Development of bis-thiobarbiturates as successful urease inhibitors and their molecular modeling studies

QR Code

Development of bis-thiobarbiturates as successful urease inhibitors and their molecular modeling studies

Bis-thiobarbiturate derivatives 1-15 have been synthesized, characterized by 1HNMR and EI-MS and screened for urease inhibition. All compounds showed various degree of urease inhibitory activity with IC50 values ranging 7.45 ± 0.12 - 74.24 ± 0.81 μmol/L while the standard thiourea behaved normally (...

Full description

Bibliographic Details
Published in:	Chinese Chemical Letters
Main Author:	Rahim F.; Ali M.; Ullah S.; Rashid U.; Ullah H.; Taha M.; Javed M.T.; Rehman W.; Khan A.A.; Abid O.U.R.; Bilal M.
Format:	Article
Language:	English
Published:	Elsevier 2016
Online Access:	https://www.scopus.com/inward/record.uri?eid=2-s2.0-84960192729&doi=10.1016%2fj.cclet.2015.12.035&partnerID=40&md5=811cfe660bde2a5cdcd83e2b4571e983

Similar Items

Synthesis and structure-activity relationship of thiobarbituric acid derivatives as potent inhibitors of urease
by: Khan K.M.; Rahim F.; Khan A.; Shabeer M.; Hussain S.; Rehman W.; Taha M.; Khan M.; Perveen S.; Choudhary M.I.
Published: (2014)

Synthesis and antiurease & antioxidant activities of bis-Schiff bases of isophthalaldehyde
by: Rahim F.; Waseeq-Ur-Rehamn; Shehzad M.; Khan A.; Taha M.; Abid O.U.R.; Quereshi M.T.; Tauseef I.; Rehman W.
Published: (2016)

Bisindolylmethane thiosemicarbazides as potential inhibitors of urease: Synthesis and molecular modeling studies
by: Taha M.; Ullah H.; Al Muqarrabun L.M.R.; Khan M.N.; Rahim F.; Ahmat N.; Javid M.T.; Ali M.; Khan K.M.
Published: (2018)

Synthesis of bis-indolylmethanes as new potential inhibitors of β-glucuronidase and their molecular docking studies
by: Taha M.; Ullah H.; Al Muqarrabun L.M.R.; Khan M.N.; Rahim F.; Ahmat N.; Ali M.; Perveen S.
Published: (2018)

Synthesis of 2-acylated and sulfonated 4-hydroxycoumarins: In vitro urease inhibition and molecular docking studies
by: Rashid U.; Rahim F.; Taha M.; Arshad M.; Ullah H.; Mahmood T.; Ali M.
Published: (2016)

Synthesis, In Vitro Enzymatic Inhibition, and Molecular Modeling of Novel Piperazine-Based Bis-Schiff Base Derivatives as Promising Anti-urease Agents
by: Masood N.; Hussain R.; Khan S.; Rahim F.; Mumtaz S.; Taha M.; Ur Rahman Abid O.; Iqbal T.; Adnan Ali Shah S.; Omar Al Wesabi E.; Magam S.M.
Published: (2024)

Synthesis, in vitro urease inhibitory potential and molecular docking study of Benzimidazole analogues
by: Zaman K.; Rahim F.; Taha M.; Ullah H.; Wadood A.; Nawaz M.; Khan F.; Wahab Z.; Shah S.A.A.; Rehman A.U.; Kawde A.-N.; Gollapalli M.
Published: (2019)

Synthesis of 4-thiazolidinone analogs as potent in vitro anti-urease agents
by: Rahim F.; Zaman K.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Ashraf M.; Uddin R.; Uddin I.; Asghar H.; Khan A.A.; Khan K.M.
Published: (2015)

Synthesis, In Vitro Enzymatic Inhibition, and Molecular Modeling of Novel Piperazine-Based Bis-Schiff Base Derivatives as Promising Anti-urease Agents
by: Masood, et al.
Published: (2024)

Triazinoindole analogs as potent inhibitors of α-glucosidase: Synthesis, biological evaluation and molecular docking studies
by: Rahim F.; Ullah K.; Ullah H.; Wadood A.; Taha M.; Rehman A.U.; Uddin I.; Ashraf M.; Shaukat A.; Rehman W.; Hussain S.; Khan K.M.
Published: (2015)

Design, synthesis, in vitro evaluation, molecular docking and ADME properties studies of hybrid bis-coumarin with thiadiazole as a new inhibitor of Urease
by: Alomari M.; Taha M.; Imran S.; Jamil W.; Selvaraj M.; Uddin N.; Rahim F.
Published: (2019)

Synthesis, molecular docking, acetylcholinesterase and butyrylcholinesterase inhibitory potential of thiazole analogs as new inhibitors for Alzheimer disease
by: Rahim F.; Javed M.T.; Ullah H.; Wadood A.; Taha M.; Ashraf M.; Qurat-Ul-Ain; Khan M.A.; Khan F.; Mirza S.; Khan K.M.
Published: (2015)

Rational design of bis-indolylmethane-oxadiazole hybrids as inhibitors of thymidine phosphorylase
by: Taha M.; Rashid U.; Imran S.; Ali M.
Published: (2018)

Synthesis of Bis-indolylmethane sulfonohydrazides derivatives as potent α-Glucosidase inhibitors
by: Gollapalli M.; Taha M.; Ullah H.; Nawaz M.; AlMuqarrabun L.M.R.; Rahim F.; Qureshi F.; Mosaddik A.; Ahmat N.; Khan K.M.
Published: (2018)

Isatin based Schiff bases as inhibitors of α-glucosidase: Synthesis, characterization, in vitro evaluation and molecular docking studies
by: Rahim F.; Malik F.; Ullah H.; Wadood A.; Khan F.; Javid M.T.; Taha M.; Rehman W.; Ur Rehman A.; Khan K.M.
Published: (2015)

Synthesis and Molecular Docking of New Bis-Thiazolidinone-Based Chalcone Analogs as Effective Inhibitors of Acetylcholinesterase and Butyrylcholinesterase
by: Hussain R.; Rahim F.; Rehman W.; Taha M.; Khan S.; Zaman K.; Adnan Ali Shah S.; Wadood A.; Imran S.; Abdellatif M.H.
Published: (2022)

Synthesis, in vitro alpha-glucosidase inhibitory potential of benzimidazole bearing bis-Schiff bases and their molecular docking study
by: Rahim F.; Zaman K.; Taha M.; Ullah H.; Ghufran M.; Wadood A.; Rehman W.; Uddin N.; Shah S.A.A.; Sajid M.; Nawaz F.; Khan K.M.
Published: (2020)

Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
by: Rahim F.; Ullah H.; Javid M.T.; Wadood A.; Taha M.; Ashraf M.; Shaukat A.; Junaid M.; Hussain S.; Rehman W.; Mehmood R.; Sajid M.; Khan M.N.; Khan K.M.
Published: (2015)

Synthesis of potent urease inhibitors based on disulfide scaffold and their molecular docking studies
by: Taha M.; Ismail N.H.; Imran S.; Wadood A.; Rahim F.; Riaz M.
Published: (2015)

Synthesis, in vitro urease inhibitory potential and molecular docking study of benzofuran-based-thiazoldinone analogues
by: Taha M.; Rahim F.; Ullah H.; Wadood A.; Farooq R.K.; Shah S.A.A.; Nawaz M.; Zakaria Z.A.
Published: (2020)

Synthesis, in vitro thymidine phosphorylase inhibitory activity and molecular docking study of novel pyridine-derived bis-oxadiazole bearing bis-schiff base derivatives
by: Hussain R.; Rehman W.; Rahim F.; Khan S.; Alanazi A.S.; Alanazi M.M.; Rasheed L.; Khan Y.; Adnan. Ali. Shah S.; Taha M.
Published: (2023)

Synthesis, biological evaluation and molecular docking study of benzimidazole derivatives as α-glucosidase inhibitors and anti-diabetes candidates
by: Hayat S.; Ullah H.; Rahim F.; Ullah I.; Taha M.; Iqbal N.; Khan F.; Khan M.S.; Shah S.A.A.; Wadood A.; Sajid M.; Abdalla A.N.
Published: (2023)

Synthesis of new arylhydrazide bearing Schiff bases/thiazolidinone: α-Amylase, urease activities and their molecular docking studies
by: Rahim F.; Taha M.; Ullah H.; Wadood A.; Selvaraj M.; Rab A.; Sajid M.; Shah S.A.A.; Uddin N.; Gollapalli M.
Published: (2019)

Synthesis of novel triazinoindole-based thiourea hybrid: A study on α-glucosidase inhibitors and their molecular docking
by: Taha M.; Alshamrani F.J.; Rahim F.; Hayat S.; Ullah H.; Zaman K.; Imran S.; Khan K.M.; Naz F.
Published: (2019)

5-Bromo-2-aryl benzimidazole derivatives as non-cytotoxic potential dual inhibitors of α-glucosidase and urease enzymes
by: Arshad T.; Khan K.M.; Rasool N.; Salar U.; Hussain S.; Asghar H.; Ashraf M.; Wadood A.; Riaz M.; Perveen S.; Taha M.; Ismail N.H.
Published: (2017)

Synthesis of new urease enzyme inhibitors as antiulcer drug and computational study
by: Taha M.; Ismail S.; Imran S.; Almandil N.B.; Alomari M.; Rahim F.; Uddin N.; Hayat S.; Zaman K.; Ibrahim M.; Alghanem B.; Islam I.; Farooq R.K.; Boudjelal M.; Khan K.M.
Published: (2022)

Multipotent Cholinesterase Inhibitors for the Treatment of Alzheimer’s Disease: Synthesis, Biological Analysis and Molecular Docking Study of Benzimidazole-Based Thiazole Derivatives
by: Hussain R.; Ullah H.; Rahim F.; Sarfraz M.; Taha M.; Iqbal R.; Rehman W.; Khan S.; Shah S.A.A.; Hyder S.; Alhomrani M.; Alamri A.S.; Abdulaziz O.; Abdelaziz M.A.
Published: (2022)

Synthesis of diindolylmethane (DIM) bearing thiadiazole derivatives as a potent urease inhibitor
by: Taha M.; Rahim F.; Khan A.A.; Anouar E.H.; Ahmed N.; Shah S.A.A.; Ibrahim M.; Zakari Z.A.
Published: (2020)

Synthesis of novel derivatives of oxindole, their urease inhibition and molecular docking studies
by: Taha M.; Ismail N.H.; Khan A.; Shah S.A.A.; Anwar A.; Halim S.A.; Fatmi M.Q.; Imran S.; Rahim F.; Khan K.M.
Published: (2015)

Anti-cancer potential of benzophenone-bis-Schiff bases on human pancreatic cancer cell line
by: Khan K.M.; Rasheed H.; Fatima B.; Hayat M.; Rahim F.; Ullah H.; Hameed A.; Taha M.; Tahir A.; Perveen S.
Published: (2016)

Synthesis, in vitro α-glucosidase activity and in silico molecular docking study of isatin analogues
by: Ullah H.; Rahim F.; Ullah E.; Hayat S.; Zada H.; Khan F.; Wadood A.; Nawaz F.; Rehman Z.U.; Shah S.A.A.
Published: (2023)

Synthesis, β-glucuronidase inhibition and molecular docking studies of hybrid bisindole-thiosemicarbazides analogs
by: Taha M.; Ismail N.H.; Imran S.; Rahim F.; Wadood A.; Khan H.; Ullah H.; Salar U.; Khan K.M.
Published: (2016)

Synthesis, DFT Studies, Molecular Docking and Biological Activity Evaluation of Thiazole-Sulfonamide Derivatives as Potent Alzheimer’s Inhibitors
by: Khan S.; Ullah H.; Taha M.; Rahim F.; Sarfraz M.; Iqbal R.; Iqbal N.; Hussain R.; Ali Shah S.A.; Ayub K.; Albalawi M.A.; Abdelaziz M.A.; Alatawi F.S.; Khan K.M.
Published: (2023)

New triazinoindole bearing thiazole/oxazole analogues: Synthesis, α-amylase inhibitory potential and molecular docking study
by: Rahim F.; Tariq S.; Taha M.; Ullah H.; Zaman K.; Uddin I.; Wadood A.; Khan A.A.; Rehman A.U.; Uddin N.; Zafar S.; Shah S.A.A.
Published: (2019)

Synthesis, biological evaluation and molecular docking study of indazole based schiff base analogues as new anti-diabetic inhibitors
by: Taha M.; Gilani S.J.; Kazmi I.; Rahim F.; Adalat B.; Ullah H.; Nawaz F.; Wadood A.; Ali Z.; Shah S.A.A.; Khan K.M.
Published: (2024)

Synthesis of quinoline derivatives as diabetic II inhibitors and molecular docking studies
by: Taha M.; Sultan S.; Imran S.; Rahim F.; Zaman K.; Wadood A.; Ur Rehman A.; Uddin N.; Mohammed Khan K.
Published: (2019)

Synthesis, biological evaluation and molecular docking study of indazole based schiff base analogues as new anti-diabetic inhibitors
by: Taha, et al.
Published: (2024)

Exploring Novel Pyridine Carboxamide Derivatives as Urease Inhibitors: Synthesis, Molecular Docking, Kinetic Studies and ADME Profile
by: Naseer A.; Osra F.A.; Awan A.N.; Imran A.; Hameed A.; Ali Shah S.A.; Iqbal J.; Zakaria Z.A.
Published: (2022)

STRUCTURAL and ELECTRONIC PROPERTIES of NBPT INHIBITOR ATTACHED to UREASE
by: Azman M.H.D.; Sin A.L.; Zuber S.Z.H.S.; Yaakob M.H.; Ghani Z.A.
Published: (2021)

Synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory potential of hydrazide based Schiff bases
by: Rahim F.; Ullah H.; Taha M.; Wadood A.; Javed M.T.; Rehman W.; Nawaz M.; Ashraf M.; Ali M.; Sajid M.; Ali F.; Khan M.N.; Khan K.M.
Published: (2016)