35353-26-5

Upstream product

• 1747-60-0 6-methoxybenzothiazol-2-ylamine 
• 98-88-4 benzoyl chloride 
• 6274-29-9 2-amino-5-methoxy-thiophenol 
• 532-55-8 Benzoyl isothiocyanate 

Downstream Products

• 91506-81-9 6-Methoxy-2-(5-phenyl-tetrazol-1-yl)-benzothiazole 

Relevant academic research and scientific papers

Tumor-Activated Benzothiazole Inhibitors of Stearoyl-CoA Desaturase

A series of N-acyl benzothiazoles shows selective and potent cytotoxicity against cancer cell lines expressing cytochrome P450 4F11. A prodrug form is metabolized by cancer cells into an active inhibitor of stearoyl-CoA desaturase (SCD). Substantial variation on the acyl portion of the inhibitors allowed the identification of (R)-27, which balanced potency, solubility, and lipophilicity to allow proof-of-concept studies in mice. The prodrugs were activated inside the tumor, where they can arrest tumor growth. Together, these observations offer promise that a tumor-activated prodrug strategy might exploit the essentiality of SCD for tumor growth, while avoiding toxicity associated with systemic SCD inhibition.

Copper promoted C-S and C-N cross-coupling Reactions:The synthesis of 2-(N-Aryolamino)benzothiazoles and 2-(N-Aryolamino)benzimidazoles

The synthesis of 2-(N-aryolamino)benzothiazoles and 2-(N-aryolamino)benzimidazoles has been accomplished in the presence of copper catalyst. These reactions involve C-S and C-N cross-coupling reaction. All electron donating and withdrawing substituent's readily underwent the reaction to give target products in good to excellent yield. In addition, the reaction also gave target product in high yield with bulk scale.

Neurodegenerative Therapies

The present invention provides a compound of formula (I) wherein: Y represents a C or N atom which may be substituted or form a cyclic group with R′″ but may not be a quaternary C atom; R′ is —OR1, —CONH2, —CF3, F, —OH, —NO2, —CN or —OCOR1 in which R1, is C1-3 alkyl and each may be in the beta or gamma position; R″ is C1-3 alkyl or H; and R′″ is H or a group consisting of 1-12 non-hydrogen atoms and may be linear, branched and/or incorporate one or more cyclic groups, cyclic groups may be aromatic and/or heterocyclic and 2 or more cyclic groups may be linked or fused and each may be substituted; or a salt, hydrate or solvate of a compound of formula (I) for use in the treatment or prevention of a neurodegenerative disorder by inhibiting formation of neurofibrillary (tau) tangles and/or by inhibiting Dyrk 1A. The invention further relates to non-therapeutic uses of these compounds.

METHODS AND COMPOSITIONS FOR SELECTIVE AND TARGETED CANCER THERAPY

Provided herein are methods and compositions for selective and targeted cancer therapy, in particular certain benzothiophenes, benzothiazoles, oxalamides, N-acyl ureas and chromones, and their use in selectively treating certain adenocarcinomas. In some embodiments, the selective toxicity of the compounds may be mediated through SCD1 and/or CYP450 such as CYP4F11.

PTSA catalyzed straightforward protocol for the synthesis of 2-(N-acyl)aminobenzimidazoles and 2-(N-acyl)aminobenzothiazoles in PEG

An efficient PTSA catalyzed synthesis of 2-(N-acyl)aminobenzimidazoles and 2-(N-acyl)aminobenzothiazoles has been described using S-ethylated-N- acylthioureas as substrates and polyethylene glycol as solvent.

ELECTROLUMINESCENT METAL COMPLEX

Metal complexes of the formula I or I' [LDH]n M [L]m (I) [LTH] (M [L]p)2 (I1) wherein n is an integer 1 or 2, m and p each is an integer 1 or 2, the sum (n+m) being 2 or 3, M is a metal with an atomic weight of

Identification of small-molecule inhibitors of the Aβ-ABAD interaction

The interaction of amyloid beta peptide (Aβ) and Aβ-binding alcohol dehydrogenase (ABAD) was recently implicated in the pathogenesis of Alzheimer's disease (AD). Using an ELISA-based screening assay, we identified frentizole, an FDA-approved immunosuppressive drug, as a novel inhibitor of the Aβ-ABAD interaction. Analysis of the frentizole structure-activity relationship led to identification of a novel benzothiazole urea with a 30-fold improvement in potency.

Synthesis, Photolysis and Pyrolysis of 1-(2'-Benzothiazolyl)-5-aryltetrazoles

Aroylaminobenzothiazoles (II), have been converted into 1-(2'-benzothiazolyl)-5-aryltetrazoles (IV) by treatment with PCl5 followed by azidolysis with sodium azide in aequeous acetone solution.Pyrolysis of IV in tetralin affords exclusively 2-aryl-s-triaz