The potential inhibitory role of teucrolivins against human dipeptidyl peptidase 4 protein as a promising strategy for treatment of type 2 diabetes

Al-Zahrani, Ateeq Ahmed

doi:10.1504/ijcbdd.2019.10025248

“…To showcase the versatile and robust utility of our reaction in the rapid construction of diverse bridged and fused polycyclic scaffolds, we selected 2v , 2h , 2p and 4 g as examples and converted them into vital intermediates that are promising for the synthesis of bioactive natural products or functional materials (Scheme 2). First, the Bayer‐Villiger oxidation of 2 v afforded a lactone 6 , which is the main scaffold of neoclerodane diterpenoids [18] and has been used to treat type 2 diabetes [19] . Second, tricyclic structure 7 could be successively accessed from 2 h via IBX oxidation and an aldol reaction.…”

Section: Resultsmentioning

confidence: 99%

Asymmetric Intramolecular Hydroalkylation of Internal Olefin with Cycloalkanone to Directly Access Polycyclic Systems

Wang

¹

,

Tian

²

,

Zhao

³

et al. 2023

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An asymmetric intramolecular hydroalkylation of unactivated internal olefins with tethered cyclic ketones was realized by the cooperative catalysis of a newly designed chiral amine (SPD‐NH2) and PdII complex, providing straightforward access to either bridged or fused bicyclic systems containing three stereogenic centers with excellent enantioselectivity (up to 99 % ee) and diastereoselectivity (up to >20 : 1 dr). Notably, the bicyclic products could be conveniently transformed into a diverse range of key structures frequently found in bioactive terpenes, such as Δ6‐protoilludene, cracroson D, and vulgarisins. The steric hindrance between the Ar group of the SPD‐NH2 catalyst and the branched chain of the substrate, hydrogen‐bonding interactions between the N−H of the enamine motif and the C=O of the directing group MQ, and the counterion of the PdII complex were identified as key factors for excellent stereoinduction in this dual catalytic process by density functional theory calculations.

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Asymmetric Intramolecular Hydroalkylation of Internal Olefin with Cycloalkanone to Directly Access Polycyclic Systems

Wang

¹

,

Tian

²

,

Zhao

³

et al. 2023

View full text Add to dashboard Cite

An asymmetric intramolecular hydroalkylation of unactivated internal olefins with tethered cyclic ketones was realized by the cooperative catalysis of a newly designed chiral amine (SPD‐NH2) and PdII complex, providing straightforward access to either bridged or fused bicyclic systems containing three stereogenic centers with excellent enantioselectivity (up to 99 % ee) and diastereoselectivity (up to >20 : 1 dr). Notably, the bicyclic products could be conveniently transformed into a diverse range of key structures frequently found in bioactive terpenes, such as Δ6‐protoilludene, cracroson D, and vulgarisins. The steric hindrance between the Ar group of the SPD‐NH2 catalyst and the branched chain of the substrate, hydrogen‐bonding interactions between the N−H of the enamine motif and the C=O of the directing group MQ, and the counterion of the PdII complex were identified as key factors for excellent stereoinduction in this dual catalytic process by density functional theory calculations.

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Rutin as a Promising Inhibitor of Main Protease and Other Protein Targets of COVID-19: In Silico Study

Al-Zahrani

¹

2020

Natural Product Communications

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The process of investigating a possible cure for coronavirus disease 2019 (COVID-19) in vitro and in vivo may take a long time. For this reason, several in silico studies were performed in order to produce preliminary results that could lead to treatment. Extract of Juniperus procera Hochst is used as a traditional medicine for recovery from flu in Saudi Arabia. In the present study, more than 51 phytochemicals of J. procera were docked against the main protease of COVID-19. Rutin gave the highest interaction score among all the phytochemicals and the commercially available antiviral drugs. Lopinavir showed the second highest binding score. Rutin and lopinavir were further investigated using homology models of COVID-19. Rutin showed a better inhibition score in 9 of the 11 of homology models compared with lopinavir. Analysis of ligand-protein interaction contacts revealed that 3 residues (Glu166, Gly143, and Thr45) of the main protease formed hydrogen bonds with rutin. This simulation study suggests that rutin could be a possible effective inhibitor of several COVID-19 protein targets, including the main protease. Rutin, already available for commercial use, was evaluated for its ability as a possible drug. To our knowledge, this is the first study that suggests rutin having a possible strong inhibitory role against several protein targets of COVID-19.

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The potential inhibitory role of teucrolivins against human dipeptidyl peptidase 4 protein as a promising strategy for treatment of type 2 diabetes

Cited by 3 publications

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Asymmetric Intramolecular Hydroalkylation of Internal Olefin with Cycloalkanone to Directly Access Polycyclic Systems

Asymmetric Intramolecular Hydroalkylation of Internal Olefin with Cycloalkanone to Directly Access Polycyclic Systems

Asymmetric Intramolecular Hydroalkylation of Internal Olefin with Cycloalkanone to Directly Access Polycyclic Systems

Rutin as a Promising Inhibitor of Main Protease and Other Protein Targets of COVID-19: In Silico Study

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