WO2012033878A3 - Compounds and methods for acemif inhibition and the treatment of parasites - Google Patents

Compounds and methods for acemif inhibition and the treatment of parasites Download PDF

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Publication number
WO2012033878A3
WO2012033878A3 PCT/US2011/050767 US2011050767W WO2012033878A3 WO 2012033878 A3 WO2012033878 A3 WO 2012033878A3 US 2011050767 W US2011050767 W US 2011050767W WO 2012033878 A3 WO2012033878 A3 WO 2012033878A3
Authority
WO
WIPO (PCT)
Prior art keywords
acemif
racemif
activity
furosemide
fda
Prior art date
Application number
PCT/US2011/050767
Other languages
French (fr)
Other versions
WO2012033878A2 (en
Inventor
Elias Lolis
Yoonsang Cho
Richard Bucala
Michael Cappello
Jon J. Vermeire
Original Assignee
Yale University
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Yale University filed Critical Yale University
Publication of WO2012033878A2 publication Critical patent/WO2012033878A2/en
Publication of WO2012033878A3 publication Critical patent/WO2012033878A3/en

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
    • A61K31/122—Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/196—Carboxylic acids, e.g. valproic acid having an amino group the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

The screening of bioactive compound libraries can be an effective approach for repositioning FDA-approved drugs or discovering new pharmacophores, Hookworms are blood-feeding, intestinal nematode parasites infect up to 600 million people worldwide. Vaccination with recombinant Ancylostoma ceylanicum macrophage migration inhibitory factor (rAceMIF) provided partial protection from disease, thus establishing a "proof-of-concept" for targeting AceMIF to prevent or treat infection. A high-throughput screen (HTS) against rAceMIF identified six AceMIF-specific inhibitors. A non-steroidal anti-inflammatory drug (NSAID), sodium meclofenamate, could be tested in an animal model to assess the therapeutic efficacy in treating hookworm disease. Furosemide, an FDA-approved diuretic, exhibited submicromolar inhibition of rAceMIF tautomerase activity. Structure-activity relationships of a pharmacophore based on furosemide included one analogue that binds similarly to the active site, yet does not inhibit the Na-K-Cl symporter (NKCC1) responsible for diuretic activity. Compounds and methods for inhibiting AceMIF and treating parasitic, including hookworm infections represent additional aspects of the invention.
PCT/US2011/050767 2010-09-08 2011-09-08 Compounds and methods for acemif inhibition and the treatment of parasites WO2012033878A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US38085810P 2010-09-08 2010-09-08
US61/380,858 2010-09-08

Publications (2)

Publication Number Publication Date
WO2012033878A2 WO2012033878A2 (en) 2012-03-15
WO2012033878A3 true WO2012033878A3 (en) 2012-07-19

Family

ID=45811151

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/050767 WO2012033878A2 (en) 2010-09-08 2011-09-08 Compounds and methods for acemif inhibition and the treatment of parasites

Country Status (1)

Country Link
WO (1) WO2012033878A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11173137B2 (en) * 2018-06-26 2021-11-16 The Board Of Trustees Of The Leland Stanford Junior University Compositions and methods to modulate chloride ion channel activity
CN115737648A (en) * 2021-09-03 2023-03-07 中国疾病预防控制中心寄生虫病预防控制所(国家热带病研究中心) Application of benzhydrylpiperazine compounds in treating echinococcosis

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030219467A1 (en) * 2001-09-18 2003-11-27 The Board Of Regents Of The University Of Nebraska Method for the inhibition of methanogensis
US20060153901A1 (en) * 2005-01-07 2006-07-13 Mosjidis Jorge A Method and composition for the control of gastrointestinal parasites in animals

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030219467A1 (en) * 2001-09-18 2003-11-27 The Board Of Regents Of The University Of Nebraska Method for the inhibition of methanogensis
US20060153901A1 (en) * 2005-01-07 2006-07-13 Mosjidis Jorge A Method and composition for the control of gastrointestinal parasites in animals

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
TERATOGENESIS, CARCINOGENESIS, AND MUTAGENESIS., vol. 4, no. ISSUE, 1984, pages 329 - 340 *
THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 282, no. 32, 2007 *

Also Published As

Publication number Publication date
WO2012033878A2 (en) 2012-03-15

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