Literature DB >> 27956423

Synthesis and Evaluation of Chirally Defined Side Chain Variants of 7-Chloro-4-Aminoquinoline To Overcome Drug Resistance in Malaria Chemotherapy.

Vasantha Rao Dola1, Awakash Soni2, Pooja Agarwal2, Hafsa Ahmad3, Kanumuri Siva Rama Raju4, Mamunur Rashid4, Muhammad Wahajuddin4, Kumkum Srivastava2, W Haq1, A K Dwivedi3, S K Puri2, S B Katti5.   

Abstract

A novel 4-aminoquinoline derivative [(S)-7-chloro-N-(4-methyl-1-(4-methylpiperazin-1-yl)pentan-2-yl)-quinolin-4-amine triphosphate] exhibiting curative activity against chloroquine-resistant malaria parasites has been identified for preclinical development as a blood schizonticidal agent. The lead molecule selected after detailed structure-activity relationship (SAR) studies has good solid-state properties and promising activity against in vitro and in vivo experimental malaria models. The in vitro absorption, distribution, metabolism, and excretion (ADME) parameters indicate a favorable drug-like profile.
Copyright © 2017 American Society for Microbiology.

Entities:  

Keywords:  4-aminoquinoline; antimalarial agents; chloroquine resistant; quinolines

Mesh：

Substances：

Year:  2017        PMID： 27956423      PMCID： PMC5328577          DOI： 10.1128/AAC.01152-16

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  27 in total

1.  In-vitro culture of Plasmodium falciparum: utility of modified (RPNI) medium for drug-sensitivity studies using SYBR Green I assay.

Authors:  Shubhra Singh; Rajeev Kumar Srivastava; Mukesh Srivastava; S K Puri; K Srivastava
Journal:  Exp Parasitol       Date:  2010-08-18       Impact factor: 2.011

2.  Azithromycin: antimalarial profile against blood- and sporozoite-induced infections in mice and monkeys.

Authors:  S K Puri; N Singh
Journal:  Exp Parasitol       Date:  2000-01       Impact factor: 2.011

3.  Synthesis and antimalarial activity of side chain modified 4-aminoquinoline derivatives.

Authors:  V Raja Solomon; W Haq; Kumkum Srivastava; Sunil K Puri; S B Katti
Journal:  J Med Chem       Date:  2007-01-25       Impact factor: 7.446

4.  Synthesis, self-assembling properties, and atom transfer radical polymerization of an alkylated L-phenylalanine-derived monomeric organogel from silica: a new approach to prepare packing materials for high-performance liquid chromatography.

Authors:  M Mizanur Rahman; Miklós Czaun; Makoto Takafuji; Hirotaka Ihara
Journal:  Chemistry       Date:  2008       Impact factor: 5.236

5.  Design and synthesis of 3-[(7-chloro-1-oxidoquinolin-4-ylamino)alkyl]-1,3-thiazolidin-4-ones as antimalarial agents.

Authors:  V Raja Solomon; W Haq; Kumkum Srivastava; Sunil K Puri; S B Katti
Journal:  J Enzyme Inhib Med Chem       Date:  2012-09-07       Impact factor: 5.051

6.  Design, synthesis and antimalarial activity of a new class of iron chelators.

Authors:  V Raja Solomon; W Haq; Sunil K Puri; Kumkum Srivastava; S B Katti
Journal:  Med Chem       Date:  2006-03       Impact factor: 2.745

7.  Antiplasmodial activity of new 4-aminoquinoline derivatives against chloroquine resistant strain.

Authors:  Manish Sinha; Vasanth R Dola; Pooja Agarwal; Kumkum Srivastava; Wahajul Haq; Sunil K Puri; Seturam B Katti
Journal:  Bioorg Med Chem       Date:  2014-05-20       Impact factor: 3.641

8.  Synthesis and in vitro and in vivo antimalarial activity of N1-(7-chloro-4-quinolyl)-1,4-bis(3-aminopropyl)piperazine derivatives.

Authors:  Adina Ryckebusch; Rébecca Deprez-Poulain; Louis Maes; Marie-Ange Debreu-Fontaine; Elisabeth Mouray; Philippe Grellier; Christian Sergheraert
Journal:  J Med Chem       Date:  2003-02-13       Impact factor: 7.446

9.  4-aminoquinoline analogs of chloroquine with shortened side chains retain activity against chloroquine-resistant Plasmodium falciparum.

Authors:  R G Ridley; W Hofheinz; H Matile; C Jaquet; A Dorn; R Masciadri; S Jolidon; W F Richter; A Guenzi; M A Girometta; H Urwyler; W Huber; S Thaithong; W Peters
Journal:  Antimicrob Agents Chemother       Date:  1996-08       Impact factor: 5.191

10.  Parallel synthesis and antimalarial screening of a 4-aminoquinoline library.

Authors:  Peter B Madrid; Nathan T Wilson; Joseph L DeRisi; R Kiplin Guy
Journal:  J Comb Chem       Date:  2004 May-Jun
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  4 in total

1.  Correlation between in vitro and in vivo antimalarial activity of compounds using CQ-sensitive and CQ-resistant strains of Plasmodium falciparum and CQ-resistant strain of P. yoelii.

Authors:  Kumkum Srivastava; Pooja Agarwal; Awakash Soni; S K Puri
Journal:  Parasitol Res       Date:  2017-05-13       Impact factor: 2.289

2.  Synthesis, Biological Evaluation, and Molecular Modeling Studies of Chiral Chloroquine Analogues as Antimalarial Agents.

Authors:  Srinivasarao Kondaparla; Utsab Debnath; Awakash Soni; Vasantha Rao Dola; Manish Sinha; Kumkum Srivastava; Sunil K Puri; Seturam B Katti
Journal:  Antimicrob Agents Chemother       Date:  2018-11-26       Impact factor: 5.191

3.  Synthesis and Antimalarial Activity of 4-Methylaminoquinoline Compounds against Drug-Resistant Parasite.

Authors:  Vinay Shankar Tiwari; Prince Joshi; Kanchan Yadav; Anamika Sharma; Sushobhan Chowdhury; Ashan Manhas; Niti Kumar; Renu Tripathi; Wahajul Haq
Journal:  ACS Omega       Date:  2021-05-11

4.  Chloroquine analogs as antimalarial candidates with potent in vitro and in vivo activity.

Authors:  Anna C C Aguiar; Erika Murce; Wilian A Cortopassi; Andre S Pimentel; Maria M F S Almeida; Daniele C S Barros; Jéssica S Guedes; Mario R Meneghetti; Antoniana U Krettli
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2018-10-13       Impact factor: 4.077
  4 in total

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