Month: October 2022

On September 4, 1997, Jeon, Yoon T.; Gluchowski, Charles published a patent.SDS of cas: 70202-00-5 The title of the patent was Preparation of novel indoles and benzothiazoles for cloned human alpha 2 receptors. And the patent contained the following:

The title compounds [I-IV; R1-R3 = H, C1-7 alkyl, C2-7 alkenyl, alkynyl; R4-R6 = H, halo, Oh, etc.; R7 = H, NH, C1-7 alkyl, etc.; R8 = H, C1-7 alkyl, C2-7 alkenyl, etc.; R9 = H, Ph, C1-7 alkyl, etc.; X = CH2, O, NH, S] which are selective for cloned human alpha 2 receptors and therefore useful for lowering intraocular pressure, for treating presbyopia, migraine, hypertension, alc. withdrawal, drug addiction, rheumatoid arthritis, ischemic pain, spasticity, diarrhea, nasal congestion, urinary incontinence as well as for use as analgesics, sedatives, anesthetics, cognition enhancers and ocular vasoconstriction agents, were prepared Thus, reaction of 7-bromo-5-aminoindole with 2-imidazoline-2-sulfonic acid (ISA) afforded 46% I [R1-R5 = H; R6 = Br; R7-R9 = H; X = N] which showed pEC50 of 9.36 at alpha 2 receptor. The experimental process involved the reaction of 7-chloro-benzothiazol-6-ylamine(cas: 70202-00-5).SDS of cas: 70202-00-5

The Article related to adrenoceptor agonist indole benzothiazole preparation, anesthetic indole benzothiazole preparation, sedative indole benzothiazole preparation, vasoconstriction ocular indole benzothiazole preparation, antiglaucoma agent indole benzothiazole preparation, migraine indole benzothiazole preparation, antihypertensive indole benzothiazole preparation and other aspects.SDS of cas: 70202-00-5

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

On August 16, 2001, Fotouhi, Nader; Gillespie, Paul; Guthrie, Robert William; Pietranico-Cole, Sherrie Lynn; Yun, Weiya published a patent.Synthetic Route of 19989-66-3 The title of the patent was Preparation of N-aroyldehydroamino acids as lymphocyte function associated antigen-1 antagonists.. And the patent contained the following:

Title compounds [I; R1 = H, OH, amino, halo; R2 = H, OH, halo; R3 = H; R2R3 = atoms to form Ph, pyrrole, pyrroline, pyrazole, triazole, imidazole, etc., rings; A = CH2CH2CH(OH), CH2CH2CO, CH2NHCO, etc.; R4, R5 = H, Me, Et; B = H, alkyl, (substituted) (bicyclic) (hetero)aryl, etc.; R6 = CO2H, CO2R7, CH2OH, etc.; R7 = alkyl, dimethylaminoalkyl, pyrrolidinylalkyl, etc.], were prepared Thus, Me (Z)-3-(1H-benzotriazol-5-yl)-2-[[2-chloro-4-[[(3-hydroxybenzyl)amino]carbonyl]-6-methylbenzoyl]amino]propenoate (preparation given) was stirred 125 h with LiOH in MeOH/THF/H2O to give 61% (Z)-3-(1H-benzotriazol-5-yl)-2-[[2-chloro-4-[[(3-hydroxybenzyl)amino]carbonyl]-6-methylbenzoyl]amino]propenoic acid. The latter inhibited LFA-1 binding to immobilized ICAM-1 with IC50 = 0.4 nM. The experimental process involved the reaction of Benzo[d]thiazol-6-ylmethanol(cas: 19989-66-3).Synthetic Route of 19989-66-3

The Article related to aroyldehydroamino acid preparation lymphocyte function associated antigen antagonist, propenoate aroylamino preparation lfa1 antagonist, amino acid dehydro aroyl lymphocyte function associated antigen antagonist, t cell activation inhibitor aroylaminopropenoate preparation, psoriasis graft rejection dermatitis asthma arthritis treatment aroylaminopropenoate and other aspects.Synthetic Route of 19989-66-3

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

On November 2, 2020, Zhang, KaiYue; Li, Jing; Wang, KaiXuan; An, Xiaoying; Wang, LanZhi published an article.Formula: C5H5NOS The title of the article was Atom-economical Approaches to 1,5-Benzodiazepines Containing Indole Ring via Fe3O4@SiO2-PTSA-catalyzed Multi-component Domino Reactions. And the article contained the following:

Four novel atom-economical approaches for synthesis of 1,5-dihydrospiro[benzo[b][1,4]diazepine-2,3′-indole] compounds, e.g., I via three-component or four-component domino reactions was developed in presence of a catalytic amount of magnetic nanoparticles (Fe3O4@SiO2-PTSA) in ethanol, which provided an efficient one-pot synthesis of 1,5-benzodiazepines with multi-ring system and functional groups containing indole, aryl, ester, acyl and alkyl groups in excellent yields. In a one-pot operation, two new nitrogen heterocycle (indole and diazepine) rings and four new chem. bonds (one C-C, two C-N and one C=C) were constructed by series of domino reactions. Furthermore, plausible catalytic synthesis reaction mechanisms had been proposed. The advantages of these methods were green reaction process, recyclable magnetic catalyst, mild reaction conditions, short reaction time and high yields of products. The experimental process involved the reaction of 2-Acetylthiazole(cas: 24295-03-2).Formula: C5H5NOS

The Article related to iron oxide silica supported toluenesulfonic acid nanoparticle catalyst preparation, dihydrospiro benzodiazepine indole chemoselective regioselective green preparation atom economy, phenylenediamine ketone indole multicomponent domino magnetic nanoparticle catalyst, ketone phenylenediamine indole dmf dimethylacetal multicomponent domino magnetic nanocatalyst and other aspects.Formula: C5H5NOS

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

On May 16, 2013, Harriman, Geraldine C.; Masse, Craig E.; Harwood, James; Bhat, Sathesh; Greenwood, Jeremy Robert published a patent.Application of 64987-16-2 The title of the patent was Preparation of thienopyrimidinedione derivatives as ACC inhibitors. And the patent contained the following:

The present invention provides compounds, specifically thienopyrimidine derivatives I [X = O, S, or NR; R1 = H, (un)substituted alkyl; R2 = halo, R, OR, etc.; or R1 and R2 are taken together to form (un)substituted 4-7 membered partially unsaturated carbocyclo-, or heterocyclo-, benzo-, or 5-6 membered heteroaryl- fused ring; R = H, (un)substituted alkyl, Ph, etc.; L1, L2 = a bond, alkylene, cyclobutylenyl, etc.; R3 = H, halo, CN, etc.; R4 = H, (un)substituted 3-8 membered monocyclic saturated or partially unsaturated carbocyclic ring, etc.; with the provisos], useful as inhibitors of Acetyl CoA Carboxylase (ACC), pharmaceutical compositions thereof, and methods of using the same for treating ACC-mediated disorders such as obesity, dyslipidemia, hyperlipidemia, fungal, parasitic or bacterial infections in a subject. The invention further provides a method of inhibiting ACC in a plant comprising contacting the plant with the inhibitor compound I. Over three-hundred compounds I were prepared E.g., a multi-step synthesis of (2S)-II, starting from Et 3-oxobutanoate and Et 2-cyanoacetate, was described. Exemplified compounds I were tested in in vitro ACC1 and ACC2 inhibition assays (data given). The experimental process involved the reaction of Methyl 2-(2-aminothiazol-4-yl)acetate(cas: 64987-16-2).Application of 64987-16-2

The Article related to thienopyrimidinedione preparation acetyl coa carboxylase acc inhibitor metabolic disorder, antiobesity fungicide antiparasitic antibacterial thienopyrimidinedione preparation acc inhibitor, dyslipidemia hyperiipidemia treatment thienopyrimidinedione preparation acc inhibitor, thienopyrimidine preparation acetyl coa carboxylase acc inhibitor metabolic disorder and other aspects.Application of 64987-16-2

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

On April 30, 2004, Moloney, Gerard P.; Garavelas, Agatha; Martin, Graeme R.; Maxwell, Miles; Glen, Robert C. published an article.Category: thiazole The title of the article was Synthesis and serotonergic activity of variously substituted (3-amido)phenylpiperazine derivatives and benzothiophene-4-piperazine derivatives: novel antagonists for the vascular 5-HT1B receptor. And the article contained the following:

The synthesis and vascular 5-HT1B receptor activity of a novel series of substituted 3-amido phenylpiperazine and 4-(4-methyl-1-piperazinyl)-1-benzo[b]thiophene derivatives is described. Modifications to the amido linked sidechains of the 3-amidophenyl piperazine derivatives and to the 2-side-chain of the 1-benzo[b]thiophene derivatives have been explored. Several compounds were identified which exhibited affinity at the vascular 5-HT1B receptor of pKB > 7.0. From the 3-amidophenyl-piperazine series, N-[5-(4-chlorophenyl)-2-thiazolyl]-3-(4-methyl-1-piperazinyl)benzamide (I) and from the benzo[b]thiophene-4-piperazine series N-(2-ethylphenyl)-4-(4-methyl-1-piperazinyl)benzo[b]thiophene-2-carboxamide (II) were identified as a highly potent, silent (as judged by the inability of angiotensin II to unmask 5-HT1B receptor mediated agonist activity in the rabbit femoral artery) and competitive vascular 5-HT1B receptor antagonist. The affinity of compounds from these two series of compounds for the vascular 5-HT1B receptor is discussed as well as a proposed mode of binding to the receptor pharmacophore. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Category: thiazole

The Article related to 5-ht antagonists (type 5-ht1b), 5-ht1b receptors role: bsu (biological study, unclassified), biol (biological study) (antagonists), molecular modeling, pharmacophores, structure-activity relationship, serotoninergic antagonist and other aspects.Category: thiazole

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

The author of 《Testis transcriptome profiling identified genes involved in spermatogenic arrest of cattleyak》 were Wu, Shixin; Mipam, Tserang Donko; Xu, Chuanfei; Zhao, Wangsheng; Shah, Mujahid Ali; Yi, Chuanping; Luo, Hui; Cai, Xin; Zhong, Jincheng. And the article was published in PLoS One in 2020. Recommanded Product: 95-24-9 The author mentioned the following in the article:

Much attempt has been made to examine the mechanisms of male sterility caused by spermatogenic arrest, but yet there is no research systematically and precisely elucidated testis gene expression profiling between cattleyak and yak. Methods: To explore the higher resolution comparative transcriptome map between the testes of yak and cattleyak, and further analyze the mRNA expression dynamics of spermatogenic arrest in cattleyak. We characterized the comparative transcriptome profile from the testes of yak and cattleyak using high-throughput sequencing. Then we used quant. anal. to validate several differentially expressed genes (DEGs) in testicular tissue and spermatogenic cells. Results: Testis transcriptome profiling identified 6477 DEGs (2919 upregulated and 3558 downregulated) between cattleyak and yak. Further anal. revealed that the marker genes and apoptosis regulatory genes for undifferentiated spermatogonia were upregulated, while the genes for differentiation maintenance were downregulated in cattleyak. A majority of DEGs associated with mitotic checkpoint, and cell cycle progression were downregulated in cattleyak during spermatogonial mitosis. Furthermore, almost all DEGs related to synaptonemal complex assembly, and meiotic progression presented no sign of expression in cattleyak. Even worse, dozens of genes involved in acrosome formation, and flagellar development were dominantly downregulated in cattleyak. The experimental process involved the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9Recommanded Product: 95-24-9)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Recommanded Product: 95-24-9Their presence in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications.

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

COA of Formula: C7H5ClN2SOn September 15, 2020 ,《Novel Fluorescent Azacyanine Compounds: Improved Synthesis and Optical Properties》 was published in ACS Omega. The article was written by Dogan, Kubra; Gulkaya, Aybuke; Forough, Mehrdad; Persil Cetinkol, Ozgul. The article contains the following contents:

Benzothiazoles are known to possess a number of biol. activities and therefore are considered to be an important scaffold in the design and synthesis of pharmacophores. In this study, an improved synthesis method for novel fluorescent benzothiazole-based cyclic azacyanine (CAC) dyes bearing different electron-donating/withdrawing groups on their scaffold is presented. The improved method enabled us to increase the synthesis yield for the previously reported CACs. More importantly, it allowed us to synthesize new CAC dyes that were not synthesizable with the previously reported method. The synthesized dyes were characterized by 1H and 13C NMR spectroscopy, elemental anal., and mass spectrometry and their optical (absorption and fluorescence) properties were investigated. All of the synthesized CACs were found to be displaying strong absorption within the range of 387-407 nm. The spectral shifts observed in the absorption and fluorescence measurements suggested that the spectroscopic and optical properties of CACs can be directly modulated by the nature of the electron-donating/withdrawing substituents. The fluorescence quantum yields (QYs) of the unsubstituted (parent CAC) and substituted CACs were also measured and compared. The fluorescence QY of CACs with electron-donating substituents (methoxy or ethoxy) was found to be at least four times higher than that of the parent CAC with no substitutions. In the experiment, the researchers used 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9COA of Formula: C7H5ClN2S)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.COA of Formula: C7H5ClN2SThe thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone.

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

《Flow hydrodediazoniation of aromatic heterocycles》 was published in Molecules in 2019. These research results belong to Roeder, Liesa; Nicholls, Alexander J.; Baxendale, Ian R.. SDS of cas: 95-24-9 The article mentions the following:

Continuous flow processing was applied for the rapid replacement of an aromatic amino group with a hydride. The approach was applied to a range of aromatic heterocycles RNH2 (R = 1,3-benzoxazol-2-yl, 2-pyridyl, 4-cyano-1-phenyl-1H-1,2,3-triazol-5-yl, etc.) confirming the wide scope and substituent-tolerance of the processes. Flow equipment was utilized and the process optimized to overcome the problematically-unstable intermediates that have restricted yields in previous studies relying on batch procedures. Various common organic solvents were investigated as potential hydride sources. The approach has allowed key structures, such as amino-pyrazoles and aminopyridines to be deaminated in good yield using a purely organic-soluble system.6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9SDS of cas: 95-24-9) was used in this study.

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.SDS of cas: 95-24-9Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.

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

《Synergistic effect of copolymeric resin grafted 1,2-benzisothiazol-3(2H)-one and heterocyclic groups as a marine antifouling coating》 was published in RSC Advances in 2021. These research results belong to Dong, Miao; Liu, Zheng; Gao, Yuxing; Wang, Xuemei; Chen, Junhua; Yang, Jianxin. COA of Formula: C7H5ClN2S The article mentions the following:

In order to find a new type of antifouling coating with higher biol. activity and more environmental protection, heterocyclic compounds and benzoisothiazolinone were introduced into acrylic resin to prepare a new type of antifouling resin. In this study, a series of grafted acrylic resins simultaneously containing benzoisothiazolinone and heterocyclic monomers were prepared by the copolymerization of an allyl monomer with Me methacrylate (MMA) and Bu acrylate (BA). Inhibitory activities of the copolymers against marine fouling organisms were also investigated. Results revealed that the copolymers exhibit a clear synergistic inhibitory effect on the growth of three seaweeds: Chlorella, Isochrysis galbana and Chaetoceros curvisetus, resp., and three bacteria, Staphylococcus aureus, Vibrio coralliilyticus and Vibrio parahaemolyticus, resp. In addition, the copolymers exhibited excellent inhibition against barnacle larvae. Marine field tests indicated that the resins exhibit outstanding antifouling potency against marine fouling organisms. Moreover, the introduction of the heterocyclic group led to the significantly enhanced antifouling activities of the resins; the addition of the heterocyclic unit in copolymers led to better inhibition than that observed in the case of the resin copolymerized with only the benzoisothiazolinone active monomer. The results came from multiple reactions, including the reaction of 6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9COA of Formula: C7H5ClN2S)

6-Chlorobenzothiazol-2-ylamine(cas: 95-24-9) belongs to thiazoles. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.COA of Formula: C7H5ClN2SThiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis.

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

Chehab, Rana; Coulomb, Bruno; Boudenne, Jean-Luc; Robert-Peillard, Fabien published an article on January 15 ,2020. The article was titled 《Development of an automated system for the analysis of inorganic chloramines in swimming pools via multi-syringe chromatography and photometric detection with ABTS》, and you may find the article in Talanta.Reference of ABTS Diammonium The information in the text is summarized as follows:

Inorganic chloramines are disinfection byproducts resulting from the unwanted reaction between chlorine used as disinfectant in swimming pools and nitrogenous compounds brought by bathers. This parameter (total chloramines or combined chlorine) is currently measured on site by a colorimetric method that does not allow to measure only inorganic chloramines. In this paper, a multi-syringe chromatog. system combined with a post column derivatization is applied for the first time for the specific detection of the three individual inorganic chloramines (monochloramine, dichloramine and trichloramine). These latter ones are separated using a low-pressure monolithic C18 column, and sep. detected after a post-column reaction with the chromogenic reagent ABTS (2,2′-azino-bis-(3-ethyl-benzothiazoline)-6-sulfonic acid-diammonium salt). Development of two ABTS reagents provides discrimination of chlorine and monochloramine that are not separated on the column. Optimization of the exptl. conditions enables determination of inorganic chloramines with very good detection limits (around 10 μg eq.Cl2 L-1) without interferences from other chlorinated compounds such as organic chloramines or free available chlorine. The validation of the whole procedure has been successfully applied to real swimming pools samples. In the experiment, the researchers used ABTS Diammonium(cas: 30931-67-0Reference of ABTS Diammonium)

ABTS Diammonium(cas: 30931-67-0) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Reference of ABTS Diammonium

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