ORCID Profile
0000-0001-7359-1727
Current Organisation
University of Manchester
Does something not look right? The information on this page has been harvested from data sources that may not be up to date. We continue to work with information providers to improve coverage and quality. To report an issue, use the Feedback Form.
Publisher: Elsevier BV
Date: 09-2023
Publisher: Elsevier BV
Date: 03-2019
DOI: 10.1016/J.BIOORG.2018.12.002
Abstract: An efficient one-pot four-component strategy involving aldehydes, amines, alkynes and isothiocyanates has been developed to access a novel series of thiazolidine-2-imines (5a-x). This process operates under the action of a cooperative catalysis composed of Cu(I) and Zn(II) delivering the desired five-membered heterocyclic compounds in good to excellent yields. Notably, this transformation avoids the use of pre-formed imines or propargylamines and proceeds via an intramolecular 5-exo-dig hydrothiolation reaction of the in situ formed propargyl thiourea. Furthermore, the biological application of these motifs was demonstrated in terms of their strong acetylcholinesterase (AChE) inhibitory activity where compound 5s was identified as the lead AChE inhibitor with an IC
Publisher: Elsevier BV
Date: 2020
DOI: 10.1016/J.IJBIOMAC.2019.09.105
Abstract: Combating several pathological conditions associated with ureolytic enzyme (urease) remains a formidable challenge because of the lack of effective and safe drug therapies. In this regard, the development of potent inhibitors of urease could be considered as a promising remedy. Herein, we report a new library of structurally erse hybrid heteroaromatics featuring coumarin and thiazolotriazole motifs in one combined unit. These new chemical scaffolds accessed through the integration approach were shown to inhibit the enzyme urease from jack bean at variable efficacies. An initial structure-activity relationship analysis guided through the variation of several functional groups at the aryl ring connected to the thiazole core revealed compound 6o (IC
Publisher: Elsevier BV
Date: 2020
DOI: 10.1016/J.BIOORG.2019.103479
Abstract: The inhibition of urease enzyme is very important as it plays a key role in the treatment of several urinary and gastrointestinal tract infections. This enzyme provides a suitable environment for Helicobacter pylori at the low pH of the stomach, a causative agent of gastric and peptic ulcer that may lead to cancer. In agriculture, the high urease content causes environmental and economic problems. In this pursuit, given the well-established importance of integrated pharmacophores in medicinal chemistry and to explore new inhibitors of urease featuring two distinct heterocyclic functionalities, we herein report a facile synthesis of carbazole-triazine hybrids (3a-j). These new propeller-shaped chemical scaffolds were evaluated for their urease inhibitory potential in order to identify suitable leads. The initial structure-activity survey work guided through in vitro bioactivity results recognized 3e and 3f as new starting point hits incorporating bulky iodo (3e) and strong electron-withdrawing nitro (3f) groups at the para-position of aryl amine component. The potent compounds (3e f) exhibited the highest activity with IC
Publisher: Elsevier BV
Date: 2024
Location: United Kingdom of Great Britain and Northern Ireland
Location: United Kingdom of Great Britain and Northern Ireland
Location: United Kingdom of Great Britain and Northern Ireland
No related grants have been discovered for Imtiaz Khan.