Day: February 22, 2023

Effects of certain purified Chinese herbal medicinal compound polysaccharide on cellular immunity and humoral immunity in chicken was written by Shang, Yun-xia;Zhu, Xiao-qing;Gu, Xin-li;Li, Xiao-zhen;Qiao, Hai-bo;Jia, Shu-hong;Zhang, Dong-sheng. And the article was included in Zhongguo Xumu Shouyi in 2015.Safety of (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole hydrochloride This article mentions the following:

In order to select the best dose of certain purified Chinese herbal medicinal compound polysaccharide (cCHMPS), which had been proven to significantly affect the immunity of mice, three hundred one-day-old male Liangfeng Green-feet Ma chickens were randomly divided into six groups, namely control group, levamisole hydrochloride (LM) group, Astragalus polysaccharide (APS) group, high, medium and low-dose purified cCHMPS group, and with 50 chickens for each group. Eight-day-old chickens were vaccined with physiol. saline, LM, APS, high, medium and low-dose purified cCHMPS, once a day for 7 consecutive days. On days 8, 14, 21, 28, 35 and 42 after the first vaccination, 5 chickens’ blood for each group were sampled for determination of T, B lymphocyte proliferation activities and NDV antibody levels. The results showed that APS and purified cCHMPS at different doses could significantly or extremely significantly promote the proliferation of peripheral T, B lymphocytes (P<0.05; P<0.01), increase the concentrations of NDV antibody, enhance cellular immunity and humoral immunity, and the medium-dose purified cCHMPS was the best. In the experiment, the researchers used many compounds, for example, (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole hydrochloride (cas: 16595-80-5Safety of (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole hydrochloride).

(S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole hydrochloride (cas: 16595-80-5) 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 sulfonation occurs only under forcing conditions: the action of oleum at 250 °C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Safety of (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole hydrochloride

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

Determination of the main metabolite (desethyl KBT-3022) of a new antiplatelet agent, KBT-3022, in plasma by gas chromatography was written by Nakada, Yuichiro;Shimada, Hitoshi;Awata, Norio. And the article was included in Yakugaku Zasshi in 1992.Application In Synthesis of Ethyl 2-(2-(4,5-bis(4-methoxyphenyl)thiazol-2-yl)-1H-pyrrol-1-yl)acetate This article mentions the following:

A highly sensitive, accurate and reproducible gas chromatog. method for the determination of a main metabolite, 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl] pyrrolyl acetic acid (desethyl KBT-3022) of a new antiplatelet agent, Et 2-[4,5-bis(4-methoxyphenyl)thiazol-2-yl]pyrrol-1-yl acetate (KBT-3022), in human or dog plasma has been developed. Desethyl KBT-3022 in plasma was extracted with a mixture of n-hexane and dichloromethane (1:1) and was derivatized with pentafluorobenzyl bromide. The obtained pentafluorobenzyl derivative of desethyl KBT-3022 in plasma was separated by HPLC. After the separation, the pentafluorobenzyl derivative of desethyl KBT-3022 was detected by gas chromatog. Gas chromatog. was performed with an Ultra 1 column (12 m × 0.22 mm i.d., film thickness 0.33 μm), using an electron capture detector. 2-[2-{4,5-Bis(4-methoxyphenyl)thiazol-2-yl}pyrrol-1-yl]propionic acid was used as internal standard The detection limit of desethyl KBT-3022 in plasma was 0.2 ng/mL. The coefficients of variation were <5.3%. This method was applied to th determination of the plasma concentration of desethyl KBT-3022 after oral administration of KBT-3022 to dogs. In the experiment, the researchers used many compounds, for example, Ethyl 2-(2-(4,5-bis(4-methoxyphenyl)thiazol-2-yl)-1H-pyrrol-1-yl)acetate (cas: 101001-34-7Application In Synthesis of Ethyl 2-(2-(4,5-bis(4-methoxyphenyl)thiazol-2-yl)-1H-pyrrol-1-yl)acetate).

Ethyl 2-(2-(4,5-bis(4-methoxyphenyl)thiazol-2-yl)-1H-pyrrol-1-yl)acetate (cas: 101001-34-7) 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.Application In Synthesis of Ethyl 2-(2-(4,5-bis(4-methoxyphenyl)thiazol-2-yl)-1H-pyrrol-1-yl)acetate

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

Synthesis and Evaluation of Three ¹⁸F-Labeled Aminophenylbenzothiazoles as Amyloid Imaging Agents was written by Serdons, Kim;Van Laere, Koen;Janssen, Peter;Kung, Hank F.;Bormans, Guy;Verbruggen, Alfons. And the article was included in Journal of Medicinal Chemistry in 2009.Synthetic Route of C7H4N2O2S This article mentions the following:

Three ¹⁸F-labeled fluorophenylbenzothiazoleamines I (R = H₂N, MeNH, Me₂N; R¹ = ¹⁸F) are prepared which display high in vitro binding affinity for human amyloid β plaques (K_i ≤ 10 nM). I (R¹ = ¹⁸F) are prepared by aromatic nucleophilic substitution of I [R = BocNH, BocN(Me), Me₂N; R¹ = O₂N; Boc = tert-butoxycarbonyl] with ¹⁸F-fluoride, followed by deprotection of the Boc group if required; preparation by other methods, for example cyclocondensation of diaminobenzenethiols with benzoic acids, is unsuccessful. Determination of the octanol/water partition coefficient, biodistribution studies in mice, and in vivo μPET studies in rats and a rhesus monkey show that initial brain uptake is high and brain washout is fast in normal animals. Radiometabolites are quantified in plasma and brain of mice and in monkey plasma using HPLC. Of the tested compounds, I (R = H₂N; R¹ = ¹⁸F) shows the most favorable brain kinetics in mice, rats, and a monkey; its polar plasma radiometabolites do not cross the blood-brain barrier. Preliminary results strongly suggest that I (R = H₂N; R¹ = ¹⁸F) is a promising candidate as a PET brain amyloid imaging agent. In the experiment, the researchers used many compounds, for example, 6-Nitrobenzothiazole (cas: 2942-06-5Synthetic Route of C7H4N2O2S).

6-Nitrobenzothiazole (cas: 2942-06-5) belongs to thiazole derivatives. Thiazoles in peptides or their ability to bind proteins, DNA and RNA has led to many synthetic studies and new applications. 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.Synthetic Route of C7H4N2O2S

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

Delayed re-endothelialization with rapamycin-coated stents is rescued by the addition of a glycogen synthase kinase-3β inhibitor was written by Ma, Xiaoli;Hibbert, Benjamin;Dhaliwal, Bharbhoor;Seibert, Tara;Chen, Yong-Xiang;Zhao, Xiaoling;O’Brien, Edward R.. And the article was included in Cardiovascular Research in 2010.COA of Formula: C12H12N4O4S This article mentions the following:

Aims: Drug-eluting stents (DESs) reduce neointima area and in-stent restenosis but delay re-endothelialization. Recently, we demonstrated that pharmacol. expansion and functional enhancement of endothelial progenitor cells (EPCs) can be achieved by treatment with a glycogen synthase kinase-3β inhibitor (GSKi)-even for feeble cells derived from coronary artery disease patients. GSKi treatment enhanced EPC adhesion via up-regulated expression of the α-4 integrin, ameliorated re-endothelialization, and reduced neointima formation in denuded murine arteries. Hence, we hypothesized that GSKi-coated stents (GSs) will enhance EPC adhesion and attenuate delayed vascular healing associated with rapamycin, a key DES agent. Methods and results: In vitro human EPCs adhered to GS with affinities that were 2×, 14×, and 13× greater than vehicle (VSs)-, rapamycin (RSs)-, and rapamycin plus GSKi (RGSs)-coated stents, resp. Stents were inserted in rabbit carotid arteries, and at 14 days, neointima area was 45 and 49% lower in GSs compared with bare metal stents (BMSs) and VSs. Moreover, RSs had a 47% larger neointima area than GSs, but RGSs reduced neointima area to a level comparable to GSs. Seven days after stenting, GSs displayed re-endothelialization that was 40, 33, and 42% greater than BMSs, VSs, and RSs, resp. Moreover, RGSs had 41% more re-endothelialization than RSs. At 14 days, the 7-day re-endothelialization patterns persisted. Conclusion: GSKi efficiently ameliorates the vascular response to stent implantation and has an important redeeming effect on the deleterious endothelial effects of rapamycin-coated stents. In the experiment, the researchers used many compounds, for example, 1-(4-Methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea (cas: 487021-52-3COA of Formula: C12H12N4O4S).

1-(4-Methoxybenzyl)-3-(5-nitrothiazol-2-yl)urea (cas: 487021-52-3) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. 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.COA of Formula: C12H12N4O4S

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

Peptides. XXI. Dehydrogenation of some thiazolines derived from cysteine was written by Barton, Moira A.;Kenner, G. W.;Sheppard, R. C.. And the article was included in Journal of the Chemical Society [Section] C: Organic in 1966.Name: Methyl 2-methyl-4,5-dihydrothiazole-4-carboxylate This article mentions the following:

Esters of 2-alkyl-Δ²-thiazoline-4-carboxylic acids are smoothly dehydrogenated by phenantraquinone to the corresponding thiazole derivatives Me 2-benzamidomethyl-Δ²-thiazoline-4-carboxylate is dehydrogenated only slowly by phenenthraquinone but rapidly by MnO₂. The possible application of these reactions to the detection of thiazoline rings in peptides is discussed. In the experiment, the researchers used many compounds, for example, Methyl 2-methyl-4,5-dihydrothiazole-4-carboxylate (cas: 6436-58-4Name: Methyl 2-methyl-4,5-dihydrothiazole-4-carboxylate).

Methyl 2-methyl-4,5-dihydrothiazole-4-carboxylate (cas: 6436-58-4) belongs to thiazole derivatives. The thiazole ring has been identified as a central feature of numerous natural products, perhaps the most famous example of which is epothilone. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Name: Methyl 2-methyl-4,5-dihydrothiazole-4-carboxylate

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

The opposite and amplifying effect of B ← N coordination on photophysical properties of regioisomers with an unsymmetrical backbone was written by Zeng, Chao;Yuan, Kang;Wang, Nan;Peng, Tai;Wu, Gang;Wang, Suning. And the article was included in Chemical Science in 2019.Name: 2-Bromothiazole This article mentions the following:

1,3-Dipolar cycloaddition of pyrido[2,1-a]isoindole with internal alkynes functionalized by a BMes₂ph and an N-aromatic heterocycle leads to the formation of two types of regioisomers (major a and minor b) that have distinct phys. and photophys. properties. Examination on 5 pairs of regioisomers unveils that the major isomers consistently have a smaller optical energy gap and emission energy than the corresponding minor isomers, which is greatly amplified by the formation of an internal B ← N bond. The regioisomers with a B ← N bond display contrasting temperature-dependent structural dynamics and response to fluoride ions, owing to an entropy-driven or fluoride initiated B ← N bond rupture/ring-opening process and the different B ← N bond strength. The opposite inductive effect and the Lewis pair properties of the dichotomic substituent units are responsible for the contrasting properties of the regioisomers in this system. In the experiment, the researchers used many compounds, for example, 2-Bromothiazole (cas: 3034-53-5Name: 2-Bromothiazole).

2-Bromothiazole (cas: 3034-53-5) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. 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.Name: 2-Bromothiazole

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

Synthesis of the (benzothiazolylthio)carboxylic acids by use of ultrasound irradiation in phase transfer catalysis medium was written by Li, Yingjun;Li, Lina;Sun, Shuqin;Hu, Zhijun;Song, Yongbo. And the article was included in Hebei Shifan Daxue Xuebao, Ziran Kexueban in 2011.Synthetic Route of C9H7NO2S2 This article mentions the following:

(Benzothiazolylthio)carboxylic acids, (2-benzothiazolylthio)acetic acid and 3-(2-benzothiazolylthio)propionic acid were synthesized by the technique of ultrasonic irradiation and phase transfer catalysis. Their structures were confirmed by IR, ¹HNMR and ¹³CNMR. The influences of the reaction temperature, the reaction time, the solvent, the catalyst and the ultrasonic irradiation on the reaction were investigated and optimum exptl. conditions were found. Compared with the literature methods, this synthetic method had such advantages as mild condition, simple operation, short reaction time, lower reaction temperature and higher yield. In the experiment, the researchers used many compounds, for example, 2-(Benzo[d]thiazol-2-ylthio)acetic acid (cas: 6295-57-4Synthetic Route of C9H7NO2S2).

2-(Benzo[d]thiazol-2-ylthio)acetic acid (cas: 6295-57-4) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. 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.Synthetic Route of C9H7NO2S2

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

Catalyst and additive-free regioselective oxidative C-H thio/selenocyanation of arenes and heteroarenes with elemental sulfur/selenium and TMSCN was written by Feng, Chengtao;Peng, Ya;Ding, Guangrong;Li, Xiangxiao;Cui, Chang;Yan, Yizhe. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2018.Recommanded Product: 15864-32-1 This article mentions the following:

A regioselective oxidative C-H thio/selenocyanation of arenes and heteroarenes with TMSCN and elemental sulfur/selenium was demonstrated under catalyst-free and additive-free conditions. DMSO (DMSO) was employed as the mild oxidant as well as the solvent. The reaction was operationally simple and scalable with a broad substrate scope. Compared to previous reports, this protocol was distinguished by avoiding the use of any catalyst or additive, the novel SCN/SeCN source, the different reaction mechanism and gram-scale synthesis. In the experiment, the researchers used many compounds, for example, 2-Amino-6-bromobenzothiazole (cas: 15864-32-1Recommanded Product: 15864-32-1).

2-Amino-6-bromobenzothiazole (cas: 15864-32-1) 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: 15864-32-1

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

A pharmacologic activator of endothelial KCa channels increases systemic conductance and reduces arterial pressure in an anesthetized pig model was written by Mishra, Ramesh C.;Mitchell, Jamie R.;Gibbons-Kroeker, Carol;Wulff, Heike;Belenkie, Israel;Tyberg, John V.;Braun, Andrew P.. And the article was included in Vascular Pharmacology in 2016.Safety of Naphtho[1,2-d]thiazol-2-amine This article mentions the following:

SKA-31, an activator of endothelial KCa2.3 and KCa3.1 channels, reduces systemic blood pressure in mice and dogs, however, its effects in larger mammals are not well known. We therefore examined the hemodynamic effects of SKA-31, along with sodium nitroprusside (SNP), in anesthetized, juvenile male domestic pigs. Exptl., continuous measurements of left ventricular (LV), aortic and inferior vena cava (IVC) pressures, along with flows in the ascending aorta, carotid artery, left anterior descending coronary artery and renal artery, were performed during acute administration of SKA-31 (0.1, 0.3, 1.0, 3.0 and 5.0 mg/mL/kg) and a single dose of SNP (5.0 μg/mL/kg). SKA-31 dose-dependently reduced mean aortic pressure (mP_AO), with the highest dose decreasing mP_AO to a similar extent as SNP (- 23 ± 3 and – 28 ± 4 mm Hg, resp.). IVC pressure did not change. Systemic conductance and conductance in coronary and carotid arteries increased in response to SKA-31 and SNP, but renal artery conductance was unaffected. There was no change in either LV stroke volume (SV) or heart rate (vs. the preceding control) for any infusion. With no change in SV, drug-evoked decreases in LV stroke work (SW) were attributed to reductions in mP_AO (SW vs. mP_AO, r² = 0.82, P < 0.001). In summary, SKA-31 dose-dependently reduced mP_AO by increasing systemic and arterial conductances. Primary reductions in mP_AO by SKA-31 largely account for associated decreases in SW, implying that SKA-31 does not directly impair cardiac contractility. 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. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. 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.Safety of Naphtho[1,2-d]thiazol-2-amine

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