Literature DB >> 23701465

Quinolin-4(1H)-imines are potent antiplasmodial drugs targeting the liver stage of malaria.

Tiago Rodrigues1, Filipa P da Cruz, Maria J Lafuente-Monasterio, Daniel Gonçalves, Ana S Ressurreição, Ana R Sitoe, Maria R Bronze, Jiri Gut, Gisbert Schneider, Maria M Mota, Philip J Rosenthal, Miguel Prudêncio, Francisco-Javier Gamo, Francisca Lopes, Rui Moreira.   

Abstract

We present a novel series of quinolin-4(1H)-imines as dual-stage antiplasmodials, several-fold more active than primaquine in vitro against Plasmodium berghei liver stage. Among those, compounds 5g and 5k presented low nanomolar IC50 values. The compounds are metabolically stable and modulate several drug targets. These results emphasize the value of quinolin-4(1H)-imines as a new chemotype and their suitable properties for further drug development.

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Year:  2013        PMID： 23701465     DOI： 10.1021/jm400246e

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  7 in total

1.  Improvement of Aqueous Solubility of Lapatinib-Derived Analogues: Identification of a Quinolinimine Lead for Human African Trypanosomiasis Drug Development.

Authors:  Kelly A Bachovchin; Amrita Sharma; Seema Bag; Dana M Klug; Katherine M Schneider; Baljinder Singh; Hitesh B Jalani; Melissa J Buskes; Naimee Mehta; Scott Tanghe; Jeremiah D Momper; Richard J Sciotti; Ana Rodriguez; Kojo Mensa-Wilmot; Michael P Pollastri; Lori Ferrins
Journal:  J Med Chem       Date:  2019-01-10       Impact factor: 7.446

2.  Antiplasmodial drugs in the gas phase: a CID and DFT study of quinolon-4(1H)-imine derivatives.

Authors:  Paulo J Amorim Madeira; Ana Raquel Fernandes Sitoe; Daniel Gonçalves; Tiago Rodrigues; Rita C Guedes; Francisca Lopes; Rui Moreira; M Rosário Bronze
Journal:  J Am Soc Mass Spectrom       Date:  2014-07-08       Impact factor: 3.109

3.  Biological Evaluation and Mechanistic Studies of Quinolin-(1H)-Imines as a New Chemotype against Leishmaniasis.

Authors:  Ana Georgina Gomes-Alves; Margarida Duarte; Tânia Cruz; Helena Castro; Francisca Lopes; Rui Moreira; Ana S Ressurreição; Ana M Tomás
Journal:  Antimicrob Agents Chemother       Date:  2021-06-17       Impact factor: 5.191

4.  Synthesis of New 4-Aminoquinolines and Evaluation of Their In Vitro Activity against Chloroquine-Sensitive and Chloroquine-Resistant Plasmodium falciparum.

Authors:  Chandima S K Rajapakse; Maryna Lisai; Christiane Deregnaucourt; Véronique Sinou; Christine Latour; Dipankar Roy; Joseph Schrével; Roberto A Sánchez-Delgado
Journal:  PLoS One       Date:  2015-10-16       Impact factor: 3.240

5.  Assessment of dual life stage antiplasmodial activity of british seaweeds.

Authors:  Jasmine Spavieri; Andrea Allmendinger; Marcel Kaiser; Maurice Ayamba Itoe; Gerald Blunden; Maria M Mota; Deniz Tasdemir
Journal:  Mar Drugs       Date:  2013-10-22       Impact factor: 5.118

6.  Effects of Ferrocenyl 4-(Imino)-1,4-Dihydro-quinolines on Xenopus laevis Prophase I - Arrested Oocytes: Survival and Hormonal-Induced M-Phase Entry.

Authors:  Guillaume Marchand; Nathalie Wambang; Sylvain Pellegrini; Caroline Molinaro; Alain Martoriati; Till Bousquet; Angel Markey; Arlette Lescuyer-Rousseau; Jean-François Bodart; Katia Cailliau; Lydie Pelinski; Matthieu Marin
Journal:  Int J Mol Sci       Date:  2020-04-26       Impact factor: 5.923

7.  Dependence on linkers' flexibility designed for benzenesulfonamides targeting discovery of novel hCA IX inhibitors as potent anticancer agents.

Authors:  Haytham O Tawfik; Amany Belal; Mohammed A S Abourehab; Andrea Angeli; Alessandro Bonardi; Claudiu T Supuran; Mervat H El-Hamamsy
Journal:  J Enzyme Inhib Med Chem       Date:  2022-12       Impact factor: 5.756
  7 in total

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