Day: February 22, 2023

A podocyte-based automated screening assay identifies protective small molecules was written by Lee, Ha Won;Khan, Samia Q.;Faridi, Mohd. Hafeez;Wei, Changli;Tardi, Nicholas J.;Altintas, Mehmet M.;Elshabrawy, Hatem A.;Mangos, Steve;Quick, Kevin L.;Sever, Sanja;Reiser, Jochen;Gupta, Vineet. And the article was included in Journal of the American Society of Nephrology in 2015.Reference of 1226056-71-8 This article mentions the following:

Podocyte injury and loss mark an early step in the pathogenesis of various glomerular diseases, making these cells excellent targets for therapeutics. However, cell-based high-throughput screening assays for the rational development of podocyte-directed therapeutics are currently lacking. Here, we describe a novel high-content screening-based phenotypic assay that analyzes thousands of podocytes per assay condition in 96-well plates to quant. measure dose-dependent changes in multiple cellular features. Our assay consistently produced a Z’ value >0.44, making it suitable for compound screening. On screening with >2100 pharmacol. active agents, we identified 24 small mols. that protected podocytes against injury in vitro (1% hit rate). Among the identified hits, we confirmed an 尾1-integrin agonist, pyrintegrin, as a podocyte-protective agent. Treatment with pyrintegrin prevented damage-induced decreases in F-actin stress fibers, focal adhesions, and active 尾1-integrin levels in cultured cells. In vivo, administration of pyrintegrin protected mice from LPS-induced podocyte foot process effacement and proteinuria. Anal. of the murine glomeruli showed that LPS administration reduced the levels of active 尾1 integrin in the podocytes, which was prevented by cotreatment with pyrintegrin. In rats, pyrintegrin reduced peak proteinuria caused by puromycin aminonucleoside-induced nephropathy. Our findings identify pyrintegrin as a potential therapeutic candidate and show the use of podocyte-based screening assays for identifying novel therapeutics for proteinuric kidney diseases. In the experiment, the researchers used many compounds, for example, N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8Reference of 1226056-71-8).

N-Benzyl-2-(pyrimidin-4-ylamino)thiazole-4-carboxamide (cas: 1226056-71-8) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Reference of 1226056-71-8

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

Isolation and characterization of a highly virulent Edwardsiella piscicida strain responsible for mass mortality in marbled eel (Anguilla marmorata) cultured in Korea was written by Jung, Won Joon;Kwon, Jun;Giri, Sib Sankar;Kim, Sang Guen;Kim, Sang Wha;Kang, Jeong Woo;Lee, Sung Bin;Lee, Young Min;Oh, Woo Taek;Jun, Jin Woo;Park, Se Chang. And the article was included in Aquaculture in 2022.Product Details of 78110-38-0 This article mentions the following:

Edwardsiella infections have the potential to induce immense economic losses by affecting multiple fish species, and have been increasingly reported in aquaculture. Edwardsiella tarda, Edwardsiella hoshinae, and Edwardsiella ictaluri have all been previously associated with mass mortality. Recent technol. advances in bacterial identification have identified E. piscicida and E. anguillarum as important pathogens affecting global fisheries. Strains previously identified as E. tarda have been re-grouped based on new sequence data and phylogenetic studies. E. piscicida was classified as a novel species in 2012 and has since been reported to have caused mortality in diverse fish species in numerous countries that are potentially more threatening than the mortality caused by E. tarda. Eels are one of the most consumed fish species in Asia, and Anguilla japonica is a commonly reared species in fisheries. However, due to increasing global eel consumption, attempts to culture marbled eel (A. marmorata) have been recently carried out in many Asian countries including Korea. The external clin. signs of Edwardsiella piscicida- infected marbled eel (A. marmorata) were enlarged liver, hemorrhagic congestion at the base of fins and on the skin, as well as hemorrhagic ascites and multifocal abscesses were found in the liver. Histopathol. on E. piscicida- infected tissues revealed bacteremia, multifocal necrotizing hepatitis with vasculitis and splenitis with vasculitis. This study reports the first E. piscicida infection case responsible for mass mortality in A. marmorata cultured in Korea. Our study focused on the isolation and histopathol. characterization of this bacterial strain to better understand its damage on A. marmorata. In the experiment, the researchers used many compounds, for example, 2-((((Z)-1-(2-Aminothiazol-4-yl)-2-(((2S,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropanoic acid (cas: 78110-38-0Product Details of 78110-38-0).

2-((((Z)-1-(2-Aminothiazol-4-yl)-2-(((2S,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropanoic acid (cas: 78110-38-0) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Product Details of 78110-38-0

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

Emergence and evolution of unique plasmids harboring blaIMP-70 and blaCTX-M-253 in multidrug-resistant Providencia rettgeri was written by Watanabe, Mako;Nakano, Ryuichi;Tanouchi, Ayako;Nakano, Akiyo;Suzuki, Yuki;Saito, Kai;Sakata, Ryuji;Ogawa, Miho;Yano, Hisakazu. And the article was included in Microbiology Spectrum in 2022.HPLC of Formula: 78110-38-0 This article mentions the following:

Although the prevalence of carbapenem-resistant Enterobacterales remains low in Japan, these bacteria are a growing problem worldwide, owing to their multidrug resistance phenotype. We isolated a multidrug-resistant Providencia rettgeri strain, NR1418, harboring a rare blaIMP variant, blaIMP-70, a novel blaCTX-M variant, designated blaCTX-M-253, and blaMOX-1. This strain is resistant to 尾-lactams, amikacin, levofloxacin, and colistin. Genomic anal. revealed that NR1418 carries two plasmids, designated pNR1418-1 and pNR1418-2. The pNR1418-1 plasmid harbors blaCTX-M-253, blaTEM-1, and blaMOX-1, while the pNR1418-2 plasmid harbors blaIMP-70, which is located in a class 1 integron. Both plasmids exhibit high similarities with the plasmid of the P. rettgeri isolate BML2526, which also harbors blaIMP-70 and was identified in the same region of Japan as NR1418 at a different point in time. This indicates the possibility of the emergence and evolution of IMP-70-producing P. rettgeri and suggests that the plasmid of BML2526 may have occurred following recombination of the two plasmids harbored by NR1418. Further, blaIMP-70 and blaCTX-M-253 were found on unique plasmids, indicating that they likely evolved through mutations and recombination. In the experiment, the researchers used many compounds, for example, 2-((((Z)-1-(2-Aminothiazol-4-yl)-2-(((2S,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropanoic acid (cas: 78110-38-0HPLC of Formula: 78110-38-0).

2-((((Z)-1-(2-Aminothiazol-4-yl)-2-(((2S,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropanoic acid (cas: 78110-38-0) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.HPLC of Formula: 78110-38-0

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

Copper Acetate-Catalyzed, Mild, Highly Efficient, and Practical Synthesis of Thiazoles and Aminothiazoles was written by Meshram, H. M.;Kumar, D. Aravind;Vara Prasad, B. Ramalinga. And the article was included in Synthetic Communications in 2009.Application of 74370-93-7 This article mentions the following:

A mild and highly efficient synthesis of thiazoles by the condensation of 伪-bromo ketones with thiourea in the presence of a catalytic amount of copper acetate at room temperature has been described. The method is applicable for a variety of aryl and alkyl 伪-bromo ketones. The catalyst is inexpensive, and substituted thiazoles are obtained in good yields. In the experiment, the researchers used many compounds, for example, 4-(tert-Butyl)thiazol-2-amine (cas: 74370-93-7Application of 74370-93-7).

4-(tert-Butyl)thiazol-2-amine (cas: 74370-93-7) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Application of 74370-93-7

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

Comparative examination of compatibility of potassium canrenoate (Soldactone) at the clinical usage was written by Ozawa, Kazuo;Abe, Seiji;Nemoto, Akiko;Ito, Yoko;Satoh, Kazue;Yamamoto, Toshinori;Murayama, Jun-Ichiro. And the article was included in Iryo Yakugaku in 2002.Recommanded Product: (6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride This article mentions the following:

The authors examined the compatibility of a commercialized potassium canrenoate preparation (Soldactone) with 124 other kinds of currently prescribed injectable preparations as counter substances based upon the physicochem. parameters. The appearance, pH, and the concentration of canrenoate were used as markers after mixing for 24 h with other injectable preparations, since appearances can be deceptive. In order to estimate the remaining content of canrenoate after mixing, the concentrations of canrenoate were determined by UV absorption at the wavelength of 293 nm, using a spectrophotometer and reversed phase high-performance liquid chromatog. (HPLC). As the results, no change was detected in 53 of the 124 counter preparations in the mixture and the content of canrenoate was above 90%. Sixteen total parenteral nutrition solutions, 5 amino acid solutions and 17 antibiotics dissolved in saline were incompatible with canrenoate. We also examined the compatibility of canrenoate, which was directly added to furosemide (20 mg and 100 mg) and 5% of glucose preparations In the case of a furosemide injection (20mg), the appearance, pH and turbidity did not change, while the concentration of canrenoate decreased to less than 90% of the control. On the other hand, a glucose preparation (5%) did not show any incompatibility with the counter preparations Therefore, the canrenoate preparations can be dissolved into 5% glucose solution, prior to the clin. application. In the experiment, the researchers used many compounds, for example, (6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride (cas: 66309-69-1Recommanded Product: (6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride).

(6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride (cas: 66309-69-1) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). The nitrogen in thiazole is sp2 hybridized and the lone pair of electrons localized on the nitrogen is less reactive due to increased aromatic character and decreased basicity. It is protonated and alkylated/acylated at nitrogen forming hydrochloride and quaternary thiazolium salt.Recommanded Product: (6R,7R)-7-(2-(2-Aminothiazol-4-yl)acetamido)-3-(((1-(2-(dimethylamino)ethyl)-1H-tetrazol-5-yl)thio)methyl)-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid dihydrochloride

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

One-dimensional La(III) coordination polymer displaying multi-responsive luminescence activities towards Fe³⁺, acetone and benzothiozoles was written by Chen, Yuqian;Xian, Guoxuan;Yan, Hui;Wang, Yuhao;Li, Yunwu;Lu, Jing;Xu, Haijun;Tao, Jiayu;Wang, Suna. And the article was included in Journal of Solid State Chemistry in 2021.HPLC of Formula: 615-20-3 This article mentions the following:

Through reaction of La(NO₃)₃ with a flexible carboxylic acid ligand named 3,5-bis[(2-carboxyphenyl)oxy]benzoic acid (H₃L) under solvothermal condition, the complex with the formula of [La(L)(DMF)₂] (1) was obtained. One-dimensional chain of the complex was generated through the connection of binuclear units of La₂(COO)₄ across the flexible acid ligands. Luminescence results showed that different pollutants (Fe³⁺, acetone and benzothiophene organic compounds) could quench the luminescence of the blue emission of the complex in DMF with much low detection limit. Among several 2-substituted benzothiophene compounds, 2,2鈥?dithiobisbenzothiazole (DM) has a strongest binding constant of 10.8 x 10⁴ M^-1 and lowest detection limit of 0.332 渭M (0.110 ppm). All quenching effect was found within 15 s. The sensing mechanism was investigated through a series of experiments and theor. calculation Complex 1 could be employed as a multi-responsive chemosensor for detection of different pollutants with high sensitivity and fast response. In the experiment, the researchers used many compounds, for example, 2-Chlorobenzothiazole (cas: 615-20-3HPLC of Formula: 615-20-3).

2-Chlorobenzothiazole (cas: 615-20-3) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). Electrophilic attack at nitrogen depends on the presence of electron density at nitrogen as well as the position and nature of substituent linked to the thiazole ring.HPLC of Formula: 615-20-3

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

3,4,5-Trimethoxy Substitution on an N-DMBI Dopant with New N-Type Polymers: Polymer-Dopant Matching for Improved Conductivity-Seebeck Coefficient Relationship was written by Han, Jinfeng;Chiu, Arlene;Ganley, Connor;McGuiggan, Patty;Thon, Susanna M.;Clancy, Paulette;Katz, Howard E.. And the article was included in Angewandte Chemie, International Edition in 2021.Product Details of 3034-53-5 This article mentions the following:

Achieving high elec. conductivity and thermoelec. power factor simultaneously for n-type organic thermoelecs. is still challenging. By constructing 2 new acceptor-acceptor n-type conjugated polymers with different backbones and introducing the 3,4,5-trimethoxyphenyl group to form the new n-type dopant 1,3-dimethyl-2-(3,4,5-trimethoxyphenyl)-2,3-dihydro-1H-benzo[d]imidazole (TP-DMBI), high elec. conductivity of 11 S cm^-1 and power factor of 32渭W m^-1 K^-2 are achieved. Calculations using D. Functional Theory show that TP-DMBI presents a higher singly occupied MO (SOMO) energy level of -1.94 eV than that of the common dopant 4-(1, 3-dimethyl-2, 3-dihydro-1H-benzoimidazol-2-yl) Ph dimethylamine (N-DMBI) (-2.36 eV), which can result in a larger offset between the SOMO of dopant and LUMO (LUMO) of n-type polymers, though that effect may not be dominant. The doped polymer films exhibit higher Seebeck coefficient and power factor than films using N-DMBI at the same doping levels or similar elec. conductivity levels. Also, TP-DMBI doped polymer films offer much higher electron mobility of up to 0.53 cm² V^-1 s^-1 than films with N-DMBI doping, demonstrating the potential of TP-DMBI, and 3,4,5-trialkoxy DMBIs more broadly, for high performance n-type organic thermoelecs. In the experiment, the researchers used many compounds, for example, 2-Bromothiazole (cas: 3034-53-5Product Details of 3034-53-5).

2-Bromothiazole (cas: 3034-53-5) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. The pyridine-type nitrogen in the thiazole ring deactivates the ring for electrophilic substitution reactions, which is further reduced in acid due to protonation of the thiazole ring.Product Details of 3034-53-5

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

Plasmid-borne AFM alleles in Pseudomonas aeruginosa clinical isolates from China was written by Chen, Minhua;Cai, Heng;Li, Yue;Wang, Nanfei;Zhang, Piaopiao;Hua, Xiaoting;Yu, Yunsong;Sun, Renhua. And the article was included in Microbiology Spectrum in 2022.Related Products of 78110-38-0 This article mentions the following:

Carbapenem-resistant Pseudomonas aeruginosa (CRPA) is a pathogen of global concern due to the fact that therapeutic drugs are limited. Metallo-尾-lactamase (MBL)-producing P. aeruginosa has become a critical part of CRPA. Alcaligenes faecalis metallo-尾-lactamase (AFM) is a newly identified subclass B1b MBL. In this study, 487 P. aeruginosa strains isolated from patients and the environment in an intensive care unit were screened for AFM alleles. Five AFM-producing strains were identified, including four AFM-2-producing strains (ST262) and one AFM-4-producing strain (ST671). AFM-2-producing strains were isolated from rectal and throat swabs, and AFM-4-producing strains were isolated from the water sink. The blaAFM-₂ carrying plasmids belonged to the IncP-2 type, while the blaAFM-₄ carrying plasmid pAR19438 was a pSTY-like megaplasmid. Plasmid pAR19438 was acquired blaAFM-₄ by the integration of the Tn1403-like transposon. All blaAFM genes were embedded in an ISCR29-blaAFM unit core module flanked by class 1 integrons. The core module of blaAFM-₂ was ISCR29-螖groL-blaAFM-₂-bleMBL-螖trpF-螖ISCR, while the core module of blaAFM-₄ was ISCR29-螖groL-blaAFM-₂-bleMBL-螖trpF-ISCR-msrB-msrA-yfcG-corA-螖ISCR. The flanking sequences of ISCR29-blaAFM units also differed. The expression of AFM-2 and AFM-4 in DH5伪 and PAO1 illustrated the same effect for the evaluation of the MICs of 尾-lactams, except for aztreonam. Identification of AFM-4 underscores that the quick spread and emerging development of mutants of MBLs require continuous surveillance in P. aeruginosa. IMPORTANCE Acquiring metallo-p尾-lactamase genes is one of the important carbapenem resistance mechanisms of P. aeruginosa. Alcaligenes faecalis metallo-尾-lactamase is a newly identified metallo-尾-lactamase, the prevalence and genetic context of which need to be explored. In this study, we identified AFM-producing P. aeruginosa strains among clin. isolates and found a new mutant of AFM, AFM-4. The blaAFM-₄ carrying plasmid pAR19438 was a pSTY-like megaplasmid, unlike the plasmids encoding other blaAFM alleles. The genetic context of blaAFM-₄ was also different. However, AFM-2 and AFM-4 had the same impacts on antibiotic susceptibility. The presence and transmission of AFM alleles in P. aeruginosa pose a challenge to clin. practice. In the experiment, the researchers used many compounds, for example, 2-((((Z)-1-(2-Aminothiazol-4-yl)-2-(((2S,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropanoic acid (cas: 78110-38-0Related Products of 78110-38-0).

2-((((Z)-1-(2-Aminothiazol-4-yl)-2-(((2S,3S)-2-methyl-4-oxo-1-sulfoazetidin-3-yl)amino)-2-oxoethylidene)amino)oxy)-2-methylpropanoic acid (cas: 78110-38-0) belongs to thiazole derivatives. Thiazole rings are planar and aromatic. Thiazoles are characterized by larger pi-electron delocalization than the corresponding oxazoles and have therefore greater aromaticity. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Related Products of 78110-38-0

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

In silico study of naphtha [1, 2-d] thiazol-2-amine with adenosine A_2A receptor and its role in antagonism of haloperidol-induced motor impairments in mice was written by Luthra, Pratibha Mehta;Prakash, Amresh;Barodia, Sandeep Kumar;Kumari, Rita;Mishra, Chandra Bhushan;Kumar, J. B. Senthil. And the article was included in Neuroscience Letters in 2009.Safety of Naphtho[1,2-d]thiazol-2-amine This article mentions the following:

Loss of dopaminergic nigrostriatal neurons in the substantia nigra leads to Parkinson’s disease (PD). Adenosine A_2A receptors (A_2ARs) have been anticipated as novel therapeutic target for PD. A_2ARs potentiate locomotor behavior and are predominantly expressed in striatum. Naphtha [1, 2-d] thiazol-2-amine (NATA), a tricyclic thiazole have been studied as new anti-Parkinsonian compound AutoDock anal. and pharmacophore study of NATA with known A_2AR antagonists explicit its efficacy as a possible adenosine receptor antagonist. In vivo pharmacol. of NATA showed reduction of haloperidol (HAL)-induced motor impairments in Swiss albino male mice. Relatively elevated levels of dopamine in NATA pre-treated mice are suggestive of its possible role as neuromodulator in PD. In the experiment, the researchers used many compounds, for example, Naphtho[1,2-d]thiazol-2-amine (cas: 40172-65-4Safety of Naphtho[1,2-d]thiazol-2-amine).

Naphtho[1,2-d]thiazol-2-amine (cas: 40172-65-4) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Safety of Naphtho[1,2-d]thiazol-2-amine

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

Thiazolylalkylamines: synthesis of congeners of imidazolylethylamines and their effects on gastric secretion was written by Vitali, T.;Impicciatore, M.;Plazzi, P. V.;Bordi, F.;Morini, G.. And the article was included in Farmaco, Edizione Scientifica in 1986.Electric Literature of C5H8N2OS This article mentions the following:

Eight 2-aminothiazolylethylamines (I, R = NH₂, NHMe, or NMe₂; R¹ and R² = H, Me; X = Y = N, S), as well as 4 related compounds unsaturated in the ring or side chain, were prepared by 3 different reaction sequences, for which the mechanisms are illustrated. Since these compounds contain the S-aminoalkylisothiourea group which, in other instances stimulates gastric secretion, they were tested for histaminic-H₂ agonist activity in vitro (isolated guinea pig fundus) and in vivo (gastric acid secretion in the cat) and for some other activities. Examination of structure-activity relations excluded the possibility that the juxtanuclear NH₂ group of the compounds interacts with the H₂ receptor; the 2-aminothiazole moiety is not pharmacol. equivalent to the 2-aminoimidazole or isothiourea groups. This strengthens the hypothesis that the flexibility of the mol. is a fundamental requirement for the H₂-stimulant properties of S-(3-dimethylaminopropyl)isothiourea and that the different behavior of 2-aminohistamine relative to 2-methylhistamine is due to the existence of a hydrophilic area in the histaminic-H₂ receptor which is capable of accepting the juxtanuclear NH₂ group of the former. In the experiment, the researchers used many compounds, for example, 2-Amino-5-(2-hydroxyethyl)thiazole (cas: 105773-93-1Electric Literature of C5H8N2OS).

2-Amino-5-(2-hydroxyethyl)thiazole (cas: 105773-93-1) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, 蟺-excessive heteroaromatic containing one sulfur atom and one pyridine-type nitrogen atom at position 3 of the cyclic ring system. Thiazole is a versatile building block for the construction and lead generation of new drug discoveries. Numerous diazole-based compounds are in clinical use as anticancer, antileukemic, antiinflammatory, antiviral, antifungal, antirheumatic, immunomodulator, and antiparasitic agents.Electric Literature of C5H8N2OS

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