Category: 3034-22-8

In 2004,Helal, Christopher J.; Sanner, Mark A.; Cooper, Christopher B.; Gant, Thomas; Adam, Mavis; Lucas, John C.; Kang, Zhijun; Kupchinsky, Stanley; Ahlijanian, Michael K.; Tate, Bonnie; Menniti, Frank S.; Kelly, Kristin; Peterson, Marcia published 《Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease》.Bioorganic & Medicinal Chemistry Letters published the findings.Related Products of 3034-22-8 The information in the text is summarized as follows:

High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide. This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320 nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved. In the experimental materials used by the author, we found 5-Bromothiazol-2-amine(cas: 3034-22-8Related Products of 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) 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.Related Products of 3034-22-8

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

In 2010,Sidduri, Achyutharao; Grimsby, Joseph S.; Corbett, Wendy L.; Sarabu, Ramakanth; Grippo, Joseph F.; Lou, Jianping; Kester, Robert F.; Dvorozniak, Mark; Marcus, Linda; Spence, Cheryl; Racha, Jagdish K.; Moore, David J. published 《2,3-Disubstituted acrylamides as potent glucokinase activators》.Bioorganic & Medicinal Chemistry Letters published the findings.HPLC of Formula: 3034-22-8 The information in the text is summarized as follows:

The phenylacetamide 1 represents the archtypical glucokinase activator (GKA) in which only the R-isomer is active. In order to probe whether the chiral center could be replaced, we prepared a series of olefins 2 and show in the present work that these compounds represent a new class of GKAs. Surprisingly, the SAR of the new series paralleled that of the saturated derivatives with the exception that there was greater tolerance for larger alkyl and cycloalkyl groups at R2 region in comparison to the phenylacetamides. In normal Wistar rats, the 2,3-disubstituted acrylamide analog 10 was well absorbed and demonstrated robust glucose lowering effects. The experimental part of the paper was very detailed, including the reaction process of 5-Bromothiazol-2-amine(cas: 3034-22-8HPLC of Formula: 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.HPLC of Formula: 3034-22-8

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

In 2016,Mikherdov, Alexander S.; Kinzhalov, Mikhail A.; Novikov, Alexander S.; Boyarskiy, Vadim P.; Boyarskaya, Irina A.; Dar’in, Dmitry V.; Starova, Galina L.; Kukushkin, Vadim Yu. published 《Difference in Energy between Two Distinct Types of Chalcogen Bonds Drives Regioisomerization of Binuclear (Diaminocarbene)PdII Complexes》.Journal of the American Chemical Society published the findings.Electric Literature of C3H3BrN2S The information in the text is summarized as follows:

The reaction of cis-[PdCl2(CNXyl)2] (Xyl = 2,6-Me2C6H3) with various 1,3-thiazol- and 1,3,4-thiadiazol-2-amines in chloroform gives a mixture of two regioisomeric binuclear diaminocarbene complexes. For 1,3-thiazol-2-amines the isomeric ratio depends on the reaction conditions and kinetically (KRs) or thermodynamically (TRs) controlled regioisomers were obtained at room temperature and on heating, resp. In CHCl3 solutions, the isomers are subject to reversible isomerization accompanied by the cleavage of Pd-N and C-N bonds in the carbene fragment XylNCN(R)Xyl. Results of DFT calculations followed by the topol. anal. of the electron d. distribution within the formalism of Bader’s theory (AIM method) reveal that in CHCl3 solution the relative stability of the regioisomers (ΔGexp = 1.2 kcal/mol; ΔGcalcd = 3.2 kcal/mol) is determined by the energy difference between two types of the intramol. chalcogen bonds, viz. S···Cl in KRs (2.8-3.0 kcal/mol) and S···N in TRs (4.6-5.3 kcal/mol). In the case of the 1,3,4-thiadiazol-2-amines, the regioisomers are formed in approx. equal amounts and, accordingly, the energy difference between these species is only 0.1 kcal/mol in terms of ΔGexp (ΔGcalcd = 2.1 kcal/mol). The regioisomers were characterized by elemental analyses (C, H, N), HRESI+-MS and FTIR, 1D (1H, 13C{1H}) and 2D (1H,1H-COSY, 1H,1H-NOESY, 1H,13C-HSQC, 1H,13C-HMBC) NMR spectroscopies, and structures of six complexes (three KRs and three TRs) were elucidated by single-crystal X-ray diffraction.5-Bromothiazol-2-amine(cas: 3034-22-8Electric Literature of C3H3BrN2S) was used in this study.

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Electric Literature of C3H3BrN2S

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

In 2016,Gogliotti, Rocco D.; Blobaum, Anna L.; Morrison, Ryan M.; Daniels, J. Scott; Salovich, James M.; Cheung, Yiu-Yin; Rodriguez, Alice L.; Loch, Matthew T.; Conn, P. Jeffrey; Lindsley, Craig W.; Niswender, Colleen M.; Hopkins, Corey R. published 《Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4)》.Bioorganic & Medicinal Chemistry Letters published the findings.Product Details of 3034-22-8 The information in the text is summarized as follows:

Herein the authors report the synthesis and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as novel pos. allosteric modulators of mGlu4. The authors detail the authors’ work towards finding Ph replacements for the core scaffold of previously reported Ph sulfonamides and Ph sulfone compounds The authors’ efforts culminated in the identification of N-(1-((3,4-dimethylphenyl)sulfonyl)-1H-pyrrol-3-yl)picolinamide as a potent PAM of mGlu4. After reading the article, we found that the author used 5-Bromothiazol-2-amine(cas: 3034-22-8Product Details of 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Product Details of 3034-22-8

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

In 2014,Khanfar, Mohammad A.; Quinti, Luisa; Wang, Hua; Choi, Soo Hyuk; Kazantsev, Aleksey G.; Silverman, Richard B. published 《Development and characterization of 3-(arylsulfamoyl)benzamides as potent and selective SIRT2 inhibitors》.European Journal of Medicinal Chemistry published the findings.Application of 3034-22-8 The information in the text is summarized as follows:

Inhibitors of sirtuin-2 deacetylase (SIRT2) have been shown to be protective in various models of Huntington’s disease (HD) by decreasing polyglutamine aggregation, a hallmark of HD pathol. The present study was directed at optimizing the potency of SIRT2 inhibitors containing the neuroprotective sulfobenzoic acid scaffold and improving their pharmacol. To achieve that goal, 176 analogs were designed, synthesized, and tested in deacetylation assays against the activities of major human sirtuins SIRT1-3. This screen yielded 15 compounds with enhanced potency for SIRT2 inhibition and 11 compounds having SIRT2 inhibition equal to reference compound AK-1. The newly synthesized compounds also demonstrated higher SIRT2 selectivity over SIRT1 and SIRT3. These candidates were subjected to a dose-response bioactivity assay, measuring an increase in α-tubulin K40 acetylation in two neuronal cell lines, which yielded five compounds bioactive in both cell lines and eight compounds bioactive in at least one of the cell lines tested. These bioactive compounds were subsequently tested in a tertiary polyglutamine aggregation assay, which identified five inhibitors. ADME properties of the bioactive SIRT2 inhibitors (e.g., I) were assessed, which revealed a significant improvement of the pharmacol. properties of the new entities, reaching closer to the goal of a clin.-viable candidate. The experimental process involved the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8Application of 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Application of 3034-22-8

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

《Site-Selective Thiolation of (Multi)halogenated Heteroarenes》 was written by Sandfort, Frederik; Knecht, Tobias; Pinkert, Tobias; Daniliuc, Constantin G.; Glorius, Frank. Reference of 5-Bromothiazol-2-amine And the article was included in Journal of the American Chemical Society in 2020. The article conveys some information:

A general and simple strategy for the site-selective thiolation of various pharmaceutically relevant electron-rich heteroarenes with thiols is reported. This mild and reliable photocatalytic protocol enables C-S coupling at the most electron-rich position of the (multi)halogenated substrates, complementing established methodologies. Exptl. and computational studies suggest a radical chain mechanism with the key step being a homolytic aromatic substitution of the heteroaryl halide by an electrophilic thiyl radical, highlighting an underdeveloped reactivity mode. In the part of experimental materials, we found many familiar compounds, such as 5-Bromothiazol-2-amine(cas: 3034-22-8Reference of 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Reference of 5-Bromothiazol-2-amine

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

Safety of 5-Bromothiazol-2-amineIn 2011 ,《Synthesis and anticonvulsant activity of some new thiazolo[3,2-a][1,3]diazepine, benzo[d]thiazolo[5,2-a][12,6]diazepine and benzo[d]oxazolo[5,2-a][12,6]diazepine analogues》 was published in European Journal of Medicinal Chemistry. The article was written by El-Subbagh, Hussein I.; Hassan, Ghada S.; El-Azab, Adel S.; Abdel-Aziz, Alaa A.-M.; Kadi, Adnan A.; Al-Obaid, Abdulrahman M.; Al-Shabanah, Othman A.; Sayed-Ahmed, Mohamed M.. The article contains the following contents:

6,7-Dihydro-thiazolo[3,2-a][1,3]diazepines, benzo[d]thiazolo[5,2-a][12,6]diazepines and benzo[d]oxazolo[5,2-a][12,6]diazepine were synthesized and evaluated for their anticonvulsant activity. Compounds (E)-2-bromo-6,7-dihydro-thiazolo[3,2-a][1,3]diazepine-8(5H)-thione, 3-chloro-benzo[d]thiazolo[5,2-a][12,6]diazepin-10-one, and 4-chloro-benzo[d]oxazolo[5,2-a][12,6] diazepin-10-one showed 100% protection against PTZ- and bicuculline-induced seizures; 70%, 33%, 70% protection against MES-induced tonic extension; and 70%, 66%, 100% protection against picrotoxin-induced convulsions, resp. These compounds proved to act as GABAA receptor agonists, with ED50 values of 252, 380, 251 mg/kg; TD50 values of 398, 417, 355 mg/kg; PI values of 1.58, 1.09, 1.41; LD50 values of 380, 617, 537 mg/kg and TI values of 1.51, 1.62, 2.14, resp. After reading the article, we found that the author used 5-Bromothiazol-2-amine(cas: 3034-22-8Safety of 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Safety of 5-Bromothiazol-2-amine

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

Recommanded Product: 5-Bromothiazol-2-amineIn 2012 ,《Identification of (R)-N-(4-(4-methoxyphenyl)thiazol-2-yl)-1-tosylpiperidine-2-carboxamide, ML277, as a novel, potent and selective Kv7.1 (KCNQ1) potassium channel activator》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Mattmann, Margrith E.; Yu, Haibo; Lin, Zhihong; Xu, Kaiping; Huang, Xiaofang; Long, Shunyou; Wu, Meng; McManus, Owen B.; Engers, Darren W.; Le, Uyen M.; Li, Min; Lindsley, Craig W.; Hopkins, Corey R.. The article contains the following contents:

A high-throughput screen utilizing a depolarization-triggered thallium influx through KCNQ1 channels was developed and used to screen the MLSMR collection of over 300,000 compounds An iterative medicinal chem. approach was initiated and from this effort, ML277 (I) was identified as a potent activator of KCNQ1 channels (EC50 = 260 nM). ML277 was shown to be highly selective against other KCNQ channels (>100-fold selectivity vs. KCNQ2 and KCNQ4) as well as against the distantly related hERG potassium channel. The experimental process involved the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8Recommanded Product: 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Recommanded Product: 5-Bromothiazol-2-amine

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

In 2013,Al-Omary, Fatmah A. M.; Hassan, Ghada S.; El-Messery, Shahenda M.; Nagi, Mahmoud N.; Habib, El-Sayed E.; El-Subbagh, Hussein I. published 《Nonclassical antifolates, part 3: Synthesis, biological evaluation and molecular modeling study of some new 2-heteroarylthio-quinazolin-4-ones》.European Journal of Medicinal Chemistry published the findings.Application In Synthesis of 5-Bromothiazol-2-amine The information in the text is summarized as follows:

Compounds I(R1 = Me, R2 = H, R3 = H, n = 0; R1 = R2 = MeO, R3 = H, CO2Et, n = 0) and 39 proved to be active DHFR inhibitors with IC50 range of 0.3-0.8 μM. Compounds I(R1 = Me, R2 = H, R3 = H, n = 0; R1 = R2 = MeO, R3 = H, CO2Et, n = 0) and 39 proved to be active DHFR inhibitors with IC50 range of 0.3-0.8 μM. Compounds I(R1 = R2 = MeO, R3 = H, n = 0; R1 = Me, R2 = H, R3 = CO2Et, n = 0, 1) and II(R1 = Me, R2 = H, n = 0; R1 = R2 = MeO, n = 1) showed broad spectrum antimicrobial activity comparable to the known antibiotic gentamicin. Compound II(R1 = Me, R2 = H, n = 1) showed broad spectrum antitumor activity toward several tumor cell lines with GI values range of 25.8-41.2%. Mol. modeling studies concluded that recognition with key amino acid Arg38 and Lys31 are essential for binding and biol. activities. Flexible alignment; electrostatic and hydrophobic mappings revealed that the obtained model could be useful for the development of new DHFR inhibitors. In the experiment, the researchers used many compounds, for example, 5-Bromothiazol-2-amine(cas: 3034-22-8Application In Synthesis of 5-Bromothiazol-2-amine)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Primary amines having a tertiary alkyl group (R3CNH2) are difficult to prepare with most methods but are made industrially by the Ritter reaction. In this method a tertiary alcohol reacts with hydrogen cyanide (HCN) in the presence of a concentrated strong acid; a formamide, RNH―CHO, is formed first, which then undergoes hydrolysis.Application In Synthesis of 5-Bromothiazol-2-amine

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

In 2004,Helal, Christopher J.; Sanner, Mark A.; Cooper, Christopher B.; Gant, Thomas; Adam, Mavis; Lucas, John C.; Kang, Zhijun; Kupchinsky, Stanley; Ahlijanian, Michael K.; Tate, Bonnie; Menniti, Frank S.; Kelly, Kristin; Peterson, Marcia published 《Discovery and SAR of 2-aminothiazole inhibitors of cyclin-dependent kinase 5/p25 as a potential treatment for Alzheimer’s disease》.Bioorganic & Medicinal Chemistry Letters published the findings.Computed Properties of C3H3BrN2S The information in the text is summarized as follows:

High-throughput screening with cyclin-dependent kinase 5 (cdk5)/p25 led to the discovery of N-(5-isopropyl-thiazol-2-yl)isobutyramide. This compound is an equipotent inhibitor of cdk5 and cyclin-dependent kinase 2 (cdk2)/cyclin E (IC50 = ca. 320 nM). Parallel and directed synthesis techniques were utilized to explore the SAR of this series. Up to 60-fold improvements in potency at cdk5 and 12-fold selectivity over cdk2 were achieved. In the experimental materials used by the author, we found 5-Bromothiazol-2-amine(cas: 3034-22-8Computed Properties of C3H3BrN2S)

5-Bromothiazol-2-amine(cas: 3034-22-8) 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.Computed Properties of C3H3BrN2S

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