Results 31 to 40 of about 3,535,364 (294)

Synthesis and biological activity of fused tetracyclic Pyrrolo[2,1-c][1,4]benzodiazepines

Heliyon, 2018
Cancer remains the second major cause of death in the world. Thus, there is a pressing need to identify potential synthetic route for the development of novel anticancer agents which will serve as lead compounds to effectively combat this life ...
Joel K. Annor-Gyamfi, John M. Jarrett, Joseph O. Osazee, Dobrusia Bialonska, Crystal Whitted, Victoria E. Palau, Abbas G. Shilabin   +6 more
doaj   +1 more source

Oxazolidinones as versatile scaffolds in medicinal chemistry

, 2023
Oxazolidinone is a five-member heterocyclic ring with several biological applications in medicinal chemistry. Among the three possible isomers, 2-oxazolidinone is the most investigated in drug discovery. Linezolid was pioneered as the first approved drug
Cauê Benito Scarim, Scarim, Cauê Benito [UNESP], Daniele Castagnolo, Fernandes, Guilherme Felipe Santos, Seong-Heun Kim, Jingyue Wu, Wu, Jingyue, Kim, Seong-Heun, Castagnolo, Daniele, Guilherme Felipe Santos Fernandes   +9 more
core   +1 more source

Development of a validated RP-HPLC/DAD method for the quantitative determination of methyl jasmonate in an insect repellent semi-solid formulation

Heliyon, 2019
A simple and efficient reversed-phase high-performance liquid chromatographic (RP-HPLC) method has been developed for the first time for the estimation of a mosquito repellent, methyl jasmonate in a cream formulation, and validated as per the ...
Johirul Islam, Saurav Phukan, Pronobesh Chattopadhyay   +2 more
doaj   +1 more source

Conserved binding mode but diverse interfaces of MreC‐PBP2 interactions

FEBS Letters, EarlyView.
The crystal structure of abMreC reveals a conserved two β‐barrel architecture and provides structural insights into its role within the bacterial elongasome. The abMreC–abPBP2 complex model identifies the molecular basis of MreC‐mediated PBP2 recognition, contributing to the regulation of peptidoglycan synthesis.
Hyunseok Jang, Hyo Been Jin, Chang Min Kim, So Yeon Lee, Hyun Ho Park   +4 more
wiley   +1 more source

New spectral resolution techniques for resolving and determining the components in binary fixed-dose combinations

Heliyon, 2019
Four spectrophotometric approaches were performed to determine a binary combination of Phenazone and Benzocaine in pure powder form and in pharmaceutical formations. This investigation submits the application of four techniques contingent on the presence
Duaa J. Al Zakri, Reem H. Obaydo, Amir Alhaj Sakur   +2 more
doaj   +1 more source

Microbiome‐blood–brain barrier interactions in aging — mechanisms and therapeutic potential

FEBS Letters, EarlyView.
Aging reshapes the gut microbiome (↓SCFA‐producing commensals; ↑pro‐inflammatory outputs), shifting circulating metabolites (↓SCFAs; ↑LPS, ↑TMAO, ↑PAA) that act at the BBB to increase nonspecific transcytosis, alter transport, and promote astrocyte reactivity, heightening brain vulnerability.
Daniel Cuervo‐Zanatta, Hari Baskar Balasubramanian, Amir Pasokh, Marietta Zille   +3 more
wiley   +1 more source

Detailed chemical characterization and molecular modeling of serotonin inclusion complex with unmodified β-cyclodextrin

Heliyon, 2019
In this study, we analyzed the capability of unmodified β-cyclodextrin (β-CD) to form the stable complex with serotonin hydrochloride (SER), as an important neurotransmitter in the brain.
F. Fateminasab, A.K. Bordbar, S. Shityakov   +2 more
doaj   +1 more source

Mono- and combinational drug therapies for global viral pandemic preparedness

iScience, 2022
Summary: Broadly effective antiviral therapies must be developed to be ready for clinical trials, which should begin soon after the emergence of new life-threatening viruses.
Aleksandr Ianevski, Rouan Yao, Ronja M. Simonsen, Vegard Myhre, Erlend Ravlo, Gerda D. Kaynova, Eva Zusinaite, Judith M. White, Stephen J. Polyak, Valentyn Oksenych, Marc P. Windisch, Qiuwei Pan, Eglė Lastauskienė, Astra Vitkauskienė, Algimantas Matukevičius, Tanel Tenson, Magnar Bjørås, Denis E. Kainov   +17 more
doaj   +1 more source

Structure‐forward targeting of claudins with synthetic binders

FEBS Letters, EarlyView.
Claudins form the paracellular barriers between epithelial and endothelial tissues at tight junctions and are targets for molecular binders with the goal of modulating barrier permeability. Claudin‐binding molecules are relevant in drug delivery or in altering claudin interactions with disease‐causing proteins.
Alex J. Vecchio
wiley   +1 more source

Coumarin derivatives as acetyl- and butyrylcholinestrase inhibitors: An in vitro, molecular docking, and molecular dynamics simulations study

Heliyon, 2019
Alzheimer's disease is an irreversible and progressive brain disease that can cause problems with memory and thinking skills. It is characterized by loss of cognitive ability and severe behavioral abnormalities, and could lead to death.
Marwa N. Abu-Aisheh, Amal Al-Aboudi, Mohammad S. Mustafa, Mustafa M. El-Abadelah, Saman Yousuf Ali, Zaheer Ul-Haq, Mohammad S. Mubarak   +6 more
doaj   +1 more source