30216-57-0

Usage

Chemical Properties

Light yellow solid

InChI:InChI=1/C4H2ClNOS/c5-3(7)4-6-1-2-8-4/h1-2H

Upstream product

• 75-44-5 phosgene 
• 79265-30-8 2-(trimethylsilyl)thiazole 
• 14190-59-1 1,3-thiazole-2-carboxylic acid 

Downstream Products

• 556025-92-4 2-chloro-1-(thiazol-2-yl)ethan-1-one 
• 30216-59-2 thiazole-2-carboxylic acid phenyl ester 
• 1185279-57-5 1,7-dimethyl-3-(2-methyl-5-(5-(thiazol-2-yl)-1,2,4-oxadiazol-3-ylamino)phenyl)-1,6-naphthyridin-2(1H)-one 
• 1134986-16-5 thiazole-2-carboxylic acid [4-(2,4-dimethylphenyl)thiazol-2-yl]amide 
• 1134986-18-7 thiazole-2-carboxylic acid [4-(2,4,6-trimethylphenyl)thiazol-2-yl]amide 
• 1107061-80-2 C₂₁H₂₂N₂O₆S₂ 
• 1107062-02-1 C₂₀H₂₀N₂O₆S₂ 
• 1232935-44-2 C₂₂H₁₉N₅OS 
• 1354042-20-8 C₂₁H₁₅FN₈O₂S 
• 1374780-10-5 2-(3-chlorobenzo[b]thiophene-2-carboxamido)-4-(thiazole-2-carboxamido)benzoic acid methyl ester 
• 1447308-16-8 C₃₂H₄₃N₇O₅S 
• 1383110-67-5 C₂₄H₂₄N₆O₂S 

Relevant academic research and scientific papers

Discovery of styrylaniline derivatives as novel alpha-synuclein aggregates ligands

Parkinson's disease (PD) is the second most common neurodegenerative disorder. Early diagnosis is the key to treatment but is still a great challenge in the clinic now. The discovery of alpha-synuclein (α-syn) aggregates ligands has become an attractive s

Discovery and Optimization of Chromeno[2,3-c]pyrrol-9(2H)-ones as Novel Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension

Phosphodiesterase 5 (PDE5) inhibitors have been used as clinical agents to treat erectile dysfunction and pulmonary arterial hypertension (PAH). Herein, we detail the discovery of a novel series of chromeno[2,3-c]pyrrol-9(2H)-one derivatives as selective and orally bioavailable inhibitors against phosphodiesterase 5. Medicinal chemistry optimization resulted in 2, which exhibits a desirable inhibitory potency of 5.6 nM with remarkable selectivity as well as excellent pharmacokinetic properties and an oral bioavailability of 63.4%. In addition, oral administration of 2 at a dose of 5.0 mg/kg caused better pharmacodynamics effects on both mPAP (mean pulmonary artery pressure) and RVHI (index of right ventricle hypertrophy) than sildenafil citrate at a dose of 10.0 mg/kg. These activities along with its reasonable druglike properties, such as human liver microsomal stability, cytochrome inhibition, hERG inhibition, and pharmacological safety, indicate that 2 is a potential candidate for the treatment of PAH.

Discovery of N-(4-sulfamoylphenyl)thioureas as Trypanosoma brucei leucyl-tRNA synthetase inhibitors

Human African trypanosomiasis (HAT) is one of the most neglected diseases in the tropic regions, which is fatal if not treated in time. There is an urgent need for new therapeutics, especially those in new chemical classes. Leucyl-tRNA synthetase (LeuRS) has been paid much attention as a recently clinically validated antimicrobial target. Our group has previously reported T. brucei LeuRS (TbLeuRS) inhibitors, including benzoxaboroles targeting the editing site and pyrrolinones targeting the synthetic site. Here we report the discovery of N-(4-sulfamoylphenyl)thioureas as a new class of TbLeuRS inhibitors. The R1 and R2 groups, reminiscent of the leucyl and adenyl regions of aa-AMP and aa-AMS, were optimized to result in a significant 13-fold increase of inhibitory activity (compound 19, IC 50 = 13.7 μM). Aided by ligand-protein docking, the 1,3-substitution at the central phenyl ring was predicted and proved to give significantly improved activity (59, IC50 = 1.1 μM). This work provided a new scaffold for the exploration of novel inhibitors against TbLeuRS, which may become potential therapeutics for the treatment of HAT.

ANTIPARASITIC TERPENE ALKALOIDS

The present invention relates to novel terpene alkaloids and their use as antiparasitic agents. The present invention also relates to an antiparasitic agent which comprises a terpene alkaloid compound of this invention as an effective ingredient in an antiparasitic formulation. More particularly, the present invention relates to derivatives of the terpene alkaloid (1S,2R,4aS,5R,8R,8aR)-2-(acetyloxy)-8a-hydroxy-3,8-dimethyl-5-(1-methylethenyl)-1,2,4a,5,6,7,8,8a-octahydronaphthalen-1-yl (2S,3aR,9bR)-6-chloro-9b-hydroxy-5-methyl-1,2,3,3a,5,9b-hexahydropyrrolo[2,3-c][2,1]benzoxazine-2-carboxylate. Pharmaceutical compositions comprising the same are also disclosed.

Differing Reactivities and Products in the Reaction of Some N-Methylimidazol-2-yl, Oxazol-2-yl and Thiazol-2-ylsilanes and -stannanes with Acid Chlorides

Some new N-methylimidazoles, oxazoles and thiazoles (compounds 7-15) with a keto-function in the 2-position have been synthesized by the reaction of heterocyclic substituted silanes and stannanes with the corresponding acyl chlorides.In cases where the si