Results 1 to 10 of about 1,316 (129)

Comparative Study of the Synthetic Approaches and Biological Activities of the Bioisosteres of 1,3,4-Oxadiazoles and 1,3,4-Thiadiazoles over the Past Decade [PDF]

Molecules, 2022
The bioisosteres of 1,3,4-oxadiazoles and 1,3,4-thiadiazoles are well-known pharmacophores for many medicinally important drugs. Throughout the past 10 years, 1,3,4-oxa-/thiadiazole nuclei have been very attractive to researchers for drug design ...
Rana M. El-Masry, Hanan H. Kadry, Azza T. Taher, Sahar M. Abou-Seri   +3 more
doaj   +2 more sources

Chemoselective synthesis of 1,3,4-thiadiazoles from acyl hydrazines and nitroalkanes using elemental sulfur [PDF]

Nature Communications
Substituted 1,3,4-thiadiazoles find extensive use in pharmaceutical, agricultural, and materials chemistry. The incorporation of adaptable heterocyclic pharmacophores results in tunable hybrid molecules with diverse medicinal properties.
Xiaonan Wang, Xiuwen Yu, Ruixi Qian, Silong Xu, Martin J. Lear, Wangxiao He, Jing Li   +6 more
doaj   +2 more sources

Design, synthesis and biological evaluation of benzoxazolinone-containing 1,3,4-thiadiazoles as TNF-α inhibitors [PDF]

Heliyon, 2019
A library of nineteen benzoxazolinone-based 1,3,4-thiadiazoles has been synthesized and screened for their anti-inflammatory activity. The compound 1f exhibited a potent anti-inflammatory activity with an inhibition of 65.83% and 32.50% after 3 h and 5 h
Saqlain Haider, Mohammad Sarwar Alam, Hinna Hamid, Abhijeet Dhulap, Deepak Kumar   +4 more
doaj   +2 more sources

Synthesis and Diuretic Activity of Substituted 1,3,4-Thiadiazoles [PDF]

Scientifica, 2022
1,3,4-Thiadiazole nuclease, a 5-membered heterocyclic ring system containing two nitrogen and one sulfur atoms in addition to carbon atoms, is compound that showed promising results in the process of searching new diuretic agents. In this study, seven 5-
Asrat Ergena, Yerra Rajeshwar, Gebremedhin Solomon   +2 more
doaj   +2 more sources

Synthesis and Antibacterial Activities of Novel Imidazo[2,1-b]-1,3,4-thiadiazoles [PDF]

Molecules, 2011
2-Amino-5-(2-aryl-2H-1,2,3-triazol-4-yl)-1,3,4-thiadiazoles 2-4 have been synthesized by the reaction of 2-aryl-2H-1,2,3-triazole-4-carboxylic acids 1 with thiosemicarbazide. Their reaction with phenacyl (p-substituted phenacyl) bromides led to formation
Kamal F. M. Atta, Omaima O.M. Farahat, Mohamed G. Marei, Alaa Z. A. Ahmed   +3 more
doaj   +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

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

Utility of N-aryl 2-aroylhydrazono-propanehydrazonoyl chlorides as precursors for synthesis of new functionalized 1,3,4-thiadiazoles with potential antimicrobial activity [PDF]

Journal of Advanced Research, 2015
Starting from N-aryl 2-aroylhydrazono-propanehydrazonoyl chlorides, a series of new functionalized 1,3,4-thiadiazoles were prepared. The structures of the compounds prepared were confirmed by both elemental and spectral analyses as well as by alternate ...
Abdou O. Abdelhamid, Sobhi M. Gomha, Ahmad S. Shawali   +2 more
doaj   +2 more sources

Synthesis and antitumor properties of some new 3-R-6-(5-arylfuran-2-yl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazoles

Фармацевтичний журнал, 2021
One of the promising methods of creating antitumor drugs is the screening of potential antitumor agents among synthesized compounds. Nitrogen-based heterocycle analogues are an extremely important class of organic substances that are widely used in ...
I. І. Myrko, Yu. І. Horak, T. I. Chaban, І. V. Drapak, V. S. Matiychuk   +4 more
doaj   +1 more source

Synthesis of Some Substituted 1,3,4-Oxadiazoles, Thiadiazoles and 1,2,4-Triazoles from Acid Chlorides [PDF]

مجلة التربية والعلم, 2013
The conversion of some acid chlorides to substituted 1,3,4-oxadiazole, 1,3,4-thiadiazoles and 1,2,4-triazoles is reported. Benzoyl chloride and 4- nitrobenzoyl chloride were treated with hydrazine hydrate in ethanol to give acid hydrazides (1,2), The ...
E. Q. Mahmood, O. Th. Ali, K. M. Daoud
doaj   +1 more source