Category: 19989-66-3

Burger, Alfred; Sawhney, S. N. published an article in 1968, the title of the article was Antimalarials. III. Benzothiazole amino alcohols.Computed Properties of 19989-66-3 And the article contains the following content:

Amino alcs. carrying a CHOH(CH2)1-3NR2 chain in position 6 of a benzothiazole nucleus, unsubstituted or substituted by Ph or CF3 in the 2 position, have been synthesized by standard methods and tested for activity against Plasmodium berghei in mice. Several of the amino alcs. showed weak antimalarial activity but only at toxic doses. 15 references. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Computed Properties of 19989-66-3

The Article related to amino alcohols: chemical synthesis, amino alcohols: therapeutic use, amino alcohols: toxicity, animals, antimalarials: chemical synthesis, antimalarials: therapeutic use, antimalarials: toxicity, mice, thiazoles: chemical synthesis, thiazoles: therapeutic use and other aspects.Computed Properties of 19989-66-3

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 21, 2008, Brak, Katrien; Doyle, Patricia S.; McKerrow, James H.; Ellman, Jonathan A. published an article.COA of Formula: C8H7NOS The title of the article was Identification of a New Class of Nonpeptidic Inhibitors of Cruzain. And the article contained the following:

Cruzain is the major cysteine protease of Trypanosoma cruzi, which is the causative agent of Chagas disease and is a promising target for the development of new chemotherapy. With the goal of developing potent nonpeptidic inhibitors of cruzain, the substrate activity screening (SAS) method was used to screen a library of protease substrates initially designed to target the homologous human protease cathepsin S. Structure-based design was next used to further improve substrate cleavage efficiency by introducing addnl. binding interactions in the S3 pocket of cruzain. The optimized substrates were then converted to inhibitors by the introduction of cysteine protease mechanism-based pharmacophores. Inhibitor 38 was determined to be reversible even though it incorporated the vinyl sulfone pharmacophore that is well documented to give irreversible cruzain inhibition for peptidic inhibitors. The previously unexplored β-chloro vinyl sulfone pharmacophore provided mechanistic insight that led to the development of potent irreversible acyl- and aryl-oxymethyl ketone cruzain inhibitors. For these inhibitors, potency did not solely depend on leaving group pKa, with 2,3,5,6-tetrafluorophenoxymethyl ketone 54 identified as one of the most potent inhibitors with a second-order inactivation constant of 147,000 s-1 M-1. This inhibitor completely eradicated the T. cruzi parasite from mammalian cell cultures and consequently has the potential to lead to new chemotherapeutics for Chagas disease. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).COA of Formula: C8H7NOS

The Article related to nonpeptidic inhibitor cruzain structure chagas disease, Pharmacology: Structure-Activity and other aspects.COA of Formula: C8H7NOS

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On March 20, 2003, Deghati, Paymaneh Y. F.; Borghini, Alice; Van Den Nieuwendijk, Adrianus M. C. H.; Dissen-de Groote, Miriam; IJzerman, Adriaan P. published an article.Recommanded Product: 19989-66-3 The title of the article was Inhibition of nucleoside transport By new analogues of nitrobenzylthioinosine. And the article contained the following:

Nitrobenzylthioinosine (NBTI, 1) was systematically modified by attachment of substituents at positions C6 and N9, and also by substitution of N1 with C. These modifications were chosen to reduce the polarity of the new compounds Incorporation of the nitro functionality into a benzoxadiazole ring system was considered first. These new nucleosides showed high affinity (1.5-10 nM) towards the nucleoside transport protein as present on human erythrocyte ghosts. Next, modification of this benzoxadiazole ring system with C, S and O in different positions produced a number of less polar nucleosides with affinity in the higher nanomolar range. Modification of N9 was achieved with different alkyl and alc. substituents. An Bu substituent proved best, although all variations yielded substantial decreases in affinity. Replacement of N1 by a carbon atom in combination with a 2-Cl substituent also resulted in a relatively potent NBTI derivative (47 nM). The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Recommanded Product: 19989-66-3

The Article related to nitrobenzylthioinosine analog preparation structure activity nucleoside transport protein, Pharmacology: Structure-Activity and other aspects.Recommanded Product: 19989-66-3

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On September 22, 2005, Lynch, John K.; Collins, Christine A.; Freeman, Jennifer C.; Gao, Ju; Iyengar, Rajesh R.; Judd, Andrew S.; Kym, Philip R.; Mulhern, Mathew M.; Sham, Hing L.; Souers, Andrew J.; Zhao, Gang; Wodka, Dariusz published a patent.Safety of Benzo[d]thiazol-6-ylmethanol The title of the patent was Preparation of piperidinyl chromenecarboxamides as antagonists of melanin concentrating hormone effects on the melanin concentrating hormone receptor. And the patent contained the following:

The present invention is directed to compounds of formula (I, variables defined below), which antagonize the effects of melanin-concentrating hormone (MCH) through the melanin concentrating hormone receptor which is useful for the prevention or treatment of eating disorders, weight gain, obesity, abnormalities in reproduction and sexual behavior, thyroid hormone secretion, diuresis and water/electrolyte homeostasis, sensory processing, memory, sleeping, arousal, anxiety, depression, seizures, neurodegeneration and psychiatric disorders. The variables for I are: L = a bond or alkylene, alkenylene, alkynylene, CH2O, SO2NH, C(O)NH, NHCO, NHSO2, CO, SO and SO2; X = O and N(R13); Z = CH2, C(N-Rc), CO and CS; m = 1 or 2; n = 0-2; R1, R2 and R3 = H, alkenyl, alkoxy, alkyl, alkylcarbonyl, alkylcarbonyl-NH-, alkyl-NH-carbonyl, alkylsulfonyl-NH-, alkyl-NH-sulfonyl, alkylsulfonyl, alkylthio, alkynyl, cyano, halogen, haloalkyl, haloalkoxy, haloalkylthio, nitro, RaRbN, RaRbNC(O)- or R1 and R2 together with intervening atoms form a heteroaryl or heterocycle; R4 = H, alkyl, alkylcarbonyl-NH-, alkylsulfonyl-NH-, aryl and halogen; R5 = H and alkyl; R6 = H, alkyl, aryl, cycloalkyl, heteroaryl and heterocycle; R7 = aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocycle and heterocyclealkyl, or R6 and R7 together with attached atoms form a cycloalkyl or heterocycle; R8 = H, alkyl and alkoxy; R9 = H and alkyl; R10 and R11= H, alkyl, alkoxylalkyl, or R10 and R11 together with intervening atoms form a 5, 6, or 7-membered ring; R12 = H and alkyl; R13 = H, alkyl, aryl, cycloalkyl, heteroaryl and heterocycle; Ra and Rb = H, alkoxycarbonyl, alkyl, alkylcarbonyl, alkyl-NH-carbonyl, alkylsulfonyl, aryl and arylalkyl or Ra and Rb together with the attached N form a heteroaryl or heterocycle; and Rc = H and alkyl; provided that at least one of R1, R2 or R3 are not H. Pharmaceutical formulations containing I are also claimed. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Safety of Benzo[d]thiazol-6-ylmethanol

The Article related to piperidinyl chromene carboxamide preparation antagonist melanin concentration hormone antiobesity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of Benzo[d]thiazol-6-ylmethanol

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On August 25, 2005, Lynch, John K.; Collins, Christine A.; Freeman, Jennifer C.; Gao, Ju; Iyengar, Rajesh R.; Judd, Andrew Stephen; Kym, Philip R.; Mulhern, Mathew M.; Sham, Hing L.; Souers, Andrew J.; Zhao, Gang published a patent.Name: Benzo[d]thiazol-6-ylmethanol The title of the patent was Preparation of piperidinyl-chromene carboxamides as antagonists of melanin-concentrating hormone. And the patent contained the following:

Title compounds I [L = a bond, alkyl, alkenyl, etc.; W = (CH2)n; X = O or NR13; Y = (CH2)m; Z = CH2, CO, CS, etc.; m = 1-2; n = 0-2; R1, R2 and R3 independently = H, halo, alkoxy, etc.; R4 = H, aryl, alkyl-C(O)-NH-, etc.; R5 = H or alkyl; R6 = H, cycloalkyl, heterocycle, etc.; R7 = aryl, arylalkyl, heterocycloalkyl, etc.; R8 = H, alkyl or alkoxy; R9 = H or alkyl; R10 and R11 independently = H, alkyl, alkoxyalkyl, etc. or together may form 5-7 membered ring; R12 = H or alkyl; R13 = H, alkyl, aryl, etc.] and their pharmaceutically acceptable salts, are prepared and disclosed as antagonists of melanin-concentrating hormone (MCH). Thus, e.g., II was prepared by cyclization of 1-(4-chloro-2-hydroxyphenyl)ethanone (preparation given) with di-Et oxalate followed by hydrolysis and coupling with 4-amino-1-N-Boc-piperidine and subsequent deprotection and coupling with piperonal. The activity of I was evaluated in fluorescence assays following the intracellular calcium release induced by MCH and it was revealed that compounds of the invention inhibit MCH induced fluorescence at a dose of 10 μM. I as antagonists of melanin-concentration hormone should prove useful in the treatment of obesity, depression and psychiatric disorders. Pharmaceutical compositions comprising I are disclosed. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Name: Benzo[d]thiazol-6-ylmethanol

The Article related to piperidinyl chromene carboxamide preparation antagonist melanin concentration hormone antiobesity, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Name: Benzo[d]thiazol-6-ylmethanol

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On October 15, 2003, Puetz, Claudia; Sundermann, Bernd; Sundermann, Corinna; Ijzermann, Adriaan Pieter; Tromp, Reynier; Von Frijtag, Drabbe Kuenzel Jacobien published a patent.Electric Literature of 19989-66-3 The title of the patent was Preparation of analogs of nitrobenzylthioinosine for the treatment of pain, epilepsy, and other CNS-related disorders. And the patent contained the following:

This invention relates to new nucleoside analogs I, wherein or derivatives of nitrobenzylthioinosine, use of these new analogs of nitrobenzylthioinosine for the treatment of pain and various other diseases as well as pharmaceuticals comprising at least on new analog of nitrobenzylthioinosine. The derivatives of nitrobenzylthioinosine according to the invention are surprisingly effective in the treatment of pain and in other indications. Therefore a further embodiment of the invention comprises the use of a derivatives of nitrobenzylthioinosine according to the invention for the treatment of pain, especially acute, chronic and/or neuropathic pain. Treatment using derivatives of nitrobenzylthioinosine according to the invention especially for the treatment of pain, especially acute, chronic and/or neuropathic pain; the treatment of epilepsy and other CNS-related disorders as well as for neuro-protection or cardio-protection. A further embodiment of the invention comprises the use of a derivatives of nitrobenzylthioinosine according to the invention for the treatment of epilepsy and other CNS-related disorders as well as for neuroprotection or cardio-protection. Thus, 2-[6-(benzo[c]iso-thiazol-5-ylmethylsulfanyl)-purin-9-yl]-5-hydroxymethyl-tetrahydro-furan-3,4-diol was prepared and tested for the treatment of pain, epilepsy, transport protein on human erythrocyte membranes (Ki > 1.5 nM), and other CNS-related disorders. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Electric Literature of 19989-66-3

The Article related to human nitrobenzylthioinosine nucleoside preparation treatment pain epilepsy cns, Carbohydrates: Nucleosides and Nucleotides, Cobalamins, Riboflavin and other aspects.Electric Literature of 19989-66-3

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

McKillop, Alexander; Sayer, Trevor S. B.; Bellinger, Geoffrey C. A. published an article in 1976, the title of the article was Reaction of benzothiazole and substituted benzothiazoles with dimethyl acetylenedicarboxylate. A novel heterocyclic ring transformation.Safety of Benzo[d]thiazol-6-ylmethanol And the article contains the following content:

Addnl. data considered in abstracting and indexing are available from a source cited in the original document. Reaction of benzothiazole with MeO2CCCCO2Me in aqueous methanol gave trans-dimethyl 4-formyl-2,3-dihydro-1,4-benzothiazine-2,3-dicarboxylate (I) in high yield, and a mechanism via intermediates II and III was proposed for this novel transformation. The scope and limitations of the process were defined by examination of the reactions of a wide range of substituted (e.g., 5- and 6-cyano, 5- and 6-Br, 5- and 6-AcNH) benzothiazoles with MeO2CCCCO2Me in aqueous methanol; the results are fully consistent with the postulated mechanism. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Safety of Benzo[d]thiazol-6-ylmethanol

The Article related to ring enlargement benzothiazole, benzothiazinedicarboxylate, acetylenedicarboxylate reaction benzothiazole, thiazole benzo ring enlargement, thiazinedicarboxylate benzo, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Safety of Benzo[d]thiazol-6-ylmethanol

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On May 7, 2015, Burnett, Duane A.; Bursavich, Matthew Gregory; McRiner, Andrew J. published a patent.Reference of Benzo[d]thiazol-6-ylmethanol The title of the patent was Spiro-oxadiazoline compounds as agonists of α-7-nicotinic acetylcholine receptors and their preparation. And the patent contained the following:

The invention relates to spiro-oxadiazoline compounds of formula I, II, and III, that are suitable as agonists or partial agonists of α7-nAChR, and pharmaceutical compositions of the same, methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering a spiro-oxadiazoline α7-nAChR agonist or partial agonist, to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom. Compounds of formula I, II and III wherein R1 is H, C1-6 alkyl, C3-6 cycloalkyl, heteroaryl, etc.; n is 0 to 6; W is (un)substituted 5- to 6-membered heteroaryl, (un)substituted 9- to 10-membered bicyclic heteroaryl, (un)substituted aryl, etc.; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclocondensation of N-hydroxybenzimidamide with 3-quinuclidinone hydrochloride. The invention compounds were evaluated for their α7-nAChR agonistic activity. From the assay it was determined that compound IV exhibited 65% inhibition at 10 μM. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Reference of Benzo[d]thiazol-6-ylmethanol

The Article related to spirooxadiazoline preparation alpha7 nachr agonist, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Reference of Benzo[d]thiazol-6-ylmethanol

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On March 9, 2017, Smallheer, Joanne M.; Shaw, Scott A.; Halpern, Oz Scott; Hu, Carol Hui; Kick, Ellen K. published a patent.Application In Synthesis of Benzo[d]thiazol-6-ylmethanol The title of the patent was Preparation of triazolopyridines as inhibitors of myeloperoxidase. And the patent contained the following:

The invention provides compounds of formula I and compositions comprising any of such compounds These compounds are myeloperoxidase (MPO) inhibitors and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments. Compounds of formula I wherein A is (un)substituted 5-membered heteroaryl; and stereoisomers, tautomers, pharmaceutically acceptable salts and solvates thereof, are claimed. Example compound II•TFA was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their MPO inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values in the range of 1 nM to 100 nM. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Application In Synthesis of Benzo[d]thiazol-6-ylmethanol

The Article related to triazolopyridine preparation myeloperoxidase inhibitor, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Application In Synthesis of Benzo[d]thiazol-6-ylmethanol

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica

On July 20, 2011, Su, Weiguo; Jia, Hong; Dai, Guangxiu published a patent.Safety of Benzo[d]thiazol-6-ylmethanol The title of the patent was Preparation of triazolo[b]pyridine and triazolo[b]pyrazine derivatives as antitumor agents. And the patent contained the following:

Title compounds I [X = N or C(R6); Y = O, S, or NR7; R1 = (un)substituted aryl, aromatic heterocyclic group, or fused aromatic hetero-bicyclic group; R2 and R3 = H or alkyl; or R2 and R3 with the carbon which they connect to form 3- to 7-membered cycloalkyl or heterocycloalkyl; R4 = alkyl, cycloalkyl, heterocyclic group, aryl, or aromatic heterocyclic group; R6 = H, OH, NH2, halo, etc.; R7 = H or alkyl], and their pharmaceutically acceptable salts as antitumor agents, which show inhibitor effects on C-Met expression. Thus, e.g., II was prepared by condensation reaction of 3,5-dibromo-2-pyrazinamine with 1H-pyrrolo[2,3-b]pyridine-3-methanamine followed by cyclization and Suzuki reaction with 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole. Compounds of the invention were evaluated for their inhibitory activity of c-Met kinase with IC50 values of typically ranging from 0.001 μM to 1 μM. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Safety of Benzo[d]thiazol-6-ylmethanol

The Article related to triazolopyridine triazolopyrazine preparation c met kinase antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Safety of Benzo[d]thiazol-6-ylmethanol

Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica