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antimalarial agents

NOT Open Access | Conjugation of N-acylhydrazone and 1,2,4-oxadiazole leads to the identification of active antimalarial agents

November 8, 2016 - 16:56 -- NOT Open Access
Author(s): 
José Maurício dos Santos Filho, Diogo Manoel Alves de Queiroz e Silva, Milena Botelho Pereira Soares, et al.
Reference: 
Bioorganic & Medicinal Chemistry, Volume 24, Issue 22, 15 November 2016, Pages 5693–5701

Malaria, caused by several Plasmodium species, is the major life-threatening parasitic infection worldwide.

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NOT Open Access | Synthesis of chiral chloroquine and its analogues as antimalarial agents

November 19, 2014 - 15:37 -- NOT Open Access
Author(s): 
Manish Sinha, Vasanth R. Dola, Awakash Soni, Pooja Agarwal, Kumkum Srivastava, Wahajul Haq, Sunil K. Puri, Seturam B. Katti
Reference: 
Bioorganic & Medicinal Chemistry, Volume 22, Issue 21, 1 November 2014, Pages 5950–5960

In this investigation, we describe a new approach to chiral synthesis of chloroquine and its analogues.

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Novel hybrid molecules based on 15-membered azalide as potential antimalarial agents

February 23, 2012 - 09:16 -- Kabogo Ndegwa
Author(s): 
Kristina Starčević, Dijana Pešić, Ana Toplak, Goran Landek, Sulejman Alihodžić, Esperanza Herreros, Santiago Ferrer, Radan Spaventi, Mihaela Perić
Reference: 
European Journal of Medicinal Chemistry, Volume 49, March 2012, Pages 365–378

MalariaWorldMalaria remains the most prevalent tropical disease, and due to the spread of resistant parasites novel therapeutics are urgently needed.

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Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles

January 24, 2012 - 14:20 -- Kabogo Ndegwa
Author(s): 
Yong-Kang Zhang, Jacob J. Plattner, Han Cui, et al.
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 22, Issue 3, 1 February 2012, Pages 1299–1307

MalariaWorldA series of new boron-containing benzoxaborole compounds was designed and synthesized for a continuing structure–activity relationship (SAR) investigation to assess the antimalarial activity changes derived from side-chain structural variation, substituent modification on the benzene ring and removal of boron from five-membered oxaborole ring.

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Synthesis of purineN9-[2-hydroxy-3-O-(phosphonomethoxy)propyl] derivatives and their side-chain modified analogs as potential antimalarial agents

January 24, 2012 - 13:31 -- Kabogo Ndegwa
Author(s): 
Marcela Krečmerová, Martin Dračínský, Dana Hocková, Antonín Holý, Dianne T. Keough, Luke W. Guddat
Reference: 
Bioorganic & Medicinal Chemistry, Volume 20, Issue 3, 1 February 2012, Pages 1222–1230

MalariaWorld6-Oxopurine acyclic nucleoside phosphonates (ANPs) have been shown to be potent inhibitors of hypoxanthine-guanine-xanthine phosphoribosyltransferase (HGXPRT), a key enzyme of the purine salvage pathway in human malarial parasites.

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Aza vinyl sulfones: Synthesis and evaluation as antiplasmodial agents

November 29, 2011 - 09:40 -- Kabogo Ndegwa
Author(s): 
Paulo M.C. Glória, Jiri Gut, Lídia M. Gonçalves, Philip J. Rosenthal, Rui Moreira, Maria M.M. Santos
Reference: 
Bioorganic & Medicinal Chemistry, Volume 19, Issue 24, 15 December 2011, Pages 7635-7642

MalariaWorldA series of novel aza vinyl sulfones were designed, synthesized in good yields and evaluated as antiplasmodial agents.

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Cyclopropyl Carboxamides, a Chemically Novel Class of Antimalarial Agents Identified in a Phenotypic Screen

November 15, 2011 - 07:25 -- Kabogo Ndegwa
Author(s): 
Laura M. Sanz, M. Belen Jiménez-Díaz, Francisco-Javier Gamo, et al.
Reference: 
Antimicrob. Agents Chemother. December 2011 vol. 55 no. 12 5740-5745

MalariaWorldMalaria is one of the deadliest infectious diseases in the world, with the eukaryotic parasite Plasmodium falciparum causing the most severe form of the disease.

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Aryl piperazine and pyrrolidine as antimalarial agents. Synthesis and investigation of structure–activity relationships

April 14, 2011 - 12:14 -- Kabogo Ndegwa
Author(s): 
Adela Mendoza, Silvia Pérez-Silanes, Miguel Quiliano, Adriana Pabón, Silvia Galiano, Germán González, Giovanny Garavito, Mirko Zimic, Abraham Vaisberg, Ignacio Aldana, Antonio Monge, Eric Deharo
Reference: 
Experimental Parasitology, Volume 128, Issue 2, June 2011, Pages 97-103

Piperazine and pyrrolidine derivatives were synthesised and evaluated for their capacity to inhibit the growth of Plasmodium falciparum chloroquine-resistant (FCR-3) strain in culture.

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4-Anilinoquinoline triazines: A novel class of hybrid antimalarial agents

January 25, 2011 - 08:55 -- Kabogo Ndegwa
Author(s): 
Ashok, Kumar | Kumkum, Srivastava | S., Raja Kumar | M.I., Siddiqi | Sunil K., Puri | Jitendra K., Sexana | Prem M.S., Chauhan
Reference: 
European Journal of Medicinal Chemistry, Volume 46, Issue 2, February 2011, Pages 676-690

A novel class of hybrid 4-anilinoquinoline triazines have been synthesized and evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of P. falciparum as well as for their cytotoxicity toward VERO cell line.

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Synthesis and structure–activity relationships of novel benzoxaboroles as a new class of antimalarial agents

January 12, 2011 - 10:32 -- Kabogo Ndegwa
Author(s): 
Yong-Kang Zhang, Jacob J. Plattner, Yvonne R. Freund, Eric E. Easom, Yasheen Zhou, Jiri Gut, Philip J. Rosenthal, David Waterson, Francisco-Javier Gamo, Inigo Angulo-Barturen, Min Ge, Zhiya Li, Lingchao Li, Yong Jian, Han Cui, Hailong Wang, Jian Yang
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 21, Issue 2, 15 January 2011, Pages 644-651

A series of boron-containing benzoxaborole compounds was designed and synthesized for a structure–activity relationship investigation surrounding 7-(HOOCCH2CH2)-1,3-dihydro-1-hydroxy-2,1-benzoxaborole (1) with the goal of discovering a new antimalarial treatment.

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