Literature DB >> 26571076

Novel Amino-pyrazole Ureas with Potent In Vitro and In Vivo Antileishmanial Activity.

Charles E Mowbray1, Stéphanie Braillard1, William Speed1, Paul A Glossop2, Gavin A Whitlock2, Karl R Gibson2, James E J Mills2, Alan D Brown3, J Mark F Gardner4, Yafeng Cao5, Wen Hua5, Garreth L Morgans6, Pim-Bart Feijens7, An Matheeussen7, Louis J Maes7.   

Abstract

Visceral leishmaniasis is a severe parasitic disease that is one of the most neglected tropical diseases. Treatment options are limited, and there is an urgent need for new therapeutic agents. Following an HTS campaign and hit optimization, a novel series of amino-pyrazole ureas has been identified with potent in vitro antileishmanial activity. Furthermore, compound 26 shows high levels of in vivo efficacy (>90%) against Leishmania infantum, thus demonstrating proof of concept for this series.

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Year:  2015        PMID: 26571076     DOI: 10.1021/acs.jmedchem.5b01456

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


  13 in total

Review 1.  Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

Authors:  Khalid Karrouchi; Smaail Radi; Youssef Ramli; Jamal Taoufik; Yahia N Mabkhot; Faiz A Al-Aizari; M'hammed Ansar
Journal:  Molecules       Date:  2018-01-12       Impact factor: 4.411

2.  Identification of a Hit Series of Antileishmanial Compounds through the Use of Mixture-Based Libraries.

Authors:  Marc A Giulianotti; Brian A Vesely; Ala Azhari; Ashley Souza; Travis LaVoi; Richard A Houghten; Dennis E Kyle; James W Leahy
Journal:  ACS Med Chem Lett       Date:  2017-07-10       Impact factor: 4.345

Review 3.  Recent Development of Visceral Leishmaniasis Treatments: Successes, Pitfalls, and Perspectives.

Authors:  Fabiana Alves; Graeme Bilbe; Séverine Blesson; Vishal Goyal; Séverine Monnerat; Charles Mowbray; Gina Muthoni Ouattara; Bernard Pécoul; Suman Rijal; Joelle Rode; Alexandra Solomos; Nathalie Strub-Wourgaft; Monique Wasunna; Susan Wells; Eduard E Zijlstra; Byron Arana; Jorge Alvar
Journal:  Clin Microbiol Rev       Date:  2018-08-29       Impact factor: 26.132

4.  Synthesis and Leishmanicidal Activity of Novel Urea, Thiourea, and Selenourea Derivatives of Diselenides.

Authors:  Marta Díaz; Héctor de Lucio; Esther Moreno; Socorro Espuelas; Carlos Aydillo; Antonio Jiménez-Ruiz; Miguel Ángel Toro; Killian Jesús Gutiérrez; Victor Martínez-Merino; Alfonso Cornejo; Juan Antonio Palop; Carmen Sanmartín; Daniel Plano
Journal:  Antimicrob Agents Chemother       Date:  2019-04-25       Impact factor: 5.191

5.  Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.

Authors:  Andrew M Thompson; Patrick D O'Connor; Andrew J Marshall; Adrian Blaser; Vanessa Yardley; Louis Maes; Suman Gupta; Delphine Launay; Stephanie Braillard; Eric Chatelain; Baojie Wan; Scott G Franzblau; Zhenkun Ma; Christopher B Cooper; William A Denny
Journal:  J Med Chem       Date:  2018-03-06       Impact factor: 7.446

6.  In Vitro and in Vivo Activity of mTOR Kinase and PI3K Inhibitors Against Leishmania donovani and Trypanosoma brucei.

Authors:  Trong-Nhat Phan; Kyung-Hwa Baek; Nakyung Lee; Soo Young Byun; David Shum; Joo Hwan No
Journal:  Molecules       Date:  2020-04-23       Impact factor: 4.411

Review 7.  Of Drugs and Trypanosomatids: New Tools and Knowledge to Reduce Bottlenecks in Drug Discovery.

Authors:  Arijit Bhattacharya; Audrey Corbeil; Rubens L do Monte-Neto; Christopher Fernandez-Prada
Journal:  Genes (Basel)       Date:  2020-06-29       Impact factor: 4.096

8.  In vitro and in vivo pharmacodynamics of three novel antileishmanial lead series.

Authors:  M Van den Kerkhof; D Mabille; E Chatelain; C E Mowbray; S Braillard; S Hendrickx; L Maes; G Caljon
Journal:  Int J Parasitol Drugs Drug Resist       Date:  2018-01-31       Impact factor: 4.077

Review 9.  Pharmacokinetics and pharmacodynamics in the treatment of cutaneous leishmaniasis - challenges and opportunities.

Authors:  Katrien Van Bocxlaer; Simon L Croft
Journal:  RSC Med Chem       Date:  2021-01-07

10.  Discovery of ( ±)-3-(1H-pyrazol-1-yl)-6,7-dihydro-5H-[1,2,4]triazolo[3,4-b][1,3,4] thiadiazine derivatives with promising in vitro anticoronavirus and antitumoral activity.

Authors:  Parameshwara Chary Jilloju; Leentje Persoons; Sathish Kumar Kurapati; Dominique Schols; Steven De Jonghe; Dirk Daelemans; Rajeswar Rao Vedula
Journal:  Mol Divers       Date:  2021-06-24       Impact factor: 2.943

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