Literature DB >> 21243104

Evaluation of Diarylureas for Activity Against Plasmodium falciparum.

Yiqun Zhang1, Marc Anderson, Jennifer L Weisman, Min Lu, Cindy J Choy, Vincent A Boyd, Jeanine Price, Martina Sigal, Julie Clark, Michele Connelly, Fangyi Zhu, W Armand Guiguemde, Cynthia Jeffries, Lei Yang, Andrew Lemoff, Ally P Liou, Thomas R Webb, Joseph L Derisi, R Kiplin Guy.   

Abstract

A library of diarylurea IGFR inhibitors was screened for activity against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. The 4-aminoquinaldine-derived diarylureas displayed promising antimalarial potency. Further exploration of the B ring of 4-aminoquinaldinyl ureas allowed identification of several quinaldin-4-yl ureas 4{13, 39} and 4{13, 58} sufficiently potent against both 3D7 and K1 strains to qualify as bone fide leads.

Entities:  

Year:  2010        PMID： 21243104      PMCID： PMC3019604          DOI： 10.1021/ml100083c

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  17 in total

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Journal:  Bioorg Med Chem Lett       Date:  2004-04-19       Impact factor: 2.823

Review 2.  Hemoglobin metabolism in the malaria parasite Plasmodium falciparum.

Authors:  S E Francis; D J Sullivan; D E Goldberg
Journal:  Annu Rev Microbiol       Date:  1997       Impact factor: 15.500

3.  Search for new pharmacophores for antimalarial activity. Part II: synthesis and antimalarial activity of new 6-ureido-4-anilinoquinazolines.

Authors:  S Madapa; Z Tusi; A Mishra; K Srivastava; S K Pandey; R Tripathi; S K Puri; S Batra
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4.  High-throughput screening for potent and selective inhibitors of Plasmodium falciparum dihydroorotate dehydrogenase.

Authors:  Jeffrey Baldwin; Carolyn H Michnoff; Nicholas A Malmquist; John White; Michael G Roth; Pradipsinh K Rathod; Margaret A Phillips
Journal:  J Biol Chem       Date:  2005-03-28       Impact factor: 5.157

Review 5.  Drug-resistant malaria.

Authors:  John E Hyde
Journal:  Trends Parasitol       Date:  2005-09-02

6.  A genomic perspective of protein kinases in Plasmodium falciparum.

Authors:  N Srinivasan; A Krupa
Journal:  Proteins       Date:  2005-01-01

Review 7.  Modeling the molecular basis of atovaquone resistance in parasites and pathogenic fungi.

Authors:  Jacques J Kessl; Steven R Meshnick; Bernard L Trumpower
Journal:  Trends Parasitol       Date:  2007-09-07

8.  Artemisinin resistance in Plasmodium falciparum malaria.

Authors:  Arjen M Dondorp; François Nosten; Poravuth Yi; Debashish Das; Aung Phae Phyo; Joel Tarning; Khin Maung Lwin; Frederic Ariey; Warunee Hanpithakpong; Sue J Lee; Pascal Ringwald; Kamolrat Silamut; Mallika Imwong; Kesinee Chotivanich; Pharath Lim; Trent Herdman; Sen Sam An; Shunmay Yeung; Pratap Singhasivanon; Nicholas P J Day; Niklas Lindegardh; Duong Socheat; Nicholas J White
Journal:  N Engl J Med       Date:  2009-07-30       Impact factor: 91.245

9.  Cytotoxic effects of inhibitors of de novo pyrimidine biosynthesis upon Plasmodium falciparum.

Authors:  K K Seymour; S D Lyons; L Phillips; K H Rieckmann; R I Christopherson
Journal:  Biochemistry       Date:  1994-05-03       Impact factor: 3.162

Review 10.  Protein kinases of the human malaria parasite Plasmodium falciparum: the kinome of a divergent eukaryote.

Authors:  Pauline Ward; Leila Equinet; Jeremy Packer; Christian Doerig
Journal:  BMC Genomics       Date:  2004-10-12       Impact factor: 3.969
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  15 in total

1.  Progress in antischistosomal N,N'-diaryl urea SAR.

Authors:  Jianbo Wu; Chunkai Wang; Derek Leas; Mireille Vargas; Karen L White; David M Shackleford; Gong Chen; Austin G Sanford; Ryan M Hemsley; Paul H Davis; Yuxiang Dong; Susan A Charman; Jennifer Keiser; Jonathan L Vennerstrom
Journal:  Bioorg Med Chem Lett       Date:  2017-12-29       Impact factor: 2.823

2.  Synthesis of unsymmetrical diarylureas via Pd-catalyzed C-N cross-coupling reactions.

Authors:  Simon Breitler; Nathan J Oldenhuis; Brett P Fors; Stephen L Buchwald
Journal:  Org Lett       Date:  2011-05-23       Impact factor: 6.005

3.  Development of 1-((1,4-trans)-4-Aryloxycyclohexyl)-3-arylurea Activators of Heme-Regulated Inhibitor as Selective Activators of the Eukaryotic Initiation Factor 2 Alpha (eIF2α) Phosphorylation Arm of the Integrated Endoplasmic Reticulum Stress Response.

Authors:  Revital Yefidoff-Freedman; Jing Fan; Lu Yan; Qingwen Zhang; Guillermo Rodrigo Reis Dos Santos; Sandeep Rana; Jacob I Contreras; Rupam Sahoo; Debin Wan; Jun Young; Karina Luiza Dias Teixeira; Christophe Morisseau; Jose Halperin; Bruce Hammock; Amarnath Natarajan; Peimin Wang; Michael Chorev; Bertal H Aktas
Journal:  J Med Chem       Date:  2017-06-19       Impact factor: 7.446

4.  Identification of novel phenyl butenonyl C-glycosides with ureidyl and sulfonamidyl moieties as antimalarial agents.

Authors:  K Kumar G Ramakrishna; Sarika Gunjan; Akhilesh Kumar Shukla; Venkata Reddy Pasam; Vishal M Balaramnavar; Abhisheak Sharma; Swati Jaiswal; Jawahar Lal; Renu Tripathi; Ravishankar Ramachandran; Rama Pati Tripathi
Journal:  ACS Med Chem Lett       Date:  2014-06-02       Impact factor: 4.345

5.  Cyclopropyl Carboxamides: A New Oral Antimalarial Series Derived from the Tres Cantos Anti-Malarial Set (TCAMS).

Authors:  Lourdes Rueda; Isabel Castellote; Julia Castro-Pichel; Maria J Chaparro; Juan Carlos de la Rosa; Adolfo Garcia-Perez; Mariola Gordo; Maria Belen Jimenez-Diaz; Albane Kessler; Simon J F Macdonald; Maria Santos Martinez; Laura M Sanz; Francisco Javier Gamo; Esther Fernandez
Journal:  ACS Med Chem Lett       Date:  2011-08-29       Impact factor: 4.345

6.  Novel diaryl ureas with efficacy in a mouse model of malaria.

Authors:  John W Anderson; Dimitri Sarantakis; Jacek Terpinski; T R Santha Kumar; Han-Chun Tsai; Mack Kuo; Arba L Ager; William R Jacobs; Guy A Schiehser; Sean Ekins; James C Sacchettini; David P Jacobus; David A Fidock; Joel S Freundlich
Journal:  Bioorg Med Chem Lett       Date:  2012-12-20       Impact factor: 2.823

7.  Activities of N,N'-Diarylurea MMV665852 analogs against Schistosoma mansoni.

Authors:  Noemi Cowan; Philipp Dätwyler; Beat Ernst; Chunkai Wang; Jonathan L Vennerstrom; Thomas Spangenberg; Jennifer Keiser
Journal:  Antimicrob Agents Chemother       Date:  2015-01-12       Impact factor: 5.191

8.  Diaryl Ureas as an Antiprotozoal Chemotype.

Authors:  Derek A Leas; Austin G Sanford; Jianbo Wu; Monica Cal; Marcel Kaiser; Sergio Wittlin; Ryan M Hemsley; Elyssa B Darner; LeeAnna M Lui; Paul H Davis; Jonathan L Vennerstrom
Journal:  ACS Infect Dis       Date:  2021-05-10       Impact factor: 5.578

9.  In Vitro, In Vivo, and Absorption, Distribution, Metabolism, and Excretion Evaluation of SF5-Containing N,N'-Diarylureas as Antischistosomal Agents.

Authors:  Alexandra Probst; Eugènia Pujol; Cécile Häberli; Jennifer Keiser; Santiago Vázquez
Journal:  Antimicrob Agents Chemother       Date:  2021-07-26       Impact factor: 5.191

10.  Identification of di-substituted ureas that prevent growth of trypanosomes through inhibition of translation initiation.

Authors:  Fabricio Castro Machado; Caio Haddad Franco; Jose Vitorino Dos Santos Neto; Karina Luiza Dias-Teixeira; Carolina Borsoi Moraes; Ulisses Gazos Lopes; Bertal Huseyin Aktas; Sergio Schenkman
Journal:  Sci Rep       Date:  2018-03-20       Impact factor: 4.379
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