Synthesis of

Animals Chemistry Techniques, Synthetic Enzyme Inhibitors / chemical synthesis Inhibitory Concentration 50 Mice Molecular Docking Simulation NIH 3T3 Cells Protein Conformation Structure-Activity Relationship Sulfones / chemical synthesis Urease / antagonists & inhibitors
H. pylori Urease inhibitors non-cytotoxic peptic ulcer urolithiasis β-ketosulfones.

Journal

Medicinal chemistry (Shariqah (United Arab Emirates))
ISSN: 1875-6638
Titre abrégé: Med Chem
Pays: Netherlands
ID NLM: 101240303

Informations de publication

Date de publication:
2020
Historique:
received: 19 08 2018
revised: 18 03 2019
accepted: 08 04 2019
pubmed: 17 4 2019
medline: 15 9 2020
entrez: 17 4 2019
Statut: ppublish

Résumé

Peptic ulcer and urolithiasis are largely due to infection caused by ureaseproducing bacteria. Therefore, the discovery of urease inhibitors is an important area of medicinal chemistry research. The main aim of the work was to identify novel urease inhibitors with no cytotoxicity. During the current study, a series of β-ketosulfones 1-26 was synthesized in two steps and evaluated for their in vitro urease inhibition potential. Out of twenty-six compounds, seventeen have shown good to significant urease inhibitory activity with IC50 values ranging between 49.93-351.46 µM, in comparison to standard thiourea (IC50 = 21 ± 0.11 µM). Moreover, all compounds found to be non-cytotoxic against normal 3T3 cell line. This study has identified β-ketosulfones as novel and non-cytotoxic urease inhibitors.

Sections du résumé

BACKGROUND BACKGROUND
Peptic ulcer and urolithiasis are largely due to infection caused by ureaseproducing bacteria. Therefore, the discovery of urease inhibitors is an important area of medicinal chemistry research.
OBJECTIVE OBJECTIVE
The main aim of the work was to identify novel urease inhibitors with no cytotoxicity.
METHODS METHODS
During the current study, a series of β-ketosulfones 1-26 was synthesized in two steps and evaluated for their in vitro urease inhibition potential.
RESULTS RESULTS
Out of twenty-six compounds, seventeen have shown good to significant urease inhibitory activity with IC50 values ranging between 49.93-351.46 µM, in comparison to standard thiourea (IC50 = 21 ± 0.11 µM). Moreover, all compounds found to be non-cytotoxic against normal 3T3 cell line.
CONCLUSION CONCLUSIONS
This study has identified β-ketosulfones as novel and non-cytotoxic urease inhibitors.

Identifiants

DOI: 10.2174/1573406415666190415163309 PMID: 30987574
pubmed: 30987574
pii: MC-EPUB-98082
doi: 10.2174/1573406415666190415163309
doi:

Substances chimiques

Enzyme Inhibitors 0
Sulfones 0
Urease EC 3.5.1.5

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

244-255

Informations de copyright

Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.

Auteurs

Sarosh Iqbal (S)

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
Department of Applied Chemistry, Government College University, Faisalabad-38000, Faisalabad, Pakistan.

Ajmal Khan (A)

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
Natural and Medical Sciences Research Center, University of Nizwa, P.O. Box 33, Birkat Al Mauz, Nizwa 616, Sultanate of Oman.

Rashid Nazir (R)

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.

Shumaila Kiran (S)

Department of Applied Chemistry, Government College University, Faisalabad-38000, Faisalabad, Pakistan.

Shahnaz Perveen (S)

PCSIR Laboratories Complex Karachi, Shahrah-e-Dr. Salimuzzaman Siddiqui, Karachi-75280, Pakistan.

Khalid M Khan (KM)

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, P.O. Box 31441, Dammam, Saudi Arabia.

Muhammad I Choudhary (MI)

H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi-75270, Pakistan.
Department of Biochemistry, Faculty of Science, King Abdulaziz University, Jeddah-214412, Saudi Arabia.

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Classifications MeSH

questionsmedicales.fr › Eucaryotes › Animaux › Synthesis of
questionsmedicales.fr › Technologie, industrie et agriculture › Technologie › Technologie pharmaceutique › Techniques de chimie synthétique › Synthesis of
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Synthesis of
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes toxicologiques › Concentration inhibitrice 50 › Synthesis of
questionsmedicales.fr › Eucaryotes › Animaux › Chordés › Vertébrés › Mammifères › Eutheria › Rodentia › Muridae › Murinae › Souris › Synthesis of
questionsmedicales.fr › Sciences de l'information › Méthodologies informatiques › Simulation numérique › Simulation de docking moléculaire › Synthesis of
questionsmedicales.fr › Cellules › Cellules du tissu conjonctif › Fibroblastes › Cellules 3T3 › Cellules NIH 3T3 › Synthesis of
questionsmedicales.fr › Phénomènes chimiques › Phénomènes biochimiques › Conformation moléculaire › Conformation des protéines › Synthesis of
questionsmedicales.fr › Phénomènes physiologiques › Phénomènes pharmacologiques et toxicologiques › Phénomènes pharmacologiques › Relation structure-activité › Synthesis of
questionsmedicales.fr › Composés chimiques organiques › Composés du soufre › Sulfones › Synthesis of
questionsmedicales.fr › Enzymes et coenzymes › Enzymes › Hydrolases › Amidohydrolases › Urease › Synthesis of