Literature DB >> 19058973

Search for new pharmacophores for antimalarial activity. Part I: synthesis and antimalarial activity of new 2-methyl-6-ureido-4-quinolinamides.

S Madapa1, Z Tusi, D Sridhar, A Kumar, M I Siddiqi, K Srivastava, A Rizvi, R Tripathi, S K Puri, G B Shiva Keshava, P K Shukla, S Batra.   

Abstract

A total of 80 new 2-methyl-6-ureido-4-quinolinamides were synthesized and evaluated for their antimalarial activity. Several analogs elicited the antimalarial effect at MIC of 0.25 mg/mL against the chlooquine-sensitive P. falciparum strain. The IC(50) values of the active compounds were observed to be in ng/mL range and two of the analogs have better IC(50) value than the standard chloroquine. In the in vivo assay against mdr CQ resistant P. yoelii N67/P. yoelii nigeriensis, however, none of the compound showed complete suppression of parasitemia on day 7. One of the compounds displayed significant antibacterial effect against several strains of bacteria and was many-fold better than the standard drug gentamicin.

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Year:  2008        PMID: 19058973     DOI: 10.1016/j.bmc.2008.11.021

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  5 in total

1.  Evaluation of Diarylureas for Activity Against Plasmodium falciparum.

Authors:  Yiqun Zhang; 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
Journal:  ACS Med Chem Lett       Date:  2010-12-09       Impact factor: 4.345

2.  Quinoline: A versatile heterocyclic.

Authors:  Akranth Marella; Om Prakash Tanwar; Rikta Saha; Mohammad Rahmat Ali; Sandeep Srivastava; Mymoona Akhter; Mohammad Shaquiquzzaman; Mohammad Mumtaz Alam
Journal:  Saudi Pharm J       Date:  2012-03-29       Impact factor: 4.330

3.  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

4.  Biological evaluation, docking and molecular dynamic simulation of some novel diaryl urea derivatives bearing quinoxalindione moiety.

Authors:  Sedighe Sadeghian-Rizi; Ghadamali Ali Khodarahmi; Amirhossein Sakhteman; Ali Jahanian-Najafabadi; Mahboubeh Rostami; Mahmoud Mirzaei; Farshid Hassanzadeh
Journal:  Res Pharm Sci       Date:  2017-12

5.  Antimalarial activity of ultra-short peptides.

Authors:  Lemuel Pérez-Picaso; Benjamín Velasco-Bejarano; A Berenice Aguilar-Guadarrama; Rocío Argotte-Ramos; María Yolanda Rios
Journal:  Molecules       Date:  2009-12-08       Impact factor: 4.411

  5 in total

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