Literature DB >> 29133553

Synthesis and Evaluation of Methyl 4-(7-Hydroxy-4,4,8-Trimethyl-3-Oxabicyclo[3.3.1]Nonan-2-yl)Benzoate as an Antileishmanial Agent and Its Synergistic Effect with Miltefosine.

Prachi Bhalla1, Sabera Sultana2, Adarsh Kumar Chiranjivi1, Anil K Saikia2, Vikash Kumar Dubey3.   

Abstract

In our interest in oxabicyclic compounds as potent antileishmanial agents, the present work deals with the chemical synthesis of a new oxabicyclic derivative, methyl 4-(7-hydroxy-4,4,8-trimethyl-3-oxabicyclo[3.3.1]nonan-2-yl)benzoate (PS-207). This oxabicyclic derivative showed a good antileishmanial effect on the parasite, on both the promastigote and the amastigote. The mode of parasitic death from PS-207 seemed to be apoptosis-like. Interestingly, the combination of PS-207 with a low dose of miltefosine showed a synergistic effect against the parasite.
Copyright © 2018 American Society for Microbiology.

Entities:  

Keywords:  Leishmania donovani; drug development; miltefosine

Mesh:

Substances:

Year:  2018        PMID: 29133553      PMCID: PMC5786811          DOI: 10.1128/AAC.01810-17

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


  23 in total

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Review 3.  Leishmaniasis: current status of vaccine development.

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Review 4.  Combination therapy for visceral leishmaniasis.

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5.  Dual action of antimonial drugs on thiol redox metabolism in the human pathogen Leishmania donovani.

Authors:  Susan Wyllie; Mark L Cunningham; Alan H Fairlamb
Journal:  J Biol Chem       Date:  2004-07-13       Impact factor: 5.157

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7.  Efficacy of miltefosine in the treatment of visceral leishmaniasis in India after a decade of use.

Authors:  Shyam Sundar; Anup Singh; Madhukar Rai; Vijay K Prajapati; Avinash K Singh; Bart Ostyn; Marleen Boelaert; Jean-Claude Dujardin; Jaya Chakravarty
Journal:  Clin Infect Dis       Date:  2012-05-09       Impact factor: 9.079

8.  Combinations of ascaridole, carvacrol, and caryophyllene oxide against Leishmania.

Authors:  Jacinta Pastor; Marley García; Silvia Steinbauer; William N Setzer; Ramón Scull; Lars Gille; Lianet Monzote
Journal:  Acta Trop       Date:  2015-02-17       Impact factor: 3.112

9.  Leishmaniasis worldwide and global estimates of its incidence.

Authors:  Jorge Alvar; Iván D Vélez; Caryn Bern; Mercé Herrero; Philippe Desjeux; Jorge Cano; Jean Jannin; Margriet den Boer
Journal:  PLoS One       Date:  2012-05-31       Impact factor: 3.240

10.  WR279,396, a third generation aminoglycoside ointment for the treatment of Leishmania major cutaneous leishmaniasis: a phase 2, randomized, double blind, placebo controlled study.

Authors:  Afif Ben Salah; Pierre A Buffet; Gloria Morizot; Nathalie Ben Massoud; Amor Zâatour; Nissaf Ben Alaya; Nabil Bel Haj Hamida; Zaher El Ahmadi; Matthew T Downs; Philip L Smith; Koussay Dellagi; Max Grögl
Journal:  PLoS Negl Trop Dis       Date:  2009-05-05
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