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
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
Molecular Docking Studies of 2-Mercapto-5-(3-Methoxyphenyl) 1, 3, 4 Oxadiazole Thiones with Focal Adhesion Kinase [PDF]
The main objective of the present work is to perform molecular docking studies of the ligand 2- Mercapto-5-(3-Methoxy phenyl) 1,3,4 oxadiazole with protein focal adhesion kinase. A good correlation was observed in binding affinity of this complex.
Guruprasad, R. +2 more
core
Microwave Irradiation Promoted Reactions of Orthoesters with Carboxylic Acid Hydrazides. Preparation of 1,3,4-Oxadiazoles [PDF]
Rapid and highly efficient synthesis of 2- or 2,5-substituted 1,3,4-oxadiazoles by the condensation of aryl carboxylic acid hydrazides and orthoesters can be achieved under microwave irradiation using an unmodified commercial over in unsealed vessels.
Mohammad Sadegh Khajavi +2 more
doaj
Background Poly(ADP-ribose) polymerases (PARPs), a nuclear protein belongs to a new class of drugs, which mainly target tumours with DNA repair defects.
Narayan Shridhar Deshpande +4 more
doaj +1 more source
Synthesis and Quantitative Structure–Activity Relationship of Imidazotetrazine Prodrugs with Activity Independent of O6-Methylguanine-DNA-methyltransferase, DNA Mismatch Repair and p53. [PDF]
The antitumor prodrug Temozolomide is compromised by its dependence for activity on DNA mismatch repair (MMR) and the repair of the chemosensitive DNA lesion, O6-methylguanine (O6-MeG), by O6-methylguanine-DNA-methyltransferase (EC 2.1.1.63, MGMT). Tumor
Arris C. E. +42 more
core +1 more source
Decoding Urease Inhibition: A Comprehensive Review of Inhibitor Scaffolds
Representative functional groups known for urease inhibition are reviewed within diverse scaffolds using structure–activity analyses to identify features associated with high inhibitory activity. Urease is a metalloenzyme produced by a wide range of organisms and plays a critical role in nitrogen microbial metabolism by catalyzing the hydrolysis of ...
Nuno Martinho, Natália Aniceto
wiley +1 more source
Symmetric 3,5-Pyrazole and Isoxazole Heterocycles Comprising a Bent Core Unit: Synthesis and Mesomorphic Characterisation [PDF]
The synthesis and characterisation of some new liquid crystalline (LC) heteroaromatic compounds containing the five-membered pyrazole/isoxazole rings is reported. Some of the compounds exhibited enantiotropic LC properties.
Hariprasad, S., Srinivasa, H.T.
core +1 more source
Design, Synthesis and Evaluation of New Bioactive Oxadiazole Derivatives as Anticancer Agents Targeting Bcl-2 [PDF]
A series of 2-(1H-indol-3-yl)-5-substituted-1,3,4-oxadiazoles, 4a–m, were designed, synthesized and tested in vitro as potential pro-apoptotic Bcl-2 inhibitory anticancer agents based on our previously reported hit compounds.
El-Sadek, Mohamed +6 more
core +4 more sources
Benzo[b]thiophene‐1,3,4‐oxadizole and 1,2,4‐oxadiazole hybrids 9a–9l were tested against both antibacterial and anticancer, revealing interesting structure‐activity relationships. density functional theory calculations (DFTs) at the B3LYP/6–311++G (d,p).
Ravikumar Gupta Miriyala +5 more
wiley +1 more source

