Medicinal chemistry progression of antimalarial hits from phenotypic whole cell screening of SoftFocus libraries

被引：4
|
作者：
Cheuka, Peter M. [1 ,2 ]
Mayoka, Godfrey [1 ,3 ]
Okombo, John [4 ]
Chibale, Kelly [1 ,5 ,6 ,7 ]
机构：
[1] Univ Cape Town, Dept Chem, Cape Town, South Africa
[2] Univ Zambia, Dept Chem, Lusaka, Zambia
[3] Jomo Kenyatta Univ Agr & Technol, Sch Pharm, Dept Pharmacol & Pharmacognosy, Nairobi, Kenya
[4] Columbia Univ, Dept Microbiol & Immunol, New York, NY USA
[5] Univ Cape Town, Drug Discovery & Dev Ctr H3D, Cape Town, South Africa
[6] Univ Cape Town, Inst Infect Dis & Mol Med, Cape Town, South Africa
[7] Univ Cape Town, South African Med Res Council, Drug Discovery & Dev Res Unit, Cape Town, South Africa
来源：
MEDICINAL CHEMISTRY APPROACHES TO MALARIA AND OTHER TROPICAL DISEASES | 2019年 / 53卷
关键词：
ANTIPLASMODIAL IMIDAZOPYRIDAZINE HITS; HUMAN MALARIA PARASITE; PLASMODIUM-FALCIPARUM; PROTEIN-KINASE; SUBSTITUTED IMIDAZOPYRIDAZINES; POTENT INHIBITORS; OPTIMIZATION; IDENTIFICATION; DERIVATIVES; SOLUBILITY;
D O I：
10.1016/bs.armc.2019.04.001
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
引用
收藏
页码：25 / 71
页数：47
相关论文
共 50 条
  • [31] Colworth prize lecture 2016: exploiting new biological targets from a whole-cell phenotypic screening campaign for TB drug discovery
    Moynihan, Patrick Joseph
    Besra, Gurdyal S.
    MICROBIOLOGY-SGM, 2017, 163 (10): : 1385 - 1388
  • [32] Identification of Bacterial Surface Antigens by Screening Peptide Phage Libraries Using Whole Bacteria Cell-Purified Antisera
    Hu, Yun-Fei
    Zhao, Dun
    Yu, Xing-Long
    Hu, Yu-Li
    Li, Run-Cheng
    Ge, Meng
    Xu, Tian-Qi
    Liu, Xiao-Bo
    Liao, Hua-Yuan
    FRONTIERS IN MICROBIOLOGY, 2017, 8
  • [33] Designing new antimalarial hits from African medicinal plants at the University of Buea (Cameroon); Part I: Isolation, in vitro activity, in silico "drug-likeness" and Pharmacokinetic profiles
    Zofou, D.
    INTERNATIONAL JOURNAL OF INFECTIOUS DISEASES, 2016, 45 : 131 - 131
  • [34] Cell-Based Medicinal Chemistry Optimization of High-Throughput Screening (HTS) Hits for Orally Active Antimalarials. Part 1: Challenges in Potency and Absorption, Distribution, Metabolism, Excretion/Pharmacokinetics (ADME/PK)
    Chatterjee, Arnab K.
    JOURNAL OF MEDICINAL CHEMISTRY, 2013, 56 (20) : 7741 - 7749
  • [35] From Medicinal Chemistry to Functionalized Biomaterials: Development of Graftable RGD-Peptitomimetics for Cell Adhesion and Cell Addressing
    Marchand-Brynaert, Jacqueline
    THERMEC 2009, PTS 1-4, 2010, 638-642 : 612 - 617
  • [36] Massive virtual library (MVL) screening at biogen: An integrated approach from medicinal chemistry design to decision.
    Chin, DN
    Chuaqui, C
    van Vlijmen, H
    Zhang, X
    Petter, R
    Singh, J
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2002, 224 : U343 - U343
  • [37] Adaptation of spectroscopic tools from high-throughput screening of combinatorial chemistry libraries to process chemical analysis
    Potyrailo, RA
    FIBER OPTIC SENSOR TECHNOLOGY AND APPLICATIONS 2001, 2001, 4578 : 366 - 377
  • [38] Rapid screening method for quantitation of bacterial cell lipids from whole cells
    Izard, J
    Limberger, RJ
    JOURNAL OF MICROBIOLOGICAL METHODS, 2003, 55 (02) : 411 - 418
  • [39] Combined Whole-Cell High-Throughput Functional Screening for Identification of New Nicotinamidases/Pyrazinamidases in Metagenomic/Polygenomic Libraries
    Zapata-Perez, Ruben
    Garcia-Saura, Antonio G.
    Jebbar, Mohamed
    Golyshin, Peter N.
    Sanchez-Ferrer, Alvaro
    FRONTIERS IN MICROBIOLOGY, 2016, 7
  • [40] NEW EFFORTS AIMED AT REPLACING ACTS: THE IDENTIFICATION OF NOVEL, DRUG-LIKE, AND FAST-ACTING ANTIMALARIAL COMPOUNDS FROM A PHENOTYPIC SCREENING
    Rueda, Lourdes
    AMERICAN JOURNAL OF TROPICAL MEDICINE AND HYGIENE, 2015, 93 (04): : 295 - 295
12345