Evaluation of New Thiazolide/Thiadiazolide Derivatives Reveals Nitro Group-Independent Efficacy against In Vitro Development of Cryptosporidium parvum-Reference-Cited by-同舟云学术

Evaluation of New Thiazolide/Thiadiazolide Derivatives Reveals Nitro Group-Independent Efficacy against In Vitro Development of Cryptosporidium parvum

Published:2010-03 Issue:3 Volume:54 Page:1315-1318
ISSN:0066-4804
Container-title:Antimicrobial Agents and Chemotherapy
language:en
Short-container-title:Antimicrob Agents Chemother

Author:

Gargala Gilles¹,Le Goff Laetitia¹,Ballet Jean-Jacques²,Favennec Loic¹,Stachulski Andrew V.³,Rossignol Jean-François⁴

Affiliation:

1. Parasitology Department, Rouen University Hospital and UPRES-EA 4311-IFRMP 23, University of Rouen, Rouen, France

2. Immunology Department, Caen University Hospital and UPRES-EA 2128, University of Caen, Caen, France

3. Romark Center for Drug Discovery at the University of Liverpool, Liverpool, United Kingdom

4. Division of Gastroenterology and Hepatology, Department of Medicine, Stanford University School of Medicine, Palo Alto, California

Abstract

ABSTRACT Thirty-nine new thiazolide/thiadiazolide compounds were compared with the nitrothiazole nitazoxanide for activity against Cryptosporidium parvum development in HCT-8 cells. Twenty-seven agents exerted ≥90% inhibition. Agents with a lower 50% inhibitory concentration (IC 50 ) than nitazoxanide were either NO 2 or halogen 5 substituted on the thiazole moiety. Other 5 substitutions such as methyl, C 3 H 7 , C 6 H 11 , H, SO 2 CH 3 , and SCH 3 negatively impacted activity. Five-substituted deacetylated analogues exhibited higher IC 50 s than their acetylated counterparts. Halogeno-thiazolide/thiadiazolides may provide valuable nitro-free alternatives to nitazoxanide.

Publisher

American Society for Microbiology

Subject

Infectious Diseases,Pharmacology (medical),Pharmacology

Link

https://journals.asm.org/doi/pdf/10.1128/AAC.00614-09

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