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Novel Antigiardial Agents and Methods of Use Thereof

a technology of antigiardial agents and antigiardial agents, applied in the field of new compounds, can solve the problems of poor hygienic conditions, poor water quality control, and currently available adverse effects, and achieve the effects of improving the quality of life, reducing the risk of infection, and improving the effect of anti-aging

Inactive Publication Date: 2009-07-30
UNIVERSITY OF MISSISSIPPI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although becoming one of the most commonly recognized causes of waterborne disease (drinking and recreational) in humans in the United States, Giardiasis is more widespread in the developing countries where infection is correlated with poor hygienic conditions, poor water quality control, and overcrowding.
However, due to general toxicity and occasional drug resistance to metronidazole, an ongoing search for novel, safe, and efficacious antigiardial agents is required.
However, not all women who may benefit from HRT are willing to initiate this treatment due to fear of cancer and contraindications.
Other therapeutic agents currently available are also associated with certain adverse effects.

Method used

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  • Novel Antigiardial Agents and Methods of Use Thereof
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  • Novel Antigiardial Agents and Methods of Use Thereof

Examples

Experimental program
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examples /

Examples / Preparation of Compounds of the Present Invention

[0124]This section is presented as the best mode and for exemplary purposes. Specifically, the information and examples provided herein are intended to demonstrate certain embodiments of the present invention and not to be construed as limiting the scope of the present invention.

example 1

Preparation of Compounds of the Present Invention

[0125]This example demonstrates how compounds of the present invention may be made. Starting halogen-substituted resorcinol derivatives A1-4 (in the chart, below) may be synthesized by previously reported methods, while A5 and A6 and all phenylacetic acids B1-29 were commercially available. The synthetic sequence for the isoflavone library is depicted in Scheme 1. In the first step, Friedel-Crafts acylation of resorcinol derivatives A1-6 with substituted phenyl acetic acids B1-29 was carried out in the presence of BF3.Et2O. The resulting intermediates I(A1-6,B1-29) were subjected to Vilsmeier-Haack cyclization to furnish the final products P(A1-6,B1-29). The reaction conditions were optimized first, and the library 6×29 of isoflavones was generated using a Quest 210 (Argonaut Technologies Inc., CA).

[0126]The following chart shows compounds that may be used as building blocks for embodiments of the present invention. In the chart, halo...

example 2

MS, HPLC, and Antigiardial Screening Results of Embodiments of the Present Invention

[0133]

[M + H]+[M + H]+aPuritybIC50EntryCompd.X1X2RCalcdFound(%)(μg / mL) 1P (A1, B1)FHH25725793 2P (A1, B8)FH4′-Cl29129192>10.0 3P (A1, B9)FH4′-F27527594>10.0 4P (A1, B11)FH4′-OMe28728787 5P (A1, B16)FH4′-Ph333333>99NA 6P (A1, B17)FH4′-Br335335>99>10.0 7P (A1, B18)FH4′-OEt301301>998.8 8P (A1, B19)FH3′-Me271271>99 9P (A1, B20)FH4′-Me271271>9910P (A1, B22)FH3′,4′-di-F2932938111P (A1, B27)FH3′-Cl291291>9912P (A2, B1)ClHH273273951.713P (A2, B8)ClH4′-Cl307307844.514P (A2, B9)ClH4′-F29129192>10.015P (A2, B11)ClH4′-OMe30330378>10.016P (A2, B17)ClH4′-Br351351975.717P (A2, B18)ClH4′-OEt31731781>10.018P (A2, B19)ClH3′-Me28728775>10.019P (A2, B20)ClH4′-Me28728772>10.020P (A2, B22)ClH3′,4′-di-F309309753.721P (A2, B23)ClH3′,5′-di-F3093099422P (A2, B26)ClH3′-Br3513519723P (A2, B27)ClH3′-Cl307307971.724P (A2, B28)ClH3′-F291291985.225P (A2, B29)ClH3′-OMe303303814.826P (A3, B1)BrHH317317831.627P (A3, B8)BrH4′-Cl3513519...

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Abstract

The present invention provides a method of preventing or treating one or more of the following medical conditions, or treating symptoms of one or more of the following medical conditions: amebic infections, giardiasis, estrogen deficient states, osteoporosis, cardiovascular heart disease, high cholesterol levels, hyperlipidemia, cancer by administering to a subject having, or predisposed to, one or more of the conditions, a therapeutically effective amount of a compound of the present invention and a pharmaceutically acceptable carrier.

Description

PRIORITY CLAIM[0001]This Application claims priority to U.S. Application No. 60 / 401,664, filed Aug. 7, 2002, the contents of which are incorporated herein by reference.UNITED STATES GOVERNMENT SUPPORT[0002]This work is a result of research sponsored in part by the Center for Disease Control Grant # U50 / CCU41839. The United States Government has certain rights in this invention.TECHNICAL FIELD OF THE INVENTION[0003]The present invention relates to novel compounds and a method of treating or preventing certain medical clinical conditions with the compounds of the present invention. In particular, the method of the present invention includes preventing or treating giardiasis and giardiasis-related infections, including amebic (protozoal) infections, as well as osteoporosis, cardiovascular disease, high cholesterol, hyperlipidemia.BACKGROUND OF THE INVENTION[0004]Giardia lamblia (also known as Giardia intestinalis) is a flagellated unicellular protozoan that causes acute or chronic gast...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/5377A61K31/352A61K31/497A61K31/445A61K31/40C07D311/36C07D407/12
CPCC07D311/36C07D407/12C07D311/38Y02A50/30
Inventor AVERY, MITCHELLWALKER, LARRY A.TELANG, NAKUL
Owner UNIVERSITY OF MISSISSIPPI
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