Category: 3034-22-8

In 2008,Frechette, Sylvie; Leit, Silvana; Woo, Soon Hyung; Lapointe, Guillaume; Jeannotte, Guillaume; Moradei, Oscar; Paquin, Isabelle; Bouchain, Giliane; Raeppel, Stephane; Gaudette, Frederic; Zhou, Nancy; Vaisburg, Arkadii; Fournel, Marielle; Yan, Pu Theresa; Trachy-Bourget, Marie-Claude; Kalita, Ann; Robert, Marie-France; Lu, Aihua; Rahil, Jubrail; MacLeod, A. Robert; Besterman, Jeffrey M.; Li, Zuomei; Delorme, Daniel published 《4-(Heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs as a novel class of histone deacetylase inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Name: 5-Bromothiazol-2-amine The information in the text is summarized as follows:

The synthesis and biol. evaluation of a variety of 4-(heteroarylaminomethyl)-N-(2-aminophenyl)-benzamides and their analogs is described. Some of these compounds were shown to inhibit HDAC1 with IC50 values below the micromolar range, induce hyperacetylation of histones, upregulate expression of the tumor suppressor p21WAF1/Cip1, and inhibit proliferation of human cancer cells. In addition, certain compounds of this class were active in several human tumor xenograft models in vivo. In the experiment, the researchers used many compounds, for example, 5-Bromothiazol-2-amine(cas: 3034-22-8Name: 5-Bromothiazol-2-amine)

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.Name: 5-Bromothiazol-2-amine

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

Related Products of 3034-22-8In 2006 ,《Discovery and SAR of 2-amino-5-(thioaryl)thiazoles as potent and selective Itk inhibitors》 was published in Bioorganic & Medicinal Chemistry Letters. The article was written by Das, Jagabandhu; Furch, Joseph A.; Liu, Chunjian; Moquin, Robert V.; Lin, James; Spergel, Steven H.; McIntyre, Kim W.; Shuster, David J.; O’Day, Kathleen D.; Penhallow, Becky; Hung, Chen-Yi; Doweyko, Arthur M.; Kamath, Amrita; Zhang, Hongjian; Marathe, Punit; Kanner, Steven B.; Lin, Tai-An; Dodd, John H.; Barrish, Joel C.; Wityak, John. The article contains the following contents:

A series of structurally novel aminothiazole-based inhibitors of Itk were prepared to elucidate their structure-activity relationships (SARs), selectivity, and cell activity in inhibiting IL-2 secretion in a Jurkat T-cell assay. Compound I is identified as a potent and selective Itk inhibitor which inhibits anti-TCR antibody induced IL-2 production in mice in vivo and was previously reported to reduce lung inflammation in a mouse model of ovalbumin induced allergy/asthma. After reading the article, we found that the author used 5-Bromothiazol-2-amine(cas: 3034-22-8Related Products of 3034-22-8)

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.Related Products of 3034-22-8

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

In 2016,Li, Hongshuang; Wang, Xinran; Duan, Guiyun; Xia, Chengcai; Xiao, Yuliang; Li, Furong; Ge, Yanqing; You, Guirong; Han, Junfen; Fu, Xiaopan; Tan, Shanhui; Wang, Rongwei published 《Synthesis, antitumor activity and preliminary structure-activity relationship of 2-aminothiazole derivatives》.Chemical Research in Chinese Universities published the findings.Computed Properties of C3H3BrN2S The information in the text is summarized as follows:

In this paper, we described the synthesis of 2-aminothiazole sublibrary containing Me, bromo, Ph or butylidene at 4- or/and 5-position of its core. All target compounds were evaluated for their antitumor activities against human lung cancer cell line H1299 and human glioma cell line SHG-44. Among the compounds screened, 4,5,6,7-tetrahydrobenzo[d]thiazole(26b) exhibited the most potent antitumor activities with IC50 values of 4.89 and 4.03 μmol/L against the two tested cell lines, resp. Preliminary structure-activity relationship(SAR) studies of these compound were subsequently investigated. In the experiment, the researchers used 5-Bromothiazol-2-amine(cas: 3034-22-8Computed Properties of C3H3BrN2S)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. The methylamines occur in small amounts in some plants. Many polyfunctional amines (i.e., those having other functional groups in the molecule) occur as alkaloids in plants—for example, mescaline, 2-(3,4,5-trimethoxyphenyl)ethylamine; the cyclic amines nicotine, atropine, morphine, and cocaine; and the quaternary salt choline, N-(2-hydroxyethyl)trimethylammonium chloride, which is present in nerve synapses and in plant and animal cells.Computed Properties of C3H3BrN2S

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

In 2006,Vulpetti, Anna; Casale, Elena; Roletto, Fulvia; Amici, Raffaella; Villa, Manuela; Pevarello, Paolo published 《Structure-based drug design to the discovery of new 2-aminothiazole CDK2 inhibitors》.Journal of Molecular Graphics & Modelling published the findings.SDS of cas: 3034-22-8 The information in the text is summarized as follows:

N-(5-Bromo-1,3-thiazol-2-yl)butanamide (compound 1) was found active (IC50 = 808 nM) in a high throughput screening (HTS) for CDK2 inhibitors. By exploiting crystal structures of several complexes between CDK2 and inhibitors and applying structure-based drug design (SBDD), we rapidly discovered a very potent and selective CDK2 inhibitor 4-[(5-isopropyl-1,3-thiazol-2-yl)amino] benzenesulfonamide (compound 4, IC50 = 20 nM). The syntheses, structure-based analog design, kinases inhibition data and x-ray crystallog. structures of CDK2/inhibitor complexes are reported. The results came from multiple reactions, including the reaction of 5-Bromothiazol-2-amine(cas: 3034-22-8SDS of cas: 3034-22-8)

5-Bromothiazol-2-amine(cas: 3034-22-8) belongs to anime. Halogenation, in which one or more hydrogen atoms of an amine is replaced by a halogen atom, occurs with chlorine, bromine, and iodine, as well as with some other reagents, notably hypochlorous acid (HClO). With primary amines the reaction proceeds in two stages, producing N-chloro- and N,N-dichloro-amines, RNHCl and RNCl2, respectively. With tertiary amines, an alkyl group may be displaced by a halogen.SDS of cas: 3034-22-8

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.Reference of 5-Bromothiazol-2-amine 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: 3034-22-8Reference of 5-Bromothiazol-2-amine)

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.Reference of 5-Bromothiazol-2-amine

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.Synthetic Route of C3H3BrN2S 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: 3034-22-8Synthetic Route of C3H3BrN2S)

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.Synthetic Route of C3H3BrN2S

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. Recommanded Product: 3034-22-8 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: 3034-22-8Recommanded Product: 3034-22-8)

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.Recommanded Product: 3034-22-8

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

Recommanded Product: 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: 3034-22-8Recommanded Product: 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.Recommanded Product: 5-Bromothiazol-2-amine

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

Computed Properties of C3H3BrN2SIn 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: 3034-22-8Computed Properties of C3H3BrN2S)

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.Computed Properties of C3H3BrN2S

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.Name: 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: 3034-22-8Name: 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.Name: 5-Bromothiazol-2-amine

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