443111-03-3

Upstream product

• 321309-33-5 5-methylisoxazolyl-3-isothiocyanate 
• 95-74-9 3-chloro-p-toluidine 
• 1072-67-9 5-methylisoxazol-3-ylamine 
• 19241-37-3 2-chloro-4-isothiocyanato-1-methyl-benzene 

Downstream Products

• 1361124-42-6 1-[5-(3-chloro-4-methylphenylamino)-1,2,4-thiadiazol-3-yl]propan-2-ol 
• 1421276-58-5 N-{2'-[5-(3-chloro-4-methylphenylamino)-1,2,4-thiadiazol-3-yl]-1'-methylethyl}-(2'',2'',6'',6''-tetramethylpiperidin-4''-yl)aminodocosa-4Z,7Z,10Z,13Z,16Z,19Z-hexaenoic acid amide 
• 1371630-57-7 N-{2-[5-(4-methyl-3-chlorophenylamino)-[1,2,4]thiadiazol-3-yl]-1-methylethyl}-(2,2,6,6-tetramethylpiperidine-4-yl)-amine 
• 1371630-69-1 {2-[5-(3-chloro-4-methylphenylamino)-[1,2,4]thiadiazol-3-yl]-1-methylvinyl}(2,2,6,6-tetramethyl-piperidin-4-yl)amine 

Relevant academic research and scientific papers

Towards the rational design of novel drugs based on solubility, partitioning/distribution, biomimetic permeability and biological activity exemplified by 1,2,4-thiadiazole derivatives

Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca2+ uptake was investigated. The solubility of thiadiazoles was measured in a buffer solution (pH 7.4) at 298 K. The distribution coefficients in 1-octanol/buffer (pH 7.4) and 1-hexane/buffer (pH 7.4) immiscible phases as model systems imitating the gastrointestinal tract epithelium and the blood-brain barrier were determined. Permeation experiments the new Permeapad barrier using Franz diffusion cells were conducted and the apparent permeability coefficients were obtained. The influence of the compound structure on the physicochemical properties determining the bioavailability of drug-like substances was revealed. Solubility-permeability interplay has been assessed to evaluate potential bioavailability of the compounds studied.

5-AMINO-1,2,4-THIADIAZOLE DERIVATIVES

The present invention relates in general to the field of organic chemistry and, in particular, to novel biologically active compounds of 5-amino[1,2,4]thiadiazole derivatives of the general formula: wherein X is ONO2 or NHR3; R1, R2, and R3 may be the same or different and independently represent hydrogen, alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, as well as R1 together with R2 may represent heterocyclyl (for example, optionally substituted pyrrolidine, piperidine, azepane, piperazine, morpholine, etc.) provided that, when R1 is H, then R2 is other than hydrogen or methyl. 5-Amino-[1,2,4]thiadiazole derivatives are of special interest as drug candidates for prevention and treatment of neurodegenerative diseases, for example, Alzheimer's disease.

Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors: Approach to creation of bioavailable drugs

Novel 1,2,4-thiadiazole derivatives as potent neuroprotectors were synthesized and identified. Their ability to inhibit the glutamate stimulated Ca uptake was measured. Permeation experiments on the phospholipid membranes were conducted, and the apparent