Design and Synthesis of High Affinity Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferases Directed by Ligand Efficiency Dependent Lipophilicity (LELP) [PDF]
N-Myristoyltransferase (NMT) is an essential eukaryotic enzyme and an attractive drug target in parasitic infections such as malaria. We have previously reported that 2-(3-(piperidin-4-yloxy)benzo[b]thiophen-2-yl)-5-((1,3,5-trimethyl-1H-pyrazol-4-yl ...
Anthony A. Holder +57 more
core +1 more source
Radical Retrosynthesis of Natural Products Enabled by Iron‐Based Reductive Olefin Coupling
This review highlights iron‐catalyzed reductive olefin coupling (ROC)—a strategy for C─C bond formation driven by metal‐hydride hydrogen atom transfer (MHAT)—as a key tool in natural products synthesis. This review surveys dozens of total syntheses employing ROC‐based strategies, highlighting its power to forge strained rings, quaternary centers, and ...
Griffin L. Barnes +2 more
wiley +1 more source
Dual Acting Polymeric Nano-Aggregates for Liver Cancer Therapy [PDF]
Liver cancer treatments are often hindered by poor drug physicochemical properties, hence there is a need for improvement in order to increase patient survival and outlook.
Al-Shakarchi, W +3 more
core +4 more sources
Synthesis and Biological Evaluation of Theophylline Methyl 1,3,4-Oxadiazole as Anticancer Agents [PDF]
A series of theophylline methyl 1,3,4-oxadiazole small molecules were obtained via cyclization of theophylline-7-acetohydrazide with different benzoic acids. The compounds (IVa-j) were synthesized and characterized by using conventional methods.
Gopinatha, Vindya K. +4 more
core +1 more source
In a series of substituted 1‐[5‐(5‐nitrofuran‐2‐yl)‐1,3,4‐thiadiazol‐2‐yl]piperidine‐4‐carboxamides evaluated for in vitro antileishmanial and antitrypanosomal activity, compound 18 emerged as the most promising derivative, showing submicromolar anti‐parasitic effects targeting diverse Leishmania and Trypanosoma species and acceptable selectivity ...
Alireza Mousavi +17 more
wiley +1 more source
Synthesis, Structural Analysis and Screening of Some Novel 5-Substituted Aryl/Aralkyl-1,3,4-Oxadiazol-2-Yl 4-(Morpholin-4-Ylsulfonyl)Benzyl Sulfides as Potential Antibacterial Agents [PDF]
A series of new 5-substituted aryl/aralkyl-1,3,4-oxadiazol-2-yl 4-(morpholin-4-ylsulfonyl)benzyl sulfides 6a-k were synthesized by converting multifarious aryl/aralkyl organic acids 1a-k successively into corresponding esters 2a-k, hydrazides 3a-k and 5 ...
Abbasi, Muhammad Athar +6 more
core +1 more source
The successful color control in light‐emitting electrochemical cells based on highly emissive green‐emitting BN‐doped polyaromatic hydrocarbon with thermally activated NIR emitting assemblies. Abstract This work outlines the synthesis and photo‐/electro‐luminescent behavior of a new C‐shaped BN‐doped benzenoid hydrocarbon using N‐directed borylation in
Luca M. Cavinato +6 more
wiley +1 more source
Predicting melting points of organic molecules : applications to aqueous solubility prediction using the General Solubility Equation [PDF]
In this work we make predictions of several important molecular properties of academic and industrial importance to seek answers to two questions: 1) Can we apply efficient machine learning techniques, using inexpensive descriptors, to predict melting ...
McDonagh, James +2 more
core +1 more source
Mechanical and Solvent Transport Characteristics of Nitro and n-Butylphenyl Supported Poly(1,3,4-Oxadiazole)s [PDF]
Examination of mechanical and solvent transport properties of π-conjugated polymers (PCPs), viz;poly(2-nitro-p-phenylene-1,3,4-oxadiazole) [PNPO], poly(p-phenylenevinylene-1,3,4-oxadiazole) [PPVO], poly(p-(nitrophenylene)vinylene-1,3,4-oxadiazole) [PNPVO]
Gopalakrishnanpanicker, Unnikrishnan +2 more
core +2 more sources
Novel nitro‐substituted diaryl 1,3,4‐ and 1,2,4‐oxadiazoles were synthesised via molecular hybridisation of bioactive heterocycles. Selected derivatives exhibited potent antimicrobial activity, including against Mycobacterium tuberculosis and Staphylococcus aureus, and cholinesterase inhibitory activity, with promising selectivity.
Enikő Šikorová +9 more
wiley +1 more source

