Literature DB >> 17263523

Design and synthesis of potent antimalarial agents based on clotrimazole scaffold: exploring an innovative pharmacophore.

Sandra Gemma1, Giuseppe Campiani, Stefania Butini, Gagan Kukreja, Bhupendra P Joshi, Marco Persico, Bruno Catalanotti, Ettore Novellino, Ernesto Fattorusso, Vito Nacci, Luisa Savini, Donatella Taramelli, Nicoletta Basilico, Giulia Morace, Vanessa Yardley, Caterina Fattorusso.   

Abstract

Identification of new molecular scaffolds structurally unrelated to known antimalarials may represent a valid strategy to overcome resistance of P. falciparum (Pf) to currently available drugs. We describe herein the investigation of a new polycyclic pharmacophore, related to clotrimazole, to develop innovative antimalarial agents. This study allowed us to discover compounds characterized by a high in vitro potency, particularly against Pf CQ-resistant strains selectively targeting free heme, which are easy to synthesize by low-cost synthetic strategies.

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Year:  2007        PMID： 17263523     DOI： 10.1021/jm061429p

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


  6 in total

1.  The Ca2+-ATPase (SERCA1) is inhibited by 4-aminoquinoline derivatives through interference with catalytic activation by Ca2+, whereas the ATPase E2 state remains functional.

Authors:  Gianluca Bartolommei; Francesco Tadini-Buoninsegni; Maria Rosa Moncelli; Sandra Gemma; Caterina Camodeca; Stefania Butini; Giuseppe Campiani; David Lewis; Giuseppe Inesi
Journal:  J Biol Chem       Date:  2011-09-13       Impact factor: 5.157

2.  Antiplasmodial activity of [(aryl)arylsulfanylmethyl]Pyridine.

Authors:  Sanjay Kumar; Sajal Kumar Das; Sumanta Dey; Pallab Maity; Mithu Guha; Vinay Choubey; Gautam Panda; Uday Bandyopadhyay
Journal:  Antimicrob Agents Chemother       Date:  2007-11-19       Impact factor: 5.191

3.  Effect of clotrimazole on the pump cycle of the Na,K-ATPase.

Authors:  Gianluca Bartolommei; Nadège Devaux; Francesco Tadini-Buoninsegni; Mariarosa Moncelli; Hans-Jürgen Apell
Journal:  Biophys J       Date:  2008-05-09       Impact factor: 4.033

Review 4.  Acridine-Based Antimalarials-From the Very First Synthetic Antimalarial to Recent Developments.

Authors:  Mélanie Fonte; Natália Tassi; Paula Gomes; Cátia Teixeira
Journal:  Molecules       Date:  2021-01-24       Impact factor: 4.411

Review 5.  Multipurpose Drugs Active Against Both Plasmodium spp. and Microorganisms: Potential Application for New Drug Development.

Authors:  Takuro Endo; Hitoshi Takemae; Indu Sharma; Tetsuya Furuya
Journal:  Front Cell Infect Microbiol       Date:  2021-12-24       Impact factor: 5.293

6.  Design, synthesis, crystal structure and anti-plasmodial evaluation of tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidine derivatives.

Authors:  Kavita Pal; Md Kausar Raza; Jenny Legac; Md Ataur Rahman; Shoaib Manzoor; Philip J Rosenthal; Nasimul Hoda
Journal:  RSC Med Chem       Date:  2021-05-18
  6 in total

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