Evaluation of 2-indolcarbohydrazones as potent α-glucosidase inhibitors, in silico studies and DFT based stereochemical predictions

QR Code

Evaluation of 2-indolcarbohydrazones as potent α-glucosidase inhibitors, in silico studies and DFT based stereochemical predictions

2-Indolcarbohydrazones 1-28 were synthesized and evaluated for their α-glucosidase inhibitory potential. A varying degree of inhibitory potential with IC50 values in the range of 2.3 ± 0.11-226.4 ± 6.8 μM was observed while comparing these outcomes with the standard acarbose (IC50 = 906.0±6.3μM). Th...

Full description

Bibliographic Details
Published in:	Bioorganic Chemistry
Main Author:	Taha M.; Ismail N.H.; Javaid K.; Imran S.; Anouar E.H.; Wadood A.; Atia-Tul-Wahab; Ali M.; Khan K.M.; Saad S.M.; Rahim F.; Choudhary M.I.
Format:	Article
Language:	English
Published:	Academic Press Inc. 2015
Online Access:	https://www.scopus.com/inward/record.uri?eid=2-s2.0-84942794211&doi=10.1016%2fj.bioorg.2015.09.001&partnerID=40&md5=ab9d824d62006e2a5510d5dd701506c3

Similar Items

Synthesis of novel inhibitors of α-glucosidase based on the benzothiazole skeleton containing benzohydrazide moiety and their molecular docking studies
by: Taha M.; Ismail N.H.; Lalani S.; Fatmi M.Q.; Atia-Tul-Wahab; Siddiqui S.; Khan K.M.; Imran S.; Choudhary M.I.
Published: (2015)

Novel quinoline derivatives as potent in vitro α-glucosidase inhibitors: In silico studies and SAR predictions
by: Taha M.; Ismail N.H.; Imran S.; Wadood A.; Rahim F.; Ali M.; Rehman A.U.
Published: (2015)

Synthesis and molecular docking studies of potent α-glucosidase inhibitors based on biscoumarin skeleton
by: Khan K.M.; Rahim F.; Wadood A.; Kosar N.; Taha M.; Lalani S.; Khan A.; Fakhri M.I.; Junaid M.; Rehman W.; Khan M.; Perveen S.; Sajid M.; Choudhary M.I.
Published: (2014)

New biologically dynamic hybrid pharmacophore triazinoindole-based-thiadiazole as potent α-glucosidase inhibitors: In vitro and in silico study
by: Khan A.A.; Rahim F.; Taha M.; Rehman W.; Iqbal N.; Wadood A.; Ahmad N.; Shah S.A.A.; Ghoneim M.M.; Alshehri S.; Salahuddin M.; Khan K.M.
Published: (2022)

Identification of bisindolylmethane-hydrazone hybrids as novel inhibitors of β-glucuronidase, DFT, and in silico SAR intimations
by: Taha M.; Ismail N.H.; Imran S.; Anouar E.H.; Ali M.; Jamil W.; Uddin N.; Kashif S.M.
Published: (2016)

Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies
by: Zawawi N.K.N.A.; Taha M.; Ahmat N.; Wadood A.; Ismail N.H.; Rahim F.; Azam S.S.; Abdullah N.
Published: (2016)

Novel thiosemicarbazide-oxadiazole hybrids as unprecedented inhibitors of yeast α-glucosidase and in silico binding analysis
by: Taha M.; Ismail N.H.; Imran S.; Wadood A.; Ali M.; Rahim F.; Khan A.A.; Riaz M.
Published: (2016)

New benzoxazole-based sulphonamide hybrids analogs as potent inhibitors of α-amylase and α-glucosidase: Synthesis and in vitro evaluation along with in silico study
by: Khan S.; Rahim F.; Rehman W.; Nawaz M.; Taha M.; Fazil S.; Hussain R.; Adnan Ali Shah S.; Abdellatif M.H.
Published: (2022)

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)

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)

Aryl-oxadiazole Schiff bases: Synthesis, α-glucosidase in vitro inhibitory activity and their in silico studies
by: Ullah H.; Rahim F.; Taha M.; Hussain R.; Tabassum N.; Wadood A.; Nawaz M.; Mosaddik A.; Imran S.; Wahab Z.; Miana G.A.; Kanwal; Khan K.M.
Published: (2020)

Evaluation of bisindole as potent β-glucuronidase inhibitors: Synthesis and in silico based studies
by: Khan K.M.; Rahim F.; Wadood A.; Taha M.; Khan M.; Naureen S.; Ambreen N.; Hussain S.; Perveen S.; Choudhary M.I.
Published: (2014)

Oxindole based oxadiazole hybrid analogs: Novel α-glucosidase inhibitors
by: Taha M.; Imran S.; Rahim F.; Wadood A.; Khan K.M.
Published: (2018)

Synthesis of new oxadiazole derivatives as α-glucosidase inhibitors
by: Taha M.; Ismail N.H.; Imran S.; Rokei M.Q.B.; Saad S.M.; Khan K.M.
Published: (2015)

3-Benzyl(phenethyl)-2-thioxobenzo[g]quinazolines as a new class of potent α-glucosidase inhibitors: Synthesis and molecular docking study
by: Al-Salahi R.; Ahmad R.; Anouar E.; Iwana Nor Azman N.I.; Marzouk M.; Abuelizz H.A.
Published: (2018)

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 of Indole Based Sulfonamide Derivatives as potent inhibitors of α-glucosidase and α-amylase in management of type-II diabetes
by: Ullah W.; Rahim F.; Hayat S.; Ullah H.; Taha M.; Khan S.; Khaliq A.; Bibi S.; Gohar O.; Iqbal N.; Shah S.A.A.; Khan K.M.
Published: (2024)

Synthesis, in vitro evaluation and molecular docking studies of hybrid 4-quinolinyl bearing 1,3,4-thiadiazole-2-amine as a new inhibitor of α-amylase and α-glucosidase
by: Taha M.; Khan A.A.; Rahim F.; Hayat S.; Imran S.; Iqbal N.; Uddin N.; Khan K.M.; Anouar E.H.; Farooq R.K.; Nawaz M.; Shah S.A.A.
Published: (2023)

Evaluation and docking of indole sulfonamide as a potent inhibitor of α-glucosidase enzyme in streptozotocin –induced diabetic albino wistar rats
by: Taha M.; Imran S.; Salahuddin M.; Iqbal N.; Rahim F.; Uddin N.; Shehzad A.; Khalid Farooq R.; Alomari M.; Mohammed Khan K.
Published: (2021)

Benzimidazole Bearing Thiosemicarbazone Derivatives Act as Potent α-Amylase and α-Glucosidase Inhibitors; Synthesis, Bioactivity Screening and Molecular Docking Study
by: Ullah H.; Khan S.; Rahim F.; Taha M.; Iqbal R.; Sarfraz M.; Shah S.A.A.; Sajid M.; Awad M.F.; Omran A.; Albalawi M.A.; Abdelaziz M.A.; Al Areefy A.; Jafri I.
Published: (2022)

Synthesis, α-glucosidase inhibitory, cytotoxicity and docking studies of 2-aryl-7-methylbenzimidazoles
by: Taha M.; Ismail N.H.; Imran S.; Mohamad M.H.; Wadood A.; Rahim F.; Saad S.M.; Rehman A.U.; Khan K.M.
Published: (2016)

Hydrazinyl arylthiazole based pyridine scaffolds: Synthesis, structural characterization, in vitro α-glucosidase inhibitory activity, and in silico studies
by: Ali F.; Khan K.M.; Salar U.; Taha M.; Ismail N.H.; Wadood A.; Riaz M.; Perveen S.
Published: (2017)

In silico binding analysis and SAR elucidations of newly designed benzopyrazine analogs as potent inhibitors of thymidine phosphorylase
by: Taha M.; Ismail N.H.; Imran S.; Rahim F.; Wadood A.; Al Muqarrabun L.M.R.; Khan K.M.; Ghufran M.; Ali M.
Published: (2016)

Synthesis, biological activity and molecular docking of new tricyclic series as α-glucosidase inhibitors
by: Abuelizz H.A.; Iwana N.A.N.I.; Ahmad R.; Anouar E.-H.; Marzouk M.; Al-Salahi R.
Published: (2019)

Synthesis, molecular docking studies of hybrid benzimidazole as α-glucosidase inhibitor
by: Zawawi N.K.N.A.; Taha M.; Ahmat N.; Ismail N.H.; Wadood A.; Rahim F.
Published: (2017)

New thiazole-based thiazolidinone derivatives: Synthesis, in vitro α-amylase, α-glucosidase activities and silico molecular docking study
by: Khan S.; Ullah H.; Rahim F.; Taha M.; Hussain R.; Khan M.S.; Ali H.; Khan M.U.; Shah S.A.A.; Khan K.M.
Published: (2022)

Synthesis, molecular docking and α-glucosidase inhibition of 5-aryl-2-(6′-nitrobenzofuran-2′-yl)-1,3,4-oxadiazoles
by: Taha M.; Ismail N.H.; Imran S.; Wadood A.; Rahim F.; Saad S.M.; Khan K.M.; Nasir A.
Published: (2016)

Synthesis of modified Schiff base appended 1,2,4-triazole hybrids scaffolds: Elucidating the in vitro and in silico α-amylase and α-glucosidase inhibitors potential
by: Abbasi S.A.; Rahim F.; Hussain R.; Rehman W.; Khan S.; Taha M.; Iqbal T.; Khan Y.; Ali Shah S.A.
Published: (2024)

Synthesis, in vitro α-glucosidase inhibitory potential and molecular docking study of thiadiazole analogs
by: Javid M.T.; Rahim F.; Taha M.; Rehman H.U.; Nawaz M.; wadood A.; Imran S.; Uddin I.; Mosaddik A.; Khan K.M.
Published: (2018)

Synthesis of modified Schiff base appended 1,2,4-triazole hybrids scaffolds: elucidating the in vitro and in silico α-amylase and α-glucosidase inhibitors potential
by: Abbasi, et al.
Published: (2024)

Synthesis, in vitro and Docking Studies of New Flavone Ethers as α-Glucosidase Inhibitors
by: Imran S.; Taha M.; Ismail N.H.; Kashif S.M.; Rahim F.; Jamil W.; Wahab H.; Khan K.M.
Published: (2016)

Synthesis of Flurbiprofen Based Amide Derivatives as Potential Leads for Diabetic Management: In Vitro α-glucosidase Inhibition, Molecular Docking and DFT Simulation Approach
by: Alam A.; Zainab; Elhenawy A.A.; Ur Rehman N.; Shahidul Islam M.; Dahlous K.A.; Talab F.; Shah S.A.A.; Ali M.; Ahmad M.
Published: (2024)

Syntheses of new 3-thiazolyl coumarin derivatives, in vitro α-glucosidase inhibitory activity, and molecular modeling studies
by: Salar U.; Taha M.; Khan K.M.; Ismail N.H.; Imran S.; Perveen S.; Gul S.; Wadood A.
Published: (2016)

Synthesis crystal structure of 2-methoxybenzoylhydrazones and evaluation of their α-glucosidase and urease inhibition potential
by: Taha M.; Ismail N.H.; Baharudin M.S.; Lalani S.; Mehboob S.; Khan K.M.; Yousuf S.; Siddiqui S.; Rahim F.; Choudhary M.I.
Published: (2015)

Synthesis of Novel Soritin Sulfonamide Derivatives as Potential α-Glucosidase Inhibitor and Their Molecular Docking Studies
by: Inayatsyah N.; Ridhwan M.; Aznirulhisham A.; Rasol N.; Kasim N.; Imran S.
Published: (2024)

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)

Isatin based thiosemicarbazide derivatives as potential inhibitor of α-glucosidase, synthesis and their molecular docking study
by: Rahim F.; Taha M.; Iqbal N.; Hayat S.; Qureshi F.; Uddin I.; Zaman K.; Rab A.; Wadood A.; Uddin N.; Nawaz M.; Shah S.A.A.; Khan K.M.
Published: (2020)

Synthesis, α-glucosidase inhibitory activity and in silico study of tris-indole hybrid scaffold with oxadiazole ring: As potential leads for the management of type-II diabetes mellitus
by: Taha M.; Rahim F.; Imran S.; Ismail N.H.; Ullah H.; Selvaraj M.; Javid M.T.; Salar U.; Ali M.; Khan K.M.
Published: (2017)

Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of α-glucosidases
by: Zawawi N.K.N.A.; Taha M.; Ahmat N.; Ismail N.H.; Wadood A.; Rahim F.; Rehman A.U.
Published: (2015)

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)