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Literature DB >> 12182868

Parallel synthesis and anti-malarial activity of a sulfonamide library.

A Ryckebusch¹, R Déprez-Poulain, M A Debreu-Fontaine, R Vandaele, E Mouray, P Grellier, C Sergheraert.

Abstract

Solution-phase synthesis and evaluation of a library of 31 sulfonamides as inhibitors of a chloroquine-resistant strain of Plasmodium falciparum are described. The most potent compound displayed an activity 100-fold better than chloroquine. Experiments using a fluorescent sulfonamide derivative suggest that their site of action inside the parasite is different to that of chloroquine.

Entities: Chemical Species

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Year: 2002 PMID： 12182868 DOI： 10.1016/s0960-894x(02)00475-4

Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823

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Cited

7 in total

1. Synthesis and antimalarial activity of new 4-amino-7-chloroquinolyl amides, sulfonamides, ureas and thioureas.

Authors: Kekeli Ekoue-Kovi; Kimberly Yearick; Daniel P Iwaniuk; Jayakumar K Natarajan; John Alumasa; Angel C de Dios; Paul D Roepe; Christian Wolf
Journal: Bioorg Med Chem Date: 2008-11-12 Impact factor: 3.641

2. Identification of a New Benzimidazole Derivative as an Antiviral against Hepatitis C Virus.

Authors: Thibaut Vausselin; Karin Séron; Muriel Lavie; Ahmed Atef Mesalam; Matthieu Lemasson; Sandrine Belouzard; Lucie Fénéant; Adeline Danneels; Yves Rouillé; Laurence Cocquerel; Lander Foquet; Arielle R Rosenberg; Czeslaw Wychowski; Philip Meuleman; Patricia Melnyk; Jean Dubuisson
Journal: J Virol Date: 2016-09-12 Impact factor: 5.103

3. Combining organometallic reagents, the sulfur dioxide surrogate DABSO, and amines: a one-pot preparation of sulfonamides, amenable to array synthesis.

Authors: Alex S Deeming; Claire J Russell; Michael C Willis
Journal: Angew Chem Int Ed Engl Date: 2014-11-27 Impact factor: 15.336

4. Design and synthesis of new N-(5-trifluoromethyl)-1H-1,2,4-triazol-3-yl benzenesulfonamides as possible antimalarial prototypes.

Authors: Nubia Boechat; Luiz C S Pinheiro; Osvaldo A Santos-Filho; Isabor C Silva
Journal: Molecules Date: 2011-09-20 Impact factor: 4.411

Parallel synthesis and anti-malarial activity of a sulfonamide library.

1. Synthesis and antimalarial activity of new 4-amino-7-chloroquinolyl amides, sulfonamides, ureas and thioureas.

2. Identification of a New Benzimidazole Derivative as an Antiviral against Hepatitis C Virus.

3. Combining organometallic reagents, the sulfur dioxide surrogate DABSO, and amines: a one-pot preparation of sulfonamides, amenable to array synthesis.

4. Design and synthesis of new N-(5-trifluoromethyl)-1H-1,2,4-triazol-3-yl benzenesulfonamides as possible antimalarial prototypes.

5. New peptide derived antimalaria and antimicrobial agents bearing sulphonamide moiety.

6. Synthesis and Anticancer Activity Assay of Novel Chalcone-Sulfonamide Derivatives.

7. Synthesis and antiplasmodial activity of betulinic acid and ursolic acid analogues.