7496-60-8

Upstream product

• 536-38-9 4-chlorobenzoylmethyl bromide 
• 591-08-2 acetylthiourea 
• 2103-99-3 4-(4-chlorophenyl)-2-thiazolamine 
• 127-09-3 sodium acetate 
• 108-24-7 acetic anhydride 
• 75-36-5 acetyl chloride 

Downstream Products

• 73034-39-6 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-phenyl-benzenesulfonamide 
• 73034-48-7 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-(2-methoxy-phenyl)-benzenesulfonamide 
• 73039-32-4 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-(4-ethoxy-phenyl)-benzenesulfonamide 
• 73034-47-6 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-(3-methoxy-phenyl)-benzenesulfonamide 
• 73034-45-4 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-(2-chloro-phenyl)-benzenesulfonamide 
• 73034-44-3 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-(3-chloro-phenyl)-benzenesulfonamide 
• 73034-46-5 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-(4-methoxy-phenyl)-benzenesulfonamide 
• 73034-42-1 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-o-tolyl-benzenesulfonamide 
• 73034-49-8 5-(2-acetylamino-thiazol-4-yl)-N-(4-bromo-phenyl)-2-chloro-benzenesulfonamide 
• 73034-43-2 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-(4-chloro-phenyl)-benzenesulfonamide 
• 73034-41-0 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-m-tolyl-benzenesulfonamide 
• 73034-40-9 5-(2-acetylamino-thiazol-4-yl)-2-chloro-N-p-tolyl-benzenesulfonamide 
• 73034-70-5 5-(2-amino-thiazol-4-yl)-2-chloro-N-(2-methoxy-phenyl)-benzenesulfonamide 
• 73034-69-2 5-(2-amino-thiazol-4-yl)-2-chloro-N-(3-methoxy-phenyl)-benzenesulfonamide 

Relevant academic research and scientific papers

Antitrichomonal activity and docking analysis of thiazole derivatives as TvMP50 protease inhibitors

Trichomoniasis, caused by the protozoan Trichomonas vaginalis, is the most prevalent non-viral sexually transmitted infection that affects over 170 million people worldwide. The only type of drug recommended for the therapeutic control of trichomoniasis i

Identification and Optimization of Novel Small c-Abl Kinase Activators Using Fragment and HTS Methodologies

Abelson kinase (c-Abl) is a ubiquitously expressed, nonreceptor tyrosine kinase which plays a key role in cell differentiation and survival. It was hypothesized that transient activation of c-Abl kinase via displacement of the N-terminal autoinhibitory "myristoyl latch", may lead to an increased hematopoietic stem cell differentiation. This would increase the numbers of circulating neutrophils and so be an effective treatment for chemotherapy-induced neutropenia. This paper describes the discovery and optimization of a thiazole series of novel small molecule c-Abl activators, initially identified by a high throughput screening. Subsequently, a scaffold-hop, which exploited the improved physicochemical properties of a dihydropyrazole analogue, identified through fragment screening, delivered potent, soluble, cell-active c-Abl activators, which demonstrated the intracellular activation of c-Abl in vivo.

2-amino-4-arylthiazole derivatives as anti-giardial agents: Synthesis, biological evaluation and QSAR studies

A series of seven 2-amino-4-arylthiazoles were prepared following Hantzsch's modified method under microwave irradiation. A set of 50 derivatives was obtained and the in vitro activity against Giardia intestinalis was evaluated. The results on the biological activity revealed that, in general, the N-(5-bromo-4-aryl-thiazol-2-yl)-acetamide scaffold showed high bioactivity. In particular, compounds 6e (IC50= 0.39 μM) and 6b (IC50= 0.87 μM) were found to be more potent than the positive control metronidazole. Citoxicity and acute toxicity tests performed showed low toxicity and high selectivity of the most active compounds (6e SI = 139, 6b SI = 52.3). A QSAR analysis was applied to a data set of 37 obtained 2-amino-4-arylthiazoles derivatives and the best model described a strongly correlation between the anti-giardiasic activity and molecular descriptors as E2M, RDF115m, F10, MATS6v, and Hypnotic-80, with high statistical quality. This finding indicates that N-substituted aminothiazole scaffold should be investigated for the development of highly selective anti-giardial agent.

Preparation, antimicrobial activity, and toxicity of 2-amino-4-arylthiazole derivatives

Seven 2-amino-4-aryl-1,3-thiazoles (1a-g) and their corresponding 2-aminoacetyl (2a-g) and 2-aminoacetyl-5-bromo (3a-g) derivatives were synthesized and tested in vitro against 11 reference strains, three Gram-positive and four Gram-negative bacteria, two yeasts, and two moulds. Toxicity of the compounds was also evaluated using the brine shrimp test. Compounds 1a, 1b, 1e-g, and 3b showed moderate antimicrobial activity at different concentrations. The results indicated that acetylation of the amino group and bromination at position 5 of the thiazole moiety cause lost of activity. Compounds 1a, 1e, and 1f showed toxicity to brine shrimp nauplii below 10 ppm. Most other compounds showed moderate toxicity, LD50 above 100 ppm. Structures of all compounds were confirmed by NMR and MS data.

Structure-activity relationships of thiazole and thiadiazole derivatives as potent and selective human adenosine A3 receptor antagonists

4-(4-Methoxyphenyl)-2-aminothiazole and 3-(4-methoxyphenyl)-5- aminothiadiazole derivatives have been synthesized and evaluated as selective antagonists for human adenosine A3 receptors. A methoxy group in the 4-position of the phenyl ring and

Ac2O-Py/basic alumina as a versatile reagent for acetylations in solvent-free conditions under microwave irradiation

Acetic anhydride-pyridine over basic alumina has been used in order to carry out acetylations of hydroxy, thiol and amino groups in solvent-free conditions under microwave irradiation. The technique can be extended for selective acetylations by regulation of irradiation time.