Results 11 to 20 of about 8,042 (202)

Structure-Guided Optimization and Biological Validation of 1,3,4-Thiadiazole-Based SIRT2 Inhibitors Reinforcing Channel Entrance Interactions. [PDF]

Drug Dev Res
ABSTRACT SIRT2, the cytoplasmic member of the sirtuin family, is generally acknowledged to promote cancer and contribute to the progression of various pathologies, including neurodegeneration, inflammation, obesity, and bacterial infection through the deacetylation of target substrates.
Aksel AB, Ozgencil F, Bakar-Ates F, Gunindi HB, Massarotti A, Ozkan E, Kaya SG, Gozelle M, Ozkan Y, Eren G.   +9 more
europepmc   +2 more sources

An Imidazo[2,1-b][1,3,4]thiadiazole Derivative Inhibits the Virulence Factor α-Hemolysin by Blocking the Pullout of Its Stem Domain. [PDF]

ChemMedChem
A high‐throughput cellular screen based on Ca2+ influx in U937 monocytic cells identified thiadiazoles as small‐molecule inhibitors of α‐hemolysin, a key virulence factor of Staphylococcus aureus. The thiadiazole 1 prevents pore formation by a dual mechanism that prevents stem loop unfolding as well as membrane attachment.
Korotkov VS, Lukat P, Di Lucrezia R, Shekhar A, Degenhart C, Diestel R, Bilitewski U, Dinkel K, Blankenfeldt W, Brönstrup M.   +9 more
europepmc   +2 more sources

Exploring Novel Nitrofuryl‐1,3,4‐Thiadiazole‐Based Derivatives: Design, Synthesis, and Evaluation of In Vitro Leishmanicidal and Trypanocidal Activity [PDF]

Arch Pharm (Weinheim)
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 ...
Mousavi A, Slapničková M, Norouzbahari M, D'Alessandro S, Foroumadi P, Peytam F, Perego F, Doleželová E, Emamgholipour Z, Tehrani M, Sadat‐Ebrahimi S, Hosseinzadeh E, Ahadi E, Firoozpour L, Bijanzadeh H, Basilico N, Zíková A, Foroumadi A.   +17 more
europepmc   +2 more sources

Mechanism-based approaches of 1,3,4 thiadiazole scaffolds as potent enzyme inhibitors for cytotoxicity and antiviral activity

Medicine in Drug Discovery, 2023
Significant progress in understanding cancer pathogenesis, it remains one of the leading causes of death after cardiovascular diseases. Similarly viral infections have emerged from wildlife or re-emerged, generating serious threats to the global health ...
Davinder Kumar, Harsh Kumar, Virender Kumar, Aakash Deep, Aastha Sharma, Minakshi Gupta Marwaha, Rakesh Kumar Marwaha   +6 more
doaj   +1 more source

Synthesis of some Schiff's bases derivatives from aminoazo compounds

مجلة بغداد للعلوم, 2007
Reaction of,2- [( 4- amio phenyl ) diazenyl] 1,3,4- thiadiazole -5- thiol (S1) with p- chlorobenzeldehyde,3,4 – dimethoxy benzaldehyde and pyrrol-2- carbonxaldehyde gave -5- [{4-(4-chlorobenzylidene amino) phenyl} diezenyl]-1,3,4- thiadiazole-2- thiol ...
Baghdad Science Journal
doaj   +1 more source

In vitro assessment of antimicrobial, antioxidant, and cytotoxic properties of Saccharin-Tetrazolyl and-Thiadiazolyl derivatives: the simple dependence of the pH value on antimicrobial activity [PDF]

, 2019
The antimicrobial, antioxidant, and cytotoxic activities of a series of saccharin-tetrazolyl and -thiadiazolyl analogs were examined. The assessment of the antimicrobial properties of the referred-to molecules was completed through an evaluation of ...
Andrade, Joana M., Cabral, Lília, Cristiano, Maria de Lurdes, Frija, Luís M. T., Ntungwe, Epole, Pombeiro, Armando J. L., Rijo, Patrícia, Sitarek, Przemysław, Toma, Monika, Śliwiński, Tomasz   +9 more
core   +1 more source

Preparation of some azo compounds by diazotization and coupling of 2- amino -5 – thiol -1,3,4- thiadizaole

مجلة بغداد للعلوم, 2015
2- amino -5- thiol-1,3,4- thiadiazole (S1) was prepared by cyclic locking of thiosemicarbazide in the presence of anhydrous sodium carbonate and CS2. diazotization of (S1) compound gave diazonium salt (S2) that reacts with different activated aromatic ...
Baghdad Science Journal
doaj   +1 more source

Sulfur Bridged Multidentate Ligands Based on (Bi)pyridyl-(Bi)-1,3,4-Thiadiazolyl Conjugates

Molecules, 2003
The synthesis of a series of mixed (bi)pyridyl/(bi)1,3,4-thiadiazolyl ligands, derived from the condensation of 2-mercapto-5-methylthio-1,3,4-thiadiazole or 5-mercapto-5'-methylthio-2,2'-bi-1,3,4-thiadiazole with 2,6-bis(chloromethyl)pyridine or 6,6’
M. Teresa Clasadonte, Andrea Pappalardo, Antonino Mamo   +2 more
doaj   +1 more source

Synthesis, spectroscopic and crystal structure analysis of a compound with pharmocophoric substituent: 2-cyclohexyl-6-(2-oxo-2H-chromen-3-yl)- imidazo[2,1-b] [1,3,4]thiadiazole-5-carbaldehyde [PDF]

, 2007
Imidazo[2,1-b][1,3,4] thiadiazole derivatives are significant for their various pharmacological properties. This paper reports the synthesis and structure of one of them, 2-cyclohexyl-6-(2-oxo-2H-chromen-3-yl)imidazo[2,1-b][1,3,4]thiadiazole-5 ...
Girija, C.R., Hegde, V.S., Khazi, I.M., Kolavi, G.D., Noor Shahina Begum, ., Vasundhara, D.E.   +5 more
core   +1 more source

SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF SOME (2-AMINO-5-THIOL-1, 3, 4-THIADIAZOLE DERIVATIVES

مجلة بغداد للعلوم, 2007
Five derivatives of thiadiazole were prepared with aldehydes and alkyl halides, compoundA: 2-amino-5-thiol-1,3,4- thiadiazole, compound B :2-(o-hydroxybenzylidine)amino-5-thiol-1,3,4-thiadiazole, compoundC: 2(2-butan-lidine)amino-5-thiol-1,3,4 ...
Baghdad Science Journal
doaj   +1 more source