education via the Web: Design and Formative Evaluation The Health and Health Behaviour subject was chosen as an appropriate subject in which to implement a Web-based learning environment and ... formative evaluation of the site was conducted 470 Delivering Health Education via the Web: Design and Formative Evaluation FORMATIVE EVALUATION METHODOLOGY The formative evaluation of the prototype ... Postgraduate Award and a Social Sciences and Humanities Research Council of Canada Doctoral Fellowship 474 Delivering Health Education via the Web: Design and Formative Evaluation REFERENCES Agostinho,...
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Từ khóa: biochemical and biological evaluation of cc 1065 analogs and conjugates with polyamidessynthesis thermodynamic behavior and biological properties of metal ion specific sequestering agents for iron and the actinidesdesign and performance evaluation of dryersdesign and performance evaluation of membrane systemsdesign and performance evaluation of evaporationsynthesis and electrochemical performance of lifepo4 by solgel methodsynthesis and electrochemical performance of graphenepolyanilinesynthesis and electrochemical performance of graphenelike ws2quantitative and qualitative evaluation of darpa communicator spoken dialogue systemsdiagnostic value and prognostic evaluation of presepsin for sepsis in an emergency departmentmethods of quantitative and qualitative evaluation of proteinoutline the methods of quantitative and qualitative evaluation of proteinquantitative and qualitative evaluation of proteinfinancial and economic analysis and efficiency evaluation of investment projects and programsmolecular biology and biological functions of endothelinBáo cáo quy trình mua hàng CT CP Công Nghệ NPVNghiên cứu sự hình thành lớp bảo vệ và khả năng chống ăn mòn của thép bền thời tiết trong điều kiện khí hậu nhiệt đới việt namMột số giải pháp nâng cao chất lượng streaming thích ứng video trên nền giao thức HTTPGiáo án Sinh học 11 bài 13: Thực hành phát hiện diệp lục và carôtenôitGiáo án Sinh học 11 bài 13: Thực hành phát hiện diệp lục và carôtenôitGiáo án Sinh học 11 bài 13: Thực hành phát hiện diệp lục và carôtenôitĐỒ ÁN NGHIÊN CỨU CÔNG NGHỆ KẾT NỐI VÔ TUYẾN CỰ LY XA, CÔNG SUẤT THẤP LPWANĐỒ ÁN NGHIÊN CỨU CÔNG NGHỆ KẾT NỐI VÔ TUYẾN CỰ LY XA, CÔNG SUẤT THẤP LPWANPhát triển mạng lưới kinh doanh nước sạch tại công ty TNHH một thành viên kinh doanh nước sạch quảng ninhPhát triển du lịch bền vững trên cơ sở bảo vệ môi trường tự nhiên vịnh hạ longĐịnh tội danh từ thực tiễn huyện Cần Giuộc, tỉnh Long An (Luận văn thạc sĩ)Tìm hiểu công cụ đánh giá hệ thống đảm bảo an toàn hệ thống thông tinKiểm sát việc giải quyết tố giác, tin báo về tội phạm và kiến nghị khởi tố theo pháp luật tố tụng hình sự Việt Nam từ thực tiễn tỉnh Bình Định (Luận văn thạc sĩ)Giáo án Sinh học 11 bài 15: Tiêu hóa ở động vậtchuong 1 tong quan quan tri rui roNguyên tắc phân hóa trách nhiệm hình sự đối với người dưới 18 tuổi phạm tội trong pháp luật hình sự Việt Nam (Luận văn thạc sĩ)Giáo án Sinh học 11 bài 14: Thực hành phát hiện hô hấp ở thực vậtHIỆU QUẢ CỦA MÔ HÌNH XỬ LÝ BÙN HOẠT TÍNH BẰNG KIỀMMÔN TRUYỀN THÔNG MARKETING TÍCH HỢPQUẢN LÝ VÀ TÁI CHẾ NHỰA Ở HOA KỲ