Literature DB >> 35031451

Antischistosomal tetrahydro-γ-carboline sulfonamides.

Rongguo Ren1, Xiaofang Wang1, Derek A Leas1, Cécile Häberli2, Monica Cal2, Yuxiang Dong1, Marcel Kaiser2, Jennifer Keiser2, Jonathan L Vennerstrom3.   

Abstract

We discovered tetrahydro-γ-carboline sulfonamides as a new antischistosomal chemotype. The aryl sulfonamide and tetrahydro-γ-carboline substructures were required for high antischistosomal activity. Increasing polarity improved solubility and metabolic stability but decreased antischistosomal activity. We identified two compounds with IC50 values <5 µM against ex vivo Schistosoma mansoni.
Copyright © 2022 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Antischistosomal; SAR; Sulfonamides; Tetrahydro-γ-carboline

Mesh：

Substances：

Year:  2022        PMID： 35031451      PMCID： PMC8826590          DOI： 10.1016/j.bmcl.2022.128546

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  20 in total

1.  Polar molecular surface properties predict the intestinal absorption of drugs in humans.

Authors:  K Palm; P Stenberg; K Luthman; P Artursson
Journal:  Pharm Res       Date:  1997-05       Impact factor: 4.200

2.  Life cycle maintenance and drug-sensitivity assays for early drug discovery in Schistosoma mansoni.

Authors:  Flavio C Lombardo; Valérian Pasche; Gordana Panic; Yvette Endriss; Jennifer Keiser
Journal:  Nat Protoc       Date:  2019-02       Impact factor: 13.491

Review 3.  Pharmacology and potential physiological significance of schistosome multidrug resistance transporters.

Authors:  Ravi S Kasinathan; Robert M Greenberg
Journal:  Exp Parasitol       Date:  2011-03-21       Impact factor: 2.011

4.  A high-throughput screening method for the determination of aqueous drug solubility using laser nephelometry in microtiter plates.

Authors:  C D Bevan; R S Lloyd
Journal:  Anal Chem       Date:  2000-04-15       Impact factor: 6.986

Review 5.  Schistosomiasis.

Authors:  Bruno Gryseels
Journal:  Infect Dis Clin North Am       Date:  2012-06       Impact factor: 5.982

6.  Synthesis and antiprotozoal activity of pyridyl analogues of pentamidine.

Authors:  Svetlana M Bakunova; Stanislav A Bakunov; Tanja Wenzler; Todd Barszcz; Karl A Werbovetz; Reto Brun; Richard R Tidwell
Journal:  J Med Chem       Date:  2009-08-13       Impact factor: 7.446

Review 7.  Human schistosomiasis.

Authors:  Daniel G Colley; Amaya L Bustinduy; W Evan Secor; Charles H King
Journal:  Lancet       Date:  2014-04-01       Impact factor: 79.321

8.  Human schistosomiasis resistance to praziquantel in China: should we be worried?

Authors:  Edmund Y W Seto; Betty K Wong; Ding Lu; Bo Zhong
Journal:  Am J Trop Med Hyg       Date:  2011-07       Impact factor: 2.345

Review 9.  Controlling schistosomiasis with praziquantel: How much longer without a viable alternative?

Authors:  Robert Bergquist; Jürg Utzinger; Jennifer Keiser
Journal:  Infect Dis Poverty       Date:  2017-03-28       Impact factor: 4.520

10.  Mild and efficient Winterfeldt oxidation of 1,2,3,4-tetrahydro-γ-carbolines for the synthesis of dihydropyrrolo[3,2-b]-quinolones and pyrrolo[3,2-b]quinolones.

Authors:  Rong Sheng; Jiangwei Zhu; Yongzhou Hu
Journal:  Molecules       Date:  2012-01-30       Impact factor: 4.411
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.