8-Aminoquinolines: future role as antiprotozoal drugs.

8-Aminoquinolines: future role as antiprotozoal drugs. Research Abstract Details 

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8-Aminoquinolines: future role as antiprotozoal drugs. Abstract Text:

Babu L Tekwani,Larry A Walker,

PURPOSE OF REVIEW: This review focuses on recent developments on evaluation of 8-aminoquinoline analogs with broader efficacy and reduced toxicity, which would provide better drugs for treatment of protozoal infections. RECENT FINDINGS: The earlier efforts towards development of 8-aminoquinoline analogs have been directed to extensive derivatization programs. This has led to discovery of tafenoquine for prophylaxis against malaria infections and sitamaquine with utility for treatment of visceral leishmaniasis. Bulaquine, a primaquine pro-drug, has shown reduced methemoglobin toxicity and better malaria-transmission-blocking activity than primaquine. Stereoselective pharmacologic and toxicologic characteristics of chiral 8-aminoquinolines provided the lead for enantiomeric separation of an 8-aminoquinoline analog NPC1161B, with greatly reduced toxicity and potent antimalarial action against blood as well as tissue stages of the parasite. NPC1161B has also shown promising use as an antileishmanial agent. Better understanding of the mechanisms of toxicity and efficacy may help in development of 8-aminoquinoline analogs with superior therapeutic actions, reduced toxicity and broader utility. SUMMARY: Extensive derivatization approaches followed by better understanding of structure-activity relationships and biotransformation mechanisms of toxicity have provided 8-aminoquinoline analogs with better pharmacologic and reduced toxicologic profiles. The novel 8-aminoquinoline analogs may have broader utility in public health as future antiprotozoals.

8-Aminoquinolines: future role as antiprotozoal drugs. Publishing Authors By Initials

BL Tekwani,LA Walker,

For similar animals: invertebrates: protozoa: sarcomastigophora: mastigophora: zoomastigophora: kinetoplastida: trypanosomatina: trypanosoma research abstracts see: animals: invertebrates: protozoa: sarcomastigophora: mastigophora: zoomastigophora: kinetoplastida: trypanosomatina: trypanosoma research

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8-Aminoquinolines: future role as antiprotozoal drugs. Journal Published:

PUBLICATION TYPE: Review

Journal: Current opinion in infectious diseases

VOLUME: 19

Page Numbers: 623-31

Journal Abbreviation: Curr. Opin. Infect. Dis.

ISSN: 0951-7375

DAY: 3

MONTH: Dec

YEAR: 2006

8-Aminoquinolines: future role as antiprotozoal drugs. Information

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LANGUAGE: eng

NlmUniqueID: 8809878

8-Aminoquinolines: future role as antiprotozoal drugs. Keywords Mesh Terms:

KEYWORDS: Trypanosoma

MESH TERMS: drug effects

Chemical & Substance for Abstract: 8-Aminoquinolines: future role as antiprotozoal drugs. Information

Substance Name: 8-aminoquinoline

Registry Number: 578-66-5

Grant and Affiliation Information for 8-Aminoquinolines: future role as antiprotozoal drugs.

AFFILIATION: National Center for Natural Products Research and Department of Pharmacology, University of Mississippi, University, Mississippi 38677, USA. btekwani@olemiss.edu

Country: United States

AGENCY: United States PHS

GRANT: U50/CCU423310-03

ACRONYM: CI

MEDLINETA: Curr Opin Infect Dis

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