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Literature DB >> 30655955

Triazolopyrimidines and Imidazopyridines: Structure-Activity Relationships and in Vivo Efficacy for Trypanosomiasis.

Pendem Nagendar¹, J Robert Gillespie², Zackary M Herbst², Ranae M Ranade², Nora M R Molasky², Omeed Faghih², Rachael M Turner², Michael H Gelb¹, Frederick S Buckner².

Abstract

Better therapeutics are greatly needed to treat patients infected with trypanosomatid parasites such as Trypanosoma cruzi or Trypanosoma brucei. This report describes 28 new imidazopyridines and triazolopyrimidines with potent and selective antitrypanosomal activity. Drug-like properties were demonstrated in a number of in vitro assays. In vivo efficacy was observed for 19 and 20 in acute mouse models of T. cruzi infection. Compounds 19 and 20 represent potential leads for new anti-Chagas disease drugs.

Entities: Chemical Disease Species

Year: 2018 PMID： 30655955 PMCID： PMC6331164 DOI： 10.1021/acsmedchemlett.8b00498

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

8 in total

1. Substituted 2-phenylimidazopyridines: a new class of drug leads for human African trypanosomiasis.

Authors: Hari Babu Tatipaka; J Robert Gillespie; Arnab K Chatterjee; Neil R Norcross; Matthew A Hulverson; Ranae M Ranade; Pendem Nagendar; Sharon A Creason; Joshua McQueen; Nicole A Duster; Advait Nagle; Frantisek Supek; Valentina Molteni; Tanja Wenzler; Reto Brun; Richard Glynne; Frederick S Buckner; Michael H Gelb
Journal: J Med Chem Date: 2014-01-15 Impact factor: 7.446

2. New Class of Antitrypanosomal Agents Based on Imidazopyridines.

Authors: Daniel G Silva; J Robert Gillespie; Ranae M Ranade; Zackary M Herbst; Uyen T T Nguyen; Frederick S Buckner; Carlos A Montanari; Michael H Gelb
Journal: ACS Med Chem Lett Date: 2017-06-27 Impact factor: 4.345

Review 3. Applications of Fluorine in Medicinal Chemistry.

Authors: Eric P Gillis; Kyle J Eastman; Matthew D Hill; David J Donnelly; Nicholas A Meanwell
Journal: J Med Chem Date: 2015-07-22 Impact factor: 7.446

4. Antitrypanosomal Treatment with Benznidazole Is Superior to Posaconazole Regimens in Mouse Models of Chagas Disease.

Authors: Shilpi Khare; Xianzhong Liu; Monique Stinson; Ianne Rivera; Todd Groessl; Tove Tuntland; Vince Yeh; Ben Wen; Valentina Molteni; Richard Glynne; Frantisek Supek
Journal: Antimicrob Agents Chemother Date: 2015-08-03 Impact factor: 5.191

5. Limited Ability of Posaconazole To Cure both Acute and Chronic Trypanosoma cruzi Infections Revealed by Highly Sensitive In Vivo Imaging.

Authors: Amanda Fortes Francisco; Michael D Lewis; Shiromani Jayawardhana; Martin C Taylor; Eric Chatelain; John M Kelly
Journal: Antimicrob Agents Chemother Date: 2015-05-26 Impact factor: 5.191

6. Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage.

Authors: Amanda Fortes Francisco; Shiromani Jayawardhana; Michael D Lewis; Karen L White; David M Shackleford; Gong Chen; Jessica Saunders; Maria Osuna-Cabello; Kevin D Read; Susan A Charman; Eric Chatelain; John M Kelly
Journal: Sci Rep Date: 2016-10-17 Impact factor: 4.379

7. Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness.

Authors: Shilpi Khare; Advait S Nagle; Agnes Biggart; Yin H Lai; Fang Liang; Lauren C Davis; S Whitney Barnes; Casey J N Mathison; Elmarie Myburgh; Mu-Yun Gao; J Robert Gillespie; Xianzhong Liu; Jocelyn L Tan; Monique Stinson; Ianne C Rivera; Jaime Ballard; Vince Yeh; Todd Groessl; Glenn Federe; Hazel X Y Koh; John D Venable; Badry Bursulaya; Michael Shapiro; Pranab K Mishra; Glen Spraggon; Ansgar Brock; Jeremy C Mottram; Frederick S Buckner; Srinivasa P S Rao; Ben G Wen; John R Walker; Tove Tuntland; Valentina Molteni; Richard J Glynne; Frantisek Supek
Journal: Nature Date: 2016-08-08 Impact factor: 49.962

8. Development of Trypanosoma cruzi in vitro assays to identify compounds suitable for progression in Chagas' disease drug discovery.

Authors: Lorna M MacLean; John Thomas; Michael D Lewis; Ignacio Cotillo; David W Gray; Manu De Rycker
Journal: PLoS Negl Trop Dis Date: 2018-07-12

8 in total

7 in total

1. Novel Trypanocidal Inhibitors that Block Glycosome Biogenesis by Targeting PEX3-PEX19 Interaction.

Authors: Mengqiao Li; Stefan Gaussmann; Bettina Tippler; Julia Ott; Grzegorz M Popowicz; Wolfgang Schliebs; Michael Sattler; Ralf Erdmann; Vishal C Kalel
Journal: Front Cell Dev Biol Date: 2021-12-20

2. Scaffold-Hopping Strategy on a Series of Proteasome Inhibitors Led to a Preclinical Candidate for the Treatment of Visceral Leishmaniasis.

Authors: Michael Thomas; Stephen Brand; Manu De Rycker; Fabio Zuccotto; Iva Lukac; Peter G Dodd; Eun-Jung Ko; Sujatha Manthri; Kate McGonagle; Maria Osuna-Cabello; Jennifer Riley; Caterina Pont; Frederick Simeons; Laste Stojanovski; John Thomas; Stephen Thompson; Elisabet Viayna; Jose M Fiandor; Julio Martin; Paul G Wyatt; Timothy J Miles; Kevin D Read; Maria Marco; Ian H Gilbert
Journal: J Med Chem Date: 2021-04-27 Impact factor: 7.446

3. Early Stages of Drug Discovery in an Academic Institution and Involvement of Pharma for Advancing Promising Leads.

Authors: Michael H Gelb; Frederick S Buckner
Journal: ACS Infect Dis Date: 2021-04-19 Impact factor: 5.578

4. Anti-Trypanosomal Proteasome Inhibitors Cure Hemolymphatic and Meningoencephalic Murine Infection Models of African Trypanosomiasis.

Authors: Srinivasa P S Rao; Suresh B Lakshminarayana; Jan Jiricek; Marcel Kaiser; Ryan Ritchie; Elmarie Myburgh; Frantisek Supek; Tove Tuntland; Advait Nagle; Valentina Molteni; Pascal Mäser; Jeremy C Mottram; Michael P Barrett; Thierry T Diagana
Journal: Trop Med Infect Dis Date: 2020-02-17