Initial screening of the synthesized compounds revealed that compounds MK175 and MK169 inhibited LPS‐induced IL‐1β release in human aortic smooth muscle cells. ABSTRACT Proinflammatory cytokine interleukin (IL)‐1β is a key mediator of the inflammatory response in atherosclerosis.
Dimitra T. Pournara +6 more
wiley +1 more source
DESIGN, SYNTHESIS AND ANTIFUNGAL EVALUATION OF NOVEL SUBSTITUTED 1, 3, 4-OXADIAZOLES, AND 1, 3, 4-THIADIAZOLES [PDF]
Objective: The purpose of this research is to evaluate the antifungal activity of synthesized conjugates of thiophene with 1, 3, 4-oxadiazoles and 1, 3, 4-thiadiazoles using in vitro methods.Methods: The series of (IVa-e) and (Va-e) compounds were ...
Mishra, Pradeep, Upadhyay, Prabhat K
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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
DESIGN AND ANTIINFLAMATORY ACTIVITY OF SOME NOVEL OXADIAZOLE DERIVATIVES – AN OVERVIEW [PDF]
Oxadiazole derivates play vital role in biological field suchas anti-microbial, anti-viral, anti-tubercular, antiinflammatoryand anti-convulsant activity. Therapeuticsignificance of these clinically useful drugs in treatment ofinflammation encouraged the
A MISHRA, AK MISHRA, A GUPTA, V GUPTA,
core +1 more source
Investigation of the structure‐activity relationship on W482 (1) with a pyrimidine‐2,4‐diamine scaffold culminated in analog 51 with enhanced anti‐plasmodial activity. Forward genetics and phenotypic examination revealed the ABCI3 transporter protein as a putative resistance mechanism.
Mahta Mansouri +14 more
wiley +1 more source
A Hybrid Photo/Biocatalytic System for the Sustainable Synthesis of L‐Alanine From Urea and Pyruvate
We present a visible‐light driven photo‐biocatalytic system combining urease (URE), L‐alanine dehydrogenase (AlDH) and visible‐light driven nicotinamide adenine dinucleotide (NADH) regeneration system consisting of triethanolamine (TEOA), zinc meso‐tetra(4‐sulfonatophenyl)porphyrin tetrasodium salt (ZnTPPS4‐) and [Cp*Rh(bpy)(H2O)]2+.
Kyosuke Yamada, Yutaka Amao
wiley +1 more source
Synthesis and antiviral activity of 2-3,5 dinitropheny1-5-substituted phenyl 1,3,4-oxadiazoles [PDF]
3, 5 dinitro benzoic acid hydrazide was prepared by the hydrazinolysis of the corresponding ethyl ester. Condensation of this hydrazide with different aromatic acids in presence of POCl3 gave 2-3, 5 dinitropheny1-5-substituted pheny1 1, 3, 4-oxadiazoles.
Jyoti, Archana
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Synthesis, Characterization of some New 1, 3, 4-Oxadiazole derivatives based on 4- amino benzoic acid [PDF]
In this research various of 2,5-disubstituted 1,3,4-oxadiazole (Schiff base, oxo-thiazolidine , and other compounds) were synthesized from 2,5-di(4,4?- amino-1,3,4-oxadiazole ) which use quently synthesized from mixture of 4-amino benzoic acid and ...
Al-Sahib, Sanaa A. +3 more
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Piperazine Derivatives: A Privileged Scaffold in Modern Synthesis and Medicinal Chemistry
Piperazine‐based bioactive molecules represent a versatile class of compounds with broad therapeutic potential. Structural modification of the piperazine scaffold governs key structure–activity relationships, enabling antibacterial, antifungal, antitumor, neuroactive, and anti‐inflammatory activities.
Assel Ten +5 more
wiley +1 more source
The synthesis of potential analgesics derived from thebaine [PDF]
The thesis describes the synthesis of novel bridged thebaine derivatives with heterocyclic rings attached to C-7 and a study of the associated chemistry. Use has been made of the α-hydrazide (3) formed from the α-ester (2), itself prepared by Diels-Alder
Michael Burton (4178776)
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