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

Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases

(2020) Advait Nagle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Preclinical candidate for the treatment of visceral leishmaniasis that acts through proteasome inhibition

(2019) Susan Wyllie et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2018) Fabiana Alves et al.   CLINICAL MICROBIOLOGY REVIEWS

Challenges and recent progress in drug discovery for tropical diseases

(2018) Manu De Rycker et al.   NATURE

Cyclin-dependent kinase 12 is a drug target for visceral leishmaniasis

(2018) Susan Wyllie et al.   NATURE

Identification of GSK3186899/DDD853651 as a Preclinical Development Candidate for the Treatment of Visceral Leishmaniasis

(2018) Michael G. Thomas et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2018) Pendem Nagendar et al.   ACS Medicinal Chemistry Letters

Anti-trypanosomatid drug discovery: an ongoing challenge and a continuing need

(2017) Mark C. Field et al.   NATURE REVIEWS MICROBIOLOGY

Regioselective Synthesis of 3-Aminoimidazo[1,2-a]pyrimidines with Triflic Anhydride

(2017) Eric Talbot et al.   SYNTHESIS-STUTTGART

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

(2016) Shilpi Khare et al.   NATURE

In Vitro–in Vivo Correlation of the Effect of Supersaturation on the Intestinal Absorption of BCS Class 2 Drugs

(2014) Haruki Higashino et al.   MOLECULAR PHARMACEUTICS

SnAP Reagents for the Synthesis of Piperazines and Morpholines

(2014) Michael U. Luescher et al.   ORGANIC LETTERS

Comparison of a High-Throughput High-Content Intracellular Leishmania donovani Assay with an Axenic Amastigote Assay

(2013) Manu De Rycker et al.   ANTIMICROBIAL AGENTS AND CHEMOTHERAPY

Optimization of the electrophile of chloronitrobenzamide leads active against Trypanosoma brucei

(2013) Jong Yeon Hwang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

3-(Oxazolo[4,5-b]pyridin-2-yl)anilides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei, the causative agent for human African trypanosomiasis

(2013) Lori Ferrins et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Substituted 2-Phenylimidazopyridines: A New Class of Drug Leads for Human African Trypanosomiasis

(2013) Hari Babu Tatipaka et al.   JOURNAL OF MEDICINAL CHEMISTRY

Exploring chemistry with the fragment molecular orbital method

(2012) Dmitri G. Fedorov et al.   PHYSICAL CHEMISTRY CHEMICAL PHYSICS

Identification of Compounds with Anti-Proliferative Activity against Trypanosoma brucei brucei Strain 427 by a Whole Cell Viability Based HTS Campaign

(2012) Melissa L. Sykes et al.   PLoS Neglected Tropical Diseases

Getting physical in drug discovery II: the impact of chromatographic hydrophobicity measurements and aromaticity

(2011) Robert J. Young et al.   DRUG DISCOVERY TODAY

The Use of Biorelevant Dissolution Media to Forecast the In Vivo Performance of a Drug

(2010) Sandra Klein   AAPS Journal

Getting physical in drug discovery: a contemporary perspective on solubility and hydrophobicity

(2010) Alan P. Hill et al.   DRUG DISCOVERY TODAY