β-Amino acid derivatives as mitochondrial complex III inhibitors of L. donovani: A promising chemotype targeting visceral leishmaniasis.

Amino Acids / chemistry Animals Antiprotozoal Agents / chemistry Cell Survival / drug effects Chlorocebus aethiops Cricetinae Dose-Response Relationship, Drug Electron Transport Complex III / antagonists & inhibitors Leishmania donovani / drug effects Leishmaniasis, Visceral / drug therapy Mice Mice, Inbred BALB C Mitochondria / drug effects Molecular Structure Parasitic Sensitivity Tests Structure-Activity Relationship Vero Cells
ATP Antileishmanials Electron transport chain Macrophages Visceral leishmaniasis β-Amino acids

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
15 Nov 2019
Historique:
received: 13 06 2019
revised: 02 08 2019
accepted: 19 08 2019
pubmed: 10 9 2019
medline: 31 12 2019
entrez: 10 9 2019
Statut: ppublish

Résumé

β-amino acids and their analogues are gathering increased attention not only because of their antibacterial and antifungal activity, but also for their use in designing peptidomimetics with increased oral bioavailability and resistance to metabolic degradation. In this study, a series of α-phenyl substituted chalcones, α-phenyl, β-amino substituted dihydrochalcones and β-amino acid derivatives were synthesized and evaluated for their antileishmanial efficacy against experimental visceral leishmaniasis (VL). Among all synthesized derivatives, 10c showed promising antileishmanial efficacy against both extracellular promastigote and intracellular amastigote (IC

Identifiants

DOI: 10.1016/j.ejmech.2019.111632 PMID: 31499363
pubmed: 31499363
pii: S0223-5234(19)30766-4
doi: 10.1016/j.ejmech.2019.111632
pii:
doi:

Substances chimiques

Amino Acids 0
Antiprotozoal Agents 0
Electron Transport Complex III EC 7.1.1.8

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

111632

Informations de copyright

Copyright © 2019 Elsevier Masson SAS. All rights reserved.

Auteurs

Pragya Chandrakar (P)

Parasitology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India.

Naresh Gunaganti (N)

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.

Naveen Parmar (N)

Parasitology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India.

Ashok Kumar (A)

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.

Sandeep Kumar Singh (SK)

Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India; Pharmacokinetics and Metabolism Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.

Mamunur Rashid (M)

Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India; Pharmacokinetics and Metabolism Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.

M Wahajuddin (M)

Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India; Pharmacokinetics and Metabolism Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India.

Kalyan Mitra (K)

Sophisticated Analytical Instrument Facility Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India.

Tadigopula Narender (T)

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India. Electronic address: t_narendra@cdri.res.in.

Susanta Kar (S)

Parasitology Division, CSIR-Central Drug Research Institute, BS-10/1, Sector 10, Jankipuram Extension, Sitapur Road, Lucknow 226031, India; Academy of Scientific and Innovative Research (AcSIR), Anusandhan Bhawan, New Delhi, India. Electronic address: susantakar@cdri.res.in.

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Classifications MeSH

questionsmedicales.fr › Acides aminés, peptides et protéines › Acides aminés › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Eucaryotes › Animaux › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Utilisations thérapeutiques › Anti-infectieux › Antiparasitaires › Antiprotozoaires › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Survie cellulaire › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Primates › Haplorhini › Catarrhini › Cercopithecidae › Cercopithecinae › Cercopithecus › Cercopithecus aethiops › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Arvicolinae › Cricetinae › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Relation dose-effet des médicaments › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Métalloprotéines › Protéines de liaison au fer › Protéines à fer non hème › Ferrosulfoprotéines › Complexe III de la chaîne respiratoire › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Eucaryotes › Euglénozoaires › Kinetoplastida › Trypanosomatina › Leishmania › Leishmania donovani › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Infection › Maladies vectorielles › Leishmaniose viscérale › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Lignées consanguines de souris › Souris de lignée BALB C › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Cellules › Structures cellulaires › Fractions subcellulaires › Mitochondries › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Phénomènes chimiques › Structure moléculaire › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Techniques d'investigation › Évaluation préclinique de médicament › Tests de sensibilité parasitaire › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › β-Amino acid derivatives as mitochondrial...
questionsmedicales.fr › Cellules › Cellules épithéliales › Cellules Vero › β-Amino acid derivatives as mitochondrial...