Category: thiazole

Performance of the reveal rapid antibiotic susceptibility testing system on gram-negative blood cultures at a large urban hospital was written by Tibbetts, Robert;George, Sheeja;Burwell, Reece;Rajeev, Lara;Rhodes, Paul A.;Singh, Pragya;Samuel, Linoj. And the article was included in Journal of Clinical Microbiology in 2022.Category: thiazole This article mentions the following:

Timely and effective antibiotic treatment is vital for sepsis, with increasing incidence of antimicrobial-resistant bacteremia driving interest in rapid phenotypic susceptibility testing. To enable the widespread adoption needed to make an impact, antibiotic susceptibility testing (AST) systems need to be accurate, enable rapid intervention, have a broad antimicrobial menu and be easy to use and affordable. We evaluated the Specific Reveal (Specific Diagnostics, San Jose, CA) rapid AST system on pos. blood cultures with Gram-neg. organisms in a relatively resistant population in a large urban hospital to assess its potential for routine clin. use. One hundred four randomly selected pos. blood cultures (Virtuo; bioMorieux) were Gram stained, diluted 1:1,000 in Pluronic water, inoculated into 96-well antibiotic plates, sealed with the Reveal sensor panel, and placed in the Reveal instrument for incubation and reading. The MIC and susceptible/intermediate/resistant category was determined and compared to results from Vitek 2 (bioMorieux) for the 17 antimicrobials available and to Sensititre (Thermo Fisher) for 24 antimicrobials. Performance was also assessed with contrived blood cultures with 33 highly resistant strains. Reveal was in 98.0% essential agreement (EA) and 96.3% categorical agreement (CA) with Sensititre, with just 1.3% very major error (VME) and 97.0%/96.2%/1.3% EA/CA/VME vs. Vitek 2. Reveal results for contrived highly resistant strains were equivalent, with EA/CA/VME of 97.7%/95.2%/1.0% with CDC/FDA Antibiotic Resistance Isolate Bank references Average time to result (TTR) for Reveal was 4.6 h. Sample preparation was relatively low skill and averaged 3 min. We conclude that the Reveal system enables accurate and rapid susceptibility testing of Gram-neg. blood cultures. 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: 78110-38-0Category: thiazole).

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. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at 未 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. There are numerous natural products that possess a thiazole ring with broad pharmacological activities. Thiamine, also known as vitamin B1, possesses a thiazole ring linked with 2-methylpyrimidine-4-amine as hydrochloride salt.Category: thiazole

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

Schmidt reaction in ionic liquids: highly efficient and selective conversion of aromatic and heteroaromatic aldehydes to nitriles with [BMIM(SO₃H)][OTf] as catalyst and [BMIM][PF₆] as solvent was written by Nandi, Ganesh C.;Laali, Kenneth K.. And the article was included in Tetrahedron Letters in 2013.Name: 2-Cyanothiazole This article mentions the following:

A mild and selective method is presented for the conversion of aromatic and heteroaromatic aldehydes to nitriles via the Schmidt reaction with TMSN₃ by using [BMIM(SO₃H)][OTf] as catalyst and [BMIM][PF₆] as solvent. E.g., in the presence of this catalyst in [BMIM][PF₆], reaction of 2-MeOC₆H₄CHO with TMSN₃ gave 100% 2-MeOC₆H₄CN. The method offers high yields and simple product isolation, and avoids the use of liquid superacids or corrosive Lewis acids commonly employed for this transformation. It also offers some potential for recycling/reuse of the IL solvent. In the experiment, the researchers used many compounds, for example, 2-Cyanothiazole (cas: 1452-16-0Name: 2-Cyanothiazole).

2-Cyanothiazole (cas: 1452-16-0) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at 未 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Thiazole sulfonation occurs only under forcing conditions: the action of oleum at 250 掳C for 3 hours in the presence of mercury(II) sulfate leads to 65% formation of 5-thiazole sulfonic acid.Name: 2-Cyanothiazole

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

Dopamine receptor mediated antidepressant action of B-HT 920 in mice was written by Sharma, Alok;Kulkarni, S K.. And the article was included in Indian Journal of Experimental Biology in 1994.Reference of 36085-73-1 This article mentions the following:

Possible involvement of dopaminergic (DAergic) system in forced swimming-induced immobility (despair behavior) was investigated in mice. B-HT 920 (0.05 and 0.1 mg/kg), a post-synaptic DAergic agonist, produced a dose dependent reduction in immobility period, which was sensitive to blockade by haloperidol (0.5 mg/kg) and sulpiride (100 mg/kg). This effect was also blocked by 伪₂ antagonist yohimbine (5 mg/kg). SKF 38393 (5 mg/kg), a D₁-DA agonist potentiated the action of B-HT 920. Reserpinization (2 mg/kg, 24 h prior) produced despair immobility in mice. When a low dose of B-HT 920 (0.05 mg/kg) was given to reserpinized animals, the duration of immobility period was further increased. But on the other hand, a higher dose (0.1 mg/kg) of it reduced reserpine-induced immobility. Desipramine (5 and 10 mg/kg), elicited a dose dependent reduction in the immobility period, which was sensitive to blockade by sulpiride (100 mg/kg). Desipramine (10 mg/kg) showed a biphasic response in combination with B-HT 920, i.e., a potentiation of the response due to a low dose of B-HT 920 (0.05 mg/kg) and an antagonism of the response due to a higher dose of B-HT 920 (0.1 mg/kg), resp. SKF 38393 (5 mg/kg), potentiated the action of desipramine (5 mg/kg). SKF 38393 (5 mg/kg) further potentiated the action of desipramine (5 mg/kg) and B-HT 920 (0.05 mg/kg). These observations suggests that B-HT 920 reduces behavioral immobility by DAergic mechanism and desipramine also modulates D₂-DA receptors in its anti-depressant action. In the experiment, the researchers used many compounds, for example, 6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1Reference of 36085-73-1).

6-Allyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepin-2-amine dihydrochloride (cas: 36085-73-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Reference of 36085-73-1

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

Nickel-catalysed direct alkylation of thiophenes via double C(sp³)-H/C(sp²)-H bond cleavage: the importance of KH₂PO₄ was written by Wang, Xie;Xie, Peipei;Qiu, Renhua;Zhu, Longzhi;Liu, Ting;Li, You;Iwasaki, Takanori;Au, Chak-Tong;Xu, Xinhua;Xia, Yuanzhi;Yin, Shuang-Feng;Kambe, Nobuaki. And the article was included in Chemical Communications (Cambridge, United Kingdom) in 2017.Product Details of 3034-53-5 This article mentions the following:

The efficient Ni-catalyzed oxidative C(sp³)-H/C(sp²)-H cross-dehydrogenative coupling reaction was developed for synthesis of highly functionalized alkyl (aryl)-substituted thiophenes such as I [R¹ = Me, Et, Ph; R² = Me, Ph, Bn, 2-naphthyl; R¹ = R² = Me, Ph; R¹R² = (CH₂)₅, Ph, 2-H₃CC₆H₄; R³ = 2-thienyl, benzothien-2-yl, 4-Br-2-thienyl, etc.] from thiophenes and aliphatic (aromatic) amides that contain an 8-aminoquinoline as a removable directing group in the presence of a silver oxidant. The approach enabled the facile one-step synthesis of substituted thiophenes I with high functional group compatibility via double C(sp³)-H/C(sp²)-H bond cleavage without affecting C-Br and C-I bonds and formation of C(alkyl)-C(heteroaryl) bonds. DFT calculations verified the importance of KH₂PO₄ as an additive for promoting C-H bond cleavage and supported the involvement of a Ni(III) species for efficient C(sp²)-H cleavage and C-C coupling. 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. 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.Product Details of 3034-53-5

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

Synthesis and in vitro antileishmanial activity of 5-substituted-2′-deoxyuridine derivatives was written by Peyron, Corinne;Benhida, Rachid;Bories, Christian;Loiseau, Philippe M.. And the article was included in Bioorganic Chemistry in 2005.Category: thiazole This article mentions the following:

We report herein the synthesis and the in vitro antileishmanial evaluation of 5-substituted-2′-deoxyuridine nucleosides. The most active compound against Leishmania donovani promastigotes was Thia-dU (3a) with an IC₅₀ = 3 渭M. This compound exhibited the same activity as zidovudine (3′-azido-2′-deoxythymidine) used as nucleoside reference compound Considering the cytotoxicity of synthetic compounds on peritoneal murine macrophages, the most toxic compound was MeThio-dU (3d) with a MTC at 10 渭M. Only Methia-dU (3b) was active against intra-macrophagic amastigotes with an IC₅₀ = 6.5 渭M. This latter can now be evaluated in vivo, for further investigations through structure-based drug design. In the experiment, the researchers used many compounds, for example, 2-(Tributylstannyl)thiazole (cas: 121359-48-6Category: thiazole).

2-(Tributylstannyl)thiazole (cas: 121359-48-6) 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.Category: thiazole

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

Discovery of highly potent, selective, orally bioavailable, metabotropic glutamate subtype 5 (mGlu5) receptor antagonists devoid of cytochrome P450 1A2 inhibitory activity was written by Smith, Nicholas D.;Poon, Steve F.;Huang, Dehua;Green, Mitchell;King, Christopher;Tehrani, Lida;Roppe, Jeffrey R.;Chung, Janice;Chapman, Deborah P.;Cramer, Merryl;Cosford, Nicholas D. P.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2004.Recommanded Product: 3364-80-5 This article mentions the following:

Structure-activity relationship studies focused on bio-isosteric replacements of 2-pyridyl resulted in mGlu5 receptor antagonists with reduced inhibition of cytochrome P 450 1A2. This led to highly potent, selective and orally bioavailable 2-imidazolyl tetrazoles such as I that are devoid of cytochrome P 450 inhibitory activity. In the experiment, the researchers used many compounds, for example, Thiazole-4-carbaldehyde (cas: 3364-80-5Recommanded Product: 3364-80-5).

Thiazole-4-carbaldehyde (cas: 3364-80-5) 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.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Recommanded Product: 3364-80-5

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

Direct C-H Bond Activation of Benzoxazole and Benzothiazole with Aryl Bromides Catalyzed by Palladium(II)-N-heterocyclic Carbene Complexes was written by Kaloglu, Murat;Kaloglur, Nazan;Oezdemir, Ismail. And the article was included in Chinese Journal of Chemistry in 2018.Computed Properties of C14H11NS This article mentions the following:

Herein, a series of novel palladium(II)-NHC complexes (NHC=N-heterocyclic carbene) were synthesized. The structures of all novel complexes were characterized by ¹H NMR, ¹³C NMR, FT-IR spectroscopy and elemental anal. techniques. These palladium(II)-NHC complexes were tested as efficient catalysts in the direct C-H bond activation of benzoxazole and benzothiazole with aryl bromides in the presence of 1 mol% catalyst loading at 150 掳C for 4 h. Under the given conditions, various aryl bromides were successfully applied as the arylating reagents to achieve the 2-arylbenzoxazoles and 2-arylbenzothiazoles in acceptable to high yields. In the experiment, the researchers used many compounds, for example, 2-(4-Methylphenyl)benzothiazole (cas: 16112-21-3Computed Properties of C14H11NS).

2-(4-Methylphenyl)benzothiazole (cas: 16112-21-3) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at 未 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. 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.Computed Properties of C14H11NS

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

Synthesis of N-Substituted Methyl 4H-Thieno[3,2-b]pyrrole-5-carboxylates was written by Torosyan, S. A.;Gimalova, F. A.;Zagitov, V. V.;Erastov, A. S.;Miftakhov, M. S.. And the article was included in Russian Journal of Organic Chemistry in 2018.Formula: C8H7NO2S This article mentions the following:

The alkylation of Me 4H-thieno[3,2-b]pyrrole-5-carboxylate with Me iodide and allyl, propargyl and benzyl bromides in the presence of sodium hydride in THF afforded the corresponding N-substituted derivatives I (R = Me, CH₂=CHCH₂, CH鈮CH₂, Bn). Some reactions of the alkylation products were studied. In the experiment, the researchers used many compounds, for example, Methyl 4H-thieno[3,2-b]pyrrole-5-carboxylate (cas: 82782-85-2Formula: C8H7NO2S).

Methyl 4H-thieno[3,2-b]pyrrole-5-carboxylate (cas: 82782-85-2) 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.Formula: C8H7NO2S

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

Genomic landscape of drug response reveals mediators of anthelmintic resistance was written by Doyle, Stephen R.;Laing, Roz;Bartley, David;Morrison, Alison;Holroyd, Nancy;Maitland, Kirsty;Antonopoulos, Alistair;Chaudhry, Umer;Flis, Ilona;Howell, Sue;McIntyre, Jennifer;Gilleard, John S.;Tait, Andy;Mable, Barbara;Kaplan, Ray;Sargison, Neil;Britton, Collette;Berriman, Matthew;Devaney, Eileen;Cotton, James A.. And the article was included in Cell Reports in 2022.Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole This article mentions the following:

Like other pathogens, parasitic helminths can rapidly evolve resistance to drug treatment. Understanding the genetic basis of anthelmintic drug resistance in parasitic nematodes is key to tracking its spread and improving the efficacy and sustainability of parasite control. Here, we use an in vivo genetic cross between drug-susceptible and multi-drug-resistant strains of Haemonchus contortus in a natural host-parasite system to simultaneously map resistance loci for the three major classes of anthelmintics. This approach identifies new alleles for resistance to benzimidazoles and levamisole and implicates the transcription factor cky-1 in ivermectin resistance. This gene is within a locus under selection in ivermectin-resistant populations worldwide; expression analyses and functional validation using knockdown experiments support that cky-1 is associated with ivermectin survival. Our work demonstrates the feasibility of high-resolution forward genetics in a parasitic nematode and identifies variants for the development of mol. diagnostics to combat drug resistance in the field. In the experiment, the researchers used many compounds, for example, (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole).

(S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole (cas: 14769-73-4) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). 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.Recommanded Product: (S)-6-Phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole

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

Lack of Detection of the Analgesic Properties of PF-05089771, a Selective Na_v1.7 Inhibitor, Using a Battery of Pain Models in Healthy Subjects was written by Siebenga, Pieter;van Amerongen, Guido;Hay, Justin L.;McDonnell, Aoibhinn;Gorman, Donal;Butt, Richard;Groeneveld, Geert Jan. And the article was included in Clinical and Translational Science in 2020.Computed Properties of C18H12Cl2FN5O3S2 This article mentions the following:

The aim was to demonstrate analgesic properties of a potent selective Na_v1.7 sodium channel blocker, PF-05089771, alone and concomitantly with pregabalin in healthy subjects using a battery of human evoked pain models. This was a double-blind, double-dummy, randomized, placebo-controlled, five-period cross-over study with PF-05089771 alone and PF-05089771 concomitantly with pregabalin as treatment arms with pregabalin, ibuprofen, and placebo as control arms (NCT02349607). A battery of human evoked pain models was used to investigate analgesic properties of PF-05089771. Twenty-five subjects were enrolled in the study of which 23 subjects completed all five periods. PF-05089771 alone did not differ from placebo on the primary pain end points. The same holds when comparing PF-05089771 concomitantly with pregabalin and pregabalin alone. Pregabalin showed significant effects relative to placebo on thermal pain on the normal skin and UVB skin (least squares means with 90% confidence interval: 0.63 (0.32-0.93) and 0.53 (0.11-0.96)), pressure stimulation (1.10 (1.04-1.18)), and cold pressor (1.22 (1.14-1.32)). Ibuprofen demonstrated significant effects on thermal pain UVB skin (1.26 (0.82-1.70)) and pressure stimulation assessment (1.08 (1.01-1.15)), consistent with historical results. This study did not demonstrate analgesic properties of PF-05089771 alone or concomitantly with pregabalin in a battery of pain models. In the experiment, the researchers used many compounds, for example, 4-(2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide (cas: 1235403-62-9Computed Properties of C18H12Cl2FN5O3S2).

4-(2-(3-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy)-5-chloro-2-fluoro-N-(thiazol-4-yl)benzenesulfonamide (cas: 1235403-62-9) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1).Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.Computed Properties of C18H12Cl2FN5O3S2

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