Tag: 200-300

On February 13, 2003, Wells, Geoffrey; Berry, Jane M.; Bradshaw, Tracey D.; Burger, Angelika M.; Seaton, Angela; Wang, Bo; Westwell, Andrew D.; Stevens, Malcolm F. G. published an article.Application of 92-36-4 The title of the article was 4-Substituted 4-Hydroxycyclohexa-2,5-dien-1-ones with Selective Activities against Colon and Renal Cancer Cell Lines. And the article contained the following:

The synthesis and antitumor evaluation of a series of new heteroaromatic- and aromatic-substituted hydroxycyclohexadienones (quinols), and their imine counterparts, are described. The quinols were synthesized via the addition of a lithiated aromatic moiety to a quinone ketal followed by deprotection. When the aromatic portion of the mol. is a fused heterobicyclic structure (e.g., benzothiazole derivative I), potent in vitro antitumor activity was observed in HCT 116 (GI50 = 40 nM) and HT 29 (GI50 = 380 nM) human colon as well in as MCF-7 and MDA 468 human breast cancer cell lines. When examined on the NCI Developmental Therapeutics Screening Program in vitro screen (60 human cancer cell lines), active compounds in this series consistently displayed a highly unusual pattern of selectivity; cytotoxicity (LC50) was concentrated in certain colon and renal cell lines only. I also showed in vivo antitumor activity against human RXF 944XL renal xenografts in nude NMRI mice and is the focus of further study. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Application of 92-36-4

The Article related to hydroxycyclohexadienone aryl heteroaryl preparation antitumor colon rectal cancer, quinol aryl heteroaryl preparation antitumor colon renal cancer, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Application of 92-36-4

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

On January 8, 2009, Wang, Xueqing; Sarris, Katerina; Kage, Karen; Zhang, Di; Brown, Scott P.; Kolasa, Teodozyi; Surowy, Carol; El Kouhen, Odile F.; Muchmore, Steven W.; Brioni, Jorge D.; Stewart, Andrew O. published an article.Formula: C14H12N2S The title of the article was Synthesis and Evaluation of Benzothiazole-Based Analogues as Novel, Potent, and Selective Fatty Acid Amide Hydrolase Inhibitors. And the article contained the following:

High-throughput screening (HTS) identified benzothiazole analog (I) as a potent fatty acid amide hydrolase (FAAH) inhibitor. Structure-activity relationship (SAR) studies indicated that the sulfonyl group, the piperidine ring and benzothiazole were the key components to their activity, with II being the most potent analog in this series. Time-dependent preincubation study of compound I was consistent with it being a reversible inhibitor. Activity-based protein-profiling (ABPP) evaluation of I in rat tissues revealed that it had exceptional selectivity and no off-target activity with respect to other serine hydrolases. Mol. shape overlay of I with a known FAAH inhibitor indicated that these compounds might act as transition-state analogs, forming putative hydrogen bonds with catalytic residues and mimicking the charge distribution of the tetrahedral transition state. The modeling study also indicated that hydrophobic interactions of the benzothiazole ring with the enzyme contributed to its extraordinary potency. These compounds may provide useful tools for the study of FAAH and the endocannabinoid system. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Formula: C14H12N2S

The Article related to carboxylic acid amine acylation, azacycle preparation fatty acid amide hydrolase inhibition, structure activity antinociception human, Heterocyclic Compounds (More Than One Hetero Atom): Thiazoles, Isothiazoles and other aspects.Formula: C14H12N2S

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

On January 16, 2014, Jana, Gourhari; Kurhade, Sanjay Pralhad; Jagdale, Arun Rangnath; Kukreja, Gagan; Sinha, Neelima; Palle, Venkata P.; Kamboj, Rajender Kumar published a patent.Application of 1092942-42-1 The title of the patent was Preparation of tetrahydroquinazolinone derivatives as PARP inhibitors for treating cancer. And the patent contained the following:

Disclosed are compounds of formula I, their tautomeric forms, stereoisomers, and pharmaceutically acceptable salts thereof, (wherein M is C, CH, and N, and the dotted bond is either a single or double bond with provisos; R1 is H and (un)substituted alkyl; R2 and R3 together with the carbon atom(s) to which they are attached form a (un)substituted carbocycle; each R4 is halogen, cyano, (un)substituted alkyl, etc.; R5 and R6 are independently H, halogen, (un)substituted alkyl, etc., or R5 and R6 together constitute oxo or form part of an (un)substituted carbocycle; R7a, R8a, R7b R8b, R7c, R8c, R7d, and R8d are independently H, halogen, (un)substituted alkyl, etc., or any two form oxo or form part of an (un)substituted carbocycle or (un)substituted heterocycle, thereby making ring A either a spiro-bicycle or a fused-bicycle or a bridged-bicycle; Ar is (un)substituted aryl or (un)substituted heteroaryl; p = 0-3; and n = 1-4), pharmaceutical compositions including a compound, tautomer, stereoisomer, or salt thereof, and methods of treating or preventing diseases or disorders, for example, cancer, that are amenable to treatment or prevention by inhibiting the PARP enzyme of a subject. I can also be used to sensitize a patient that has developed a resistance to other chemotherapeutics. Synthetic procedures for preparing I are exemplified. Example compound II, prepared from intermediates Et 6-oxospiro[2.5]octane-5-carboxylate and 4-(4-(4-chlorophenyl)piperazin-1-yl)butanimidamide, had a PARP 1 inhibition IC50 between 1 nM and 500 nM. The experimental process involved the reaction of 2-Bromo-N-methylthiazole-4-carboxamide(cas: 1092942-42-1).Application of 1092942-42-1

The Article related to tetrahydroquinazolinone derivative parp inhibitor treatment cancer, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.Application of 1092942-42-1

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

Shaikh, Asif R.; Patel, Navin B.; Rajani, Dhanji published an article in 2014, the title of the article was Antimycobacterial and antimicrobial studies of newly synthesized 3-(4-(6-methylbenzo[d]thiazol-2-yl) phenyl)quinazolin-4(3H)-ones.HPLC of Formula: 92-36-4 And the article contains the following content:

The 7-chloro-2-(substituted)-3-(4-(6-methylbenzo[d]thiazol-2-yl)phenyl) quinazolin-4(3H)-ones e.g., I (R = furan-2-yl) have been prepared from the substituted acids, which were converted to substituted acetyl chlorides and cyclized with 4-chloro anthranilic acid afforded substituted benzoxazines 4(3H)-ones e.g., II and its further reaction with 4-(6-methylbenzo[d]thiazol-2-yl)aniline a gives desired compounds I. In vitro antitubercular activity was carried out against Mycobacterium tuberculosis H37Rv strain using Lowenstein-Jensen medium (conventional method) and antimicrobial activity against various bacteria and fungi using broth microdilution method. The compounds II, I were emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antituberculars. The compounds II, I showed better antitubercular activities compared to rifampicin and isoniazid. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).HPLC of Formula: 92-36-4

The Article related to quinazolinone preparation antibacterial antifungal antitubercular, Heterocyclic Compounds (More Than One Hetero Atom): Pyrimidines and Quinazolines and other aspects.HPLC of Formula: 92-36-4

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

On April 9, 2020, Qiu, Yunguang; Huang, Lu; Fu, Jie; Han, Chenxia; Fang, Jing; Liao, Ping; Chen, Zhuo; Mo, Yiqing; Sun, Peihua; Liao, Daqing; Yang, Linghui; Wang, Jing; Zhang, Qiansen; Liu, Jin; Liu, Feng; Liu, Tingting; Huang, Wei; Yang, Huaiyu; Jiang, Ruotian published an article.Product Details of 92-36-4 The title of the article was TREK Channel Family Activator with a Well-Defined Structure-Activation Relationship for Pain and Neurogenic Inflammation. And the article contained the following:

TWIK-related K+ (TREK) channels are potential analgesic targets. However, selective activators for TREK with both defined action mechanism and analgesic ability for chronic pain have been lacking. Here, we report (1S,3R)-3-((4-(6-methylbenzo[d]thiazol-2-yl)phenyl)carbamoyl)cyclopentane-1-carboxylic acid (C3001a), a selective activator for TREK, against other two-pore domain K+ (K2P) channels. C3001a binds to the cryptic binding site formed by P1 and TM4 in TREK-1, as suggested by computational modeling and exptl. anal. Furthermore, we identify the carboxyl group of C3001a as a structural determinant for binding to TREK-1/2 and the key residue that defines the subtype selectivity of C3001a. C3001a targets TREK channels in the peripheral nervous system to reduce the excitability of nociceptive neurons. In neuropathic pain, C3001a alleviated spontaneous pain and cold hyperalgesia. In a mouse model of acute pancreatitis, C3001a alleviated mech. allodynia and inflammation. Together, C3001a represents a lead compound which could advance the rational design of peripherally acting analgesics targeting K2P channels without opioid-like adverse effects. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Product Details of 92-36-4

The Article related to trek channel activator preparation pain neuroinflammation, Pharmacology: Effects Of Nervous System- and Behavior-Affecting Drugs and Neuromuscular Agents and other aspects.Product Details of 92-36-4

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

On October 15, 2006, Zhou, Yuefen; Sun, Zhongxiang; Froelich, Jamie M.; Hermann, Thomas; Wall, Daniel published an article.HPLC of Formula: 92-36-4 The title of the article was Structure-activity relationships of novel antibacterial translation inhibitors: 3,5-Diamino-piperidinyl triazines. And the article contained the following:

Structure-activity relationships of the 3,5-diamino-piperidinyl triazine series, a novel class of bacterial translation inhibitors, are described. Optimization was focused on the triazine C-4 position in which aromatic substituents that contained electron-withdrawing groups led to potent inhibitors. The initial lack of antibacterial activity was correlated with poor cellular penetration. Whole cell antibacterial activity was achieved by linking addnl. aromatic moieties at the triazine C-4 position. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).HPLC of Formula: 92-36-4

The Article related to antibacterial translation inhibition diaminopiperidinyl triazine derivative sar preparation, Air Pollution and Industrial Hygiene: Combustion Engine Exhaust Gas and Catalytic Converters and other aspects.HPLC of Formula: 92-36-4

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

On April 25, 2013, Ogamino, Takahisa; Yamazaki, Yukiyoshi; Tanikawa, Shin; Okuda, Ayumu; Fukuda, Tomoaki; Tokuda, Okihisa; Miyake, Yoshiharu; Itoh, Shinsuke; Ishiwata, Hiroyuki published a patent.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate The title of the patent was Preparation of spiroindoline compounds for activating glucokinase. And the patent contained the following:

Title compounds I [ring A = nitrogen-containing heterocyclyl; R1, R2 = independently H, halo, haloalkyl, etc.; R3 = H, (un)substituted alkyl, -COR7, etc.; R7 = H, (un)substituted alkyl, haloalkyl, etc.; R4 = H, halo, cyano, etc.; or salts or solvates thereof], useful for the treatment of diabetes, glucose intolerance, metabolic syndrome, etc., were prepared For example, reaction of 2-amino-5-chlorothiazole·HCl with 4-nitrophenyl chloroformate, treatment with tert-Bu 5-bromospiro[indoline-3,3′-pyrrolidine]-1′-carboxylate, deprotection using CF3CO2H, and acetylation afforded compound II. The invention compounds activated glucokinase activity in vitro assay, e.g., III showed 1192% activation at 1 μmol/L. The experimental process involved the reaction of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate(cas: 859522-19-3).Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

The Article related to spiroindoline preparation glucokinase activator, diabetes glucose intolerance metabolic syndrome treatment spiroindoline glucokinase activation, Heterocyclic Compounds (One Hetero Atom): Spiro Compounds With One Hetero Atom In Each Ring and other aspects.Safety of Ethyl 2-((2-aminothiazol-5-yl)thio)acetate

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

On March 31, 2005, Sekar, N. published an article.Application In Synthesis of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Thiazole – containing monoazo direct dyes. And the article contained the following:

A review. Chem. of monoazo direct dyes based on dehydrothio-p-toluidine and its higher analogs and the others containing thiazolyl residue is discussed in the light of structures documented in color index. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Application In Synthesis of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to review thiazole containing monoazo direct dye, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Reviews and other aspects.Application In Synthesis of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On September 30, 2006, Gadre, J. N.; Periaswamy, R. M. S.; Mulay, Mohit; Vaze, C. S. published an article.Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole The title of the article was Synthesis of pyridone based azo disperse dyes. And the article contained the following:

Pyridone derivatives have proved to be the best heterocyclic couplers as they provide proper nucleophilic center. In the present project N-aryl imides (pyridine-2,6-dione) were coupled with diazotized substituted aniline derivatives to yield azo disperse dyes. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole

The Article related to pyridone based azo disperse dye aryl imide pyridinedione aniline, Dyes, Organic Pigments, Fluorescent Brighteners, and Photographic Sensitizers: Azo Dyes and Pigments and other aspects.Reference of 2-(4-Aminophenyl)-6-methylbenzothiazole

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

On October 31, 2012, Lei, Ying-jie; Bi, Ye; Ouyang, Jie; Ding, Mei published an article.Electric Literature of 92-36-4 The title of the article was Synthesis of 2-(4-aminophenyl)-6-benzothiazoles derivatives in the presence of manganese(III) acetate. And the article contained the following:

Several 4-nitrophenybenzothiazole intermediates were prepared by condensation reaction of 2-aminothiophenol and(substituted) 4-nitrobenzaldehyde in the presence of manganese(III) acetate and the procedure was shown to be mild and easy, which was followed with a reduction under the Pd/C catalyst to afford the desired amino derivatives and resulted in yields of 63-79%. The formation of the corresponding products was confirmed by IR, 1HNMR and elemental anal. The experimental process involved the reaction of 2-(4-Aminophenyl)-6-methylbenzothiazole(cas: 92-36-4).Electric Literature of 92-36-4

The Article related to synthesis aminophenylbenzothiazole derivative manganese acetate, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Electric Literature of 92-36-4

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