Synthesis and structure-activity relationship of elastase inhibiting novel ethylated thiazole-triazole acetamide hybrids: Mechanistic insights through kinetics and computational contemplations

QR Code

Synthesis and structure-activity relationship of elastase inhibiting novel ethylated thiazole-triazole acetamide hybrids: Mechanistic insights through kinetics and computational contemplations

Keeping in mind the pharmacological importance of 2-aminothiazole and 1,2,4-triazole heterocyclic moieties, a series of novel ethylated bi-heterocyclic acetamide hybrids, 9a–p, was synthesized in a multi-step protocol. The structures of newly synthesized compounds were c...

Full description

Bibliographic Details
Published in:	Bioorganic Chemistry
Main Author:	Butt A.R.S.; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Hassan M.; Raza H.; Shah S.A.A.; Seo S.-Y.
Format:	Review
Language:	English
Published:	Academic Press Inc. 2019
Online Access:	https://www.scopus.com/inward/record.uri?eid=2-s2.0-85060856533&doi=10.1016%2fj.bioorg.2019.01.040&partnerID=40&md5=b1b89e8217b618d2cfdce588785cad50

Similar Items

Synthesis and structure-activity relationship of tyrosinase inhibiting novel bi-heterocyclic acetamides: Mechanistic insights through enzyme inhibition, kinetics and computational studies
by: Butt A.R.S.; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Raza H.; Hassan M.; Shah S.A.A.; Shahid M.; Seo S.-Y.
Published: (2019)

Design of potent tyrosinase inhibiting N-arylated-4-yl-benzamides bearing 2-aminothiazole-triazole bi-heterocycles: mechanistic insight through enzyme inhibition, kinetics and computational studies
by: Khan, et al.
Published: (2024)

Convergent synthesis of carbonic anhydrase inhibiting bi-heterocyclic benzamides: Structure–activity relationship and mechanistic explorations through enzyme inhibition, kinetics, and computational studies
by: Khan F.M.; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Sadiq Butt A.R.; Raza H.; Zafar A.; Ali Shah S.A.; Shahid M.; Seo S.-Y.
Published: (2021)

Design of potent tyrosinase inhibiting N-arylated-4-yl-benzamides bearing 2-aminothiazole-triazole bi-heterocycles: mechanistic insight through enzyme inhibition, kinetics and computational studies
by: Khan F.M.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Sadiq Butt A.R.; Raza H.; Hassan M.; Ali Shah S.A.; Shahid M.; Kim S.J.
Published: (2024)

Multi-step synthesis, kinetics and in silico explorations of indole-Phenyl-1,2,4-triazole Bi-heterocyclic hybrids unified with 3-substituted benzamides as elastase inhibitors
by: Shakila; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Nazir M.; Muhammad S.; Raza H.; Shah S.A.A.; Shahid M.; Chaudhry A.R.; Kim S.J.
Published: (2025)

Multi-step synthesis, kinetics and in silico explorations of indole-Phenyl-1,2,4-triazole Bi-heterocyclic hybrids unified with 3-substituted benzamides as elastase inhibitors
by: Shakila; Abbasi, et al.
Published: (2025)

Convergent synthesis, kinetics insight and allosteric computational ascriptions of thiazole-(5-aryl)oxadiazole hybrids embraced with propanamides as alkaline phosphatase inhibitors
by: Butt A.R.S.; Abbasi M.A.; Aziz-Ur-Rehman N.; Siddiqui S.Z.; Muhammad S.; Raza H.; Shah S.A.A.; Shahid M.; Alsehemi A.G.; Kim S.J.
Published: (2023)

Multi-step synthesis of indole-N-ethyltriazole hybrids amalgamated with N-arylated ethanamides: structure-activity relationship and mechanistic explorations through tyrosinase inhibition, kinetics and computational ascriptions
by: Shakila; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Nazir M.; Raza H.; Zafar A.; Shah S.A.A.; Shahid M.; Seo S.-Y.
Published: (2022)

Bi-heterocyclic benzamides as alkaline phosphatase inhibitors: Mechanistic comprehensions through kinetics and computational approaches
by: Abbasi M.A.; Nazir M.; ur-Rehman A.; Siddiqui S.Z.; Hassan M.; Raza H.; Shah S.A.A.; Shahid M.; Seo S.-Y.
Published: (2019)

Synthesis of novel N-(1,3-thiazol-2-yl)benzamide clubbed oxadiazole scaffolds: Urease inhibition, Lipinski rule and molecular docking analyses
by: Athar Abbasi M.; Raza H.; Aziz-ur-Rehman; Zahra Siddiqui S.; Adnan Ali Shah S.; Hassan M.; Seo S.-Y.
Published: (2019)

2-Aminothiazole-Oxadiazole Bearing N-Arylated Butanamides: Convergent Synthesis, Tyrosinase Inhibition, Kinetics, Structure-Activity Relationship, and Binding Conformations
by: Raza H.; Rehman Sadiq Butt A.; Athar Abbasi M.; Aziz-ur-Rehman; Zahra Siddiqui S.; Hassan M.; Adnan Ali Shah S.; Ja Kim S.
Published: (2023)

N-(5-Methyl-1,3-Thiazol-2-yl)-2-{[5-((Un)Substituted- Phenyl)1,3,4-Oxadiazol-2-yl]Sulfanyl}acetamides. Unique Biheterocycles as Promising Therapeutic Agents
by: Abbasi M.A.; Ramzan M.S.; Aziz-ur-Rehman; Siddiqui S.Z.; Shah S.A.A.; Hassan M.; Seo S.-Y.; Ashraf M.; Mirza B.; Ismail H.
Published: (2018)

Synthesis of acetamide derivatives of 1,2,4-triazole bearing azinane and their binding interactions with bovine serum albumin using spectroscopic techniques
by: Iqbal J.; Ur-Rehman A.; Abbasi M.A.; Siddiqui S.Z.; Khalid H.; Laulloo S.J.; Joondan N.; Taupass A.B.; Rasool S.; Shah S.A.A.
Published: (2018)

Design, synthesis of triazole-based scaffolds, N-(substitutedphenyl)-2-(5-(4-methoxyphenyl)-4-phenyl-4H-1,2,4-triazol-3-ylthiol)acetamides: As potential anti-cholinesterase agents for neurodegenerative diseases
by: Siddiqui S.Z.; Arfan M.; Abbasi M.A.; Aziz-ur-Rehman; Shah S.A.A.; Parveen R.; Ashraf M.; Solangi M.; Hussain S.; Khan K.M.
Published: (2023)

Innovative cholinergic scaffolds, synthesis, and characterization of substituted 1,2,4-triazole-3-ylthio-N-acetamides and their in silico studies: supplement against neurodegenerative disease
by: Arfan M.; Siddiqui S.Z.; Abbasi M.A.; Aziz-ur-Rehman; Saad S.M.; Shah S.A.A.; Ashraf M.; Hussain S.; Ali F.; Solangi M.; Khan K.M.
Published: (2023)

Synthesis, in vitro and in silico studies of novel potent urease inhibitors: N-[4-({5-[(3-Un/substituted-anilino-3-oxopropyl)sulfanyl]-1,3,4-oxadiazol-2-yl}methyl)-1,3-thiazol-2-yl]benzamides
by: Abbasi M.A.; Hassan M.; Aziz-ur-Rehman; Siddiqui S.Z.; Raza H.; Shah S.A.A.; Seo S.-Y.
Published: (2018)

Structure–activity relationship and in silico study of unique bi-heterocycles: 5-[(2-amino-1,3-thiazol-4-yl)methyl]-1,3,4-oxadiazole-2-thiol derivatives
by: Abbasi M.A.; Ramzan M.S.; Aziz-Ur-Rehman; Siddiqui S.Z.; Hassan M.; Raza H.; Shah S.A.A.; Mirza B.; Seo S.-Y.
Published: (2019)

Prospects of contemplative urban park from expert perspectives
by: Salleh M.Z.M.; Othman N.; Malek N.A.; Mohamed N.; Zainal M.H.
Published: (2021)

Synthesis of 2-{[5-(aralkyl/aryl)-1,3,4-oxadiazol-2-yl]sulfanyl}-N-(4-methyl-1,3-thiazol-2-yl)acetamides: Novel bi-heterocycles as potential therapeutic agents
by: Ramzan M.S.; Abbasi M.A.; Aziz-Ur-Rehman; Siddiqui S.Z.; Shah S.A.A.; Ashraf M.; Lodhi M.A.; Khan F.A.; Mirza B.
Published: (2018)

Synthesis of Novel Bi-Heterocycles as Valuable Anti-Diabetic Agents: 2-({5-((2-Amino-1,3-Thiazol-4-yl)methyl)-1,3,4-Oxadiazol-2-yl}sulfanyl)-N-(Substituted)acetamides
by: Muhammad Athar Abbasi; Ramzan M.S.; Aziz-ur-Rehman; Siddiqui S.Z.; Shah S.A.A.; Lodhi M.A.; Khan F.A.; Mirza B.
Published: (2020)

Synthesis, enzyme inhibitory kinetics, & computational studies of N-(substituted phenyl)-(5-(3,4-dichlorobenzyl)-4-(4-chlorophenyl)-4H-1,2,4-triazol-3-ylthio)methylbenzamides: As potent alkaline phosphatase inhibitors
by: Zeb A.; Siddiqui S.Z.; Abbasi M.A.; Aziz-ur-Rehman; Shah S.A.A.; Imran S.; Raza H.; Kim S.J.; Parveen R.; Abbas G.
Published: (2025)

Convergent synthesis, free radical scavenging, Lineweaver-Burk plot exploration, hemolysis and in silico study of novel indole-phenyltriazole hybrid bearing acetamides as potent urease inhibitors
by: Khan W.; Abbasi M.A.; Rehman A.-U.; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Raza H.; Hassan M.; Shahid M.; Seo S.Y.
Published: (2020)

Synthesis, enzyme inhibitory kinetics, & computational studies of N-(substituted phenyl)-(5-(3,4-dichlorobenzyl)-4-(4-chlorophenyl)-4H-1,2,4-triazol-3-ylthio)methylbenzamides: As potent alkaline phosphatase inhibitors
by: Zeb, et al.
Published: (2025)

Designing of promising medicinal scaffolds for Alzheimer's disease through enzyme inhibition, lead optimization, molecular docking and dynamic simulation approaches
by: Hassan M.; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Shahzadi S.; Raza H.; Hussain G.; Shah S.A.A.; Ashraf M.; Shahid M.; Seo S.-Y.; Malik A.
Published: (2019)

Synthesis, molecular docking, dynamic simulations, kinetic mechanism, cytotoxicity evaluation of N-(substituted-phenyl)-4-{(4-[(E)-3-phenyl-2-propenyl]-1-piperazinyl} butanamides as tyrosinase and melanin inhibitors: In vitro, in vivo and in silico approaches
by: Raza H.; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Hassan M.; Abbas Q.; Hong H.; Shah S.A.A.; Shahid M.; Seo S.-Y.
Published: (2020)

Synthesis of some new 2-[4-(2-furoyl)-1-piperazinyl]-N-aryl/aralkyl acetamides as potent antibacterial agents
by: Hussain G.; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Ali Shah S.A.; Ahmad I.; Shahid M.
Published: (2018)

Novel Bi-heterocycles as potent inhibitors of Urease and less cytotoxic agents: 3-({5-((2-amino-1,3-thiazol-4-yl)methyl)-1,3,4-oxadiazol-2-yl}sulfanyl)-N-(un/substituted-phenyl) propanamides
by: Abbasi M.A.; Ramzan M.S.; Aziz-Ur-Rehman; Siddiqui S.Z.; Hassan M.; Shah S.A.A.; Ashraf M.; Shahid M.; Seo S.-Y.
Published: (2020)

Exploration of synthetic multifunctional amides as new therapeutic agents for Alzheimer's disease through enzyme inhibition, chemoinformatic properties, molecular docking and dynamic simulation insights
by: Hassan M.; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Hussain G.; Shah S.A.A.; Shahid M.; Seo S.-Y.
Published: (2018)

Synthesis Of Some N-(Un/Substituted-Phenyl)-2-(4-Phenyl-1-Piperazinyl)Acetamides as Possible Antibacterial and Anticancer Agents with Mild Cytotoxicity
by: Abbasi M.A.; Nazir M.; Aziz-ur-Rehman; Siddiqui S.Z.; Shah S.A.A.; Saleem R.S.Z.; Shahid M.; Mirza B.; Ismail H.
Published: (2022)

A peptide cross-linked polyacrylamide hydrogel for the detection of human neutrophil elastase
by: Kamarun D.; Zheng X.; Milanesi L.; Hunter C.A.; Krause S.
Published: (2009)

Synthesis of promising antibacterial and antifungal agents: 2-[[(4-Chlorophenyl)sulfonyl](2,3-dihydro-1,4-benzodioxin-6-yl)amino]-N(un/substituted-phenyl)acetamides
by: Abbasi M.A.; Irshad M.; Aziz-Ur-Rehman; Siddiqui S.Z.; Nazir M.; Ali Shah S.A.; Shahid M.
Published: (2020)

Kinetics, Thermodynamics, and Mechanistic Studies of Arsenic Removal Utilizing Natural Soil as Adsorbent
by: Mohd Fairuz, et al.
Published: (2024)

Kinetics, Thermodynamics, and Mechanistic Studies of Arsenic Removal Utilizing Natural Soil as Adsorbent
by: Mohd Fairuz F.S.; Md Muslim N.Z.; Wan Abdullah W.N.; Mohd Shohaimi N.A.; Abdullah N.H.; Ab Halim A.Z.; Mohd Shukri N.; Muhamad Salleh N.F.
Published: (2024)

Synthesis of Bi-heterocyclic sulfonamides as tyrosinase inhibitors: Lineweaver-burk plot evaluation and computational ascriptions
by: Abbasi M.M.; Zia-Ur-Rehman; Aziz-Ur-Rehman; Siddiqui S.Z.; Nazir M.; Hassan M.; Raza H.; Shah S.A.A.; Seo S.-Y.
Published: (2020)

Synthesis of novel N-(2,3-dihydro-1,4-benzodioxin-6-yl)-2-{[5-(un/substituted-phenyl)-1,3,4-oxadiazol-2-yl]sulfanyl}acetamides as potent antibacterial agents
by: Abbasi M.A.; Irshad M.; Aziz-Ur-Rehman; Siddiqui S.Z.; Shah S.A.A.; Shahid M.
Published: (2022)

BSA Binding, molecular docking and in vitro biological screening of some new 1, 2, 4-triazole heterocycles bearing azinane nucleus
by: Iqbal J.; Aziz-Ur-Rehman; Abbasi M.A.; Siddiqui S.Z.; Khalid H.; Laulloo S.J.; Chohan T.A.; Rasool S.; Ali Shah S.A.
Published: (2020)

Convergent synthesis, kinetics and computational attributions of indole-N-phenyltriazole hybrids bearing N-(aryl)butanamides as alkaline phosphatase inhibitors
by: Shakila; Abbasi M.A.; Aziz-ur-Rehman; Siddiqui S.Z.; Nazir M.; Raza H.; Shah S.A.A.; Ayine-Tora D.M.; Shahid M.; Kim S.J.
Published: (2025)

Discovery of Dual Inhibitors of Acetyl and Butrylcholinesterase and Antiproliferative Activity of 1,2,4-Triazole-3-thiol: Synthesis and In Silico Molecular Study
by: Siddiqui S.Z.; Arfan M.; Abbasi M.A.; Aziz-ur-Rehman; Shah S.A.A.; Ashraf M.; Hussain S.; Saleem R.S.Z.; Rafique R.; Khan K.M.
Published: (2020)

Synthesis, β-Glucuronidase Inhibition, and Molecular Docking Studies of 1,2,4-Triazole Hydrazones
by: Jamil W.; Kumari D.; Taha M.; Khan M.N.; Baharudin M.S.; Ali M.; Kanwal M.; Lashari M.S.; Khan K.M.
Published: (2018)

Novel indole based hybrid oxadiazole scaffolds with: N -(substituted-phenyl)butanamides: Synthesis, lineweaver-burk plot evaluation and binding analysis of potent urease inhibitors
by: Nazir M.; Abbasi M.A.; Aziz-Ur-Rehman; Siddiqui S.Z.; Raza H.; Hassan M.; Ali Shah S.A.; Shahid M.; Seo S.-Y.
Published: (2018)