Results 11 to 20 of about 1,311 (155)

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

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

Synthesis and Biological Evaluation of Some Newer 1H-Benzo[b][1,5]diazepin-2(3H)-one Derivatives as Potential Anticonvulsant Agents [PDF]

Pharmaceutical Sciences, 2022
Background: Regardless of the availability of all novel and earlier treatments, seizure control is notoriously complicated. In the hopes of discovering the latest and ultimate therapy, medicinal chemists will keep on to hunt for new antiepileptic ...
Dinesh D Rishipathak, Dipak Patil, Hemant U Chikhale   +2 more
doaj   +1 more source

2-Amino-1,3,4-thiadiazoles as prospective agents in trypanosomiasis and other parasitoses

Acta Pharmaceutica, 2020
Parasitic diseases are a serious public health problem affecting hundreds of millions of people worldwide. African trypanosomiasis, American trypanosomiasis, leishmaniasis, malaria and toxoplasmosis are the main parasitic infections caused by protozoan ...
Serban Georgeta
doaj   +1 more source

Anticancer Activity of Triazolo-Thiadiazole Derivatives and Inhibition of AKT1 and AKT2 Activation

Pharmaceutics, 2021
The fusion of 1,2,4-triazole and 1,3,4-thiadiazole rings results in a class of heterocycles compounds with an extensive range of pharmacological properties.
Dimitrios T. Trafalis, Sofia Sagredou, Panayiotis Dalezis, Maria Voura, Stella Fountoulaki, Nikolaos Nikoleousakos, Konstantinos Almpanakis, Maria V. Deligiorgi, Vasiliki Sarli   +8 more
doaj   +1 more source

1,3,4-Thiadiazole Scaffold: As Anti-Epileptic Agents [PDF]

Frontiers in Chemistry, 2022
A wide range of biological activities is exhibited by 1,3,4-thiadiazole moiety such as antidiabetic, anticancer, anti-inflammatory, anticonvulsant, antiviral, antihypertensive, and antimicrobial. To date, drugs such as butazolamide, and acetazolamide.
Tulika Anthwal, Sumitra Nain
openaire   +3 more sources

A Novel Approach to the Synthesis of 1,3,4-Thiadiazole-2-amine Derivatives

Molecules, 2021
The main purpose of the study was the development of a new method for synthesis of 1,3,4-thiadiazol-2-amine derivatives in a one-pot manner using the reaction between a thiosemicarbazide and carboxylic acid without toxic additives such as POCl3 or SOCl2.
Tatiana S. Kokovina, Svyatoslav Y. Gadomsky, Alexei A. Terentiev, Nataliya A. Sanina   +3 more
doaj   +1 more source

New 1,3,4-Thiadiazole Derivatives with Anticancer Activity

Molecules, 2022
We designed and synthesized the 1,3,4-thiadiazole derivatives differing in the structure of the substituents in C2 and C5 positions. The cytotoxic activity of the obtained compounds was then determined in biological studies using MCF-7 and MDA-MB-231 breast cancer cells and normal cell line (fibroblasts).
Sara Janowska, Dmytro Khylyuk, Anna Bielawska, Anna Szymanowska, Agnieszka Gornowicz, Krzysztof Bielawski, Jarosław Noworól, Sławomir Mandziuk, Monika Wujec   +8 more
openaire   +3 more sources

Acute toxicity of 3-(2-, 3-fluorophenyl)-6-(aryl-, hetaryl)-[1,2,4]triazole[3,4-b][1,3,4]thiadiazoles

Aktualʹnì Pitannâ Farmacevtičnoï ì Medičnoï Nauki ta Praktiki, 2017
Nowadays an attempt to create a number of new biologically active compounds by many scientific groups is being one of the topical issues in the domestic pharmaceutical industry.
O. A. Bihdan, V. V. Parchenko
doaj   +1 more source

Biological activities of imidazo[2,1-b][1,3,4]thiadiazole derivatives: A review

Journal of Saudi Chemical Society, 2016
Imidazo[2,1-b][1,3,4]thiadiazole heterocycle was discovered during the 1950s. Since then, many newer derivatives are being developed and evaluated for their biological profiles. The derivatives of imidazo[2,1-b][1,3,4]thiadiazoles are widely explored for
Bhoomendra A. Bhongade, Sirajunisa Talath, Ravikiran A. Gadad, Andanappa K. Gadad   +3 more
doaj   +1 more source