Category: 55661-33-1

Total Synthesis of ME1036 Starting from Readily Available Inexpensive Materials was written by Han, Zhi-Jian;Li, Yang-Bin;Yang, Lu-Xi;Song, Ai-lin;Chen, Hao;Li, Yu-Min. And the article was included in Letters in Organic Chemistry in 2015.Related Products of 55661-33-1 This article mentions the following:

This work demonstrates the effective total synthesis of a new broad-spectrum parenteral carbapenem I starting from the readily available and inexpensive N-Cbz-protected glycine amide in high yield with easy work-up under mild reaction conditions. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Related Products of 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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. 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.Related Products of 55661-33-1

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

Exploration of novel piperazine or piperidine constructed non-covalent peptidyl derivatives as proteasome inhibitors was written by Zhuang, Rangxiao;Gao, Lixin;Lv, Xiaoqing;Xi, Jianjun;Sheng, Li;Zhao, Yanmei;He, Ruoyu;Hu, Xiaobei;Shao, Yidan;Pan, Xuwang;Liu, Shourong;Huang, Weiwei;Zhou, Yubo;Li, Jia;Zhang, Jiankang. And the article was included in European Journal of Medicinal Chemistry in 2017.SDS of cas: 55661-33-1 This article mentions the following:

A series of novel piperazine or piperidine-containing non-covalent peptidyl derivatives possessing a neopentyl-asparagine residue were designed, synthesized and evaluated as proteasome inhibitors. All target compounds were screened for their 20S proteasome chymotrypsin-like inhibitory activities, and 15 ones displayed more potent activities than carfilzomib with IC₅₀ values lower than 10 nM. Subsequently, the most potent 10 analogs were tested for their cytotoxic activities against two multiple myeloma (MM) cell lines RPMI-8226 and MM-1S. Based on these experiments, selected derivatives were further evaluated for their ex vivo and in vivo blood cell proteasome inhibitory activities. The most potential compound (I) (proteasome inhibition IC₅₀: 1.2 ± 0.1 nM) with potent anti-proliferation (IC₅₀: RPMI-8226 8.4 ± 0.8 nM; MM-1S: 6.3 ± 0.8 nM), ex vivo and in vivo activities also had a prolonged half life in plasma, which demonstrated that the enzymic stabilities of this series of compounds have been improved by constructing a six-membered ring into the peptide skeleton. All the experiments confirmed the correctness of design concept, which made this series of compounds potential leads for exploring new anti-MM drugs. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1SDS of cas: 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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.SDS of cas: 55661-33-1

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

Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors was written by Han, Yongxin;Giroux, Andre;Colucci, John;Bayly, Christopher I.;Mckay, Daniel J.;Roy, Sophie;Xanthoudakis, Steve;Vaillancourt, John;Rasper, Dita M.;Tam, John;Tawa, Paul;Nicholson, Donald W.;Zamboni, Robert J.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2005.COA of Formula: C4H6N2S This article mentions the following:

The iterative process for the discovery of a series of pyrazinone mono-amides as potent, selective and reversible non-peptide caspase-3 inhibitors (e.g., M826 and M867) is reported. The studied compounds were prepared according to modified literature procedure from ethylaminobutyrate hydrochloride via intermediate acids (e. g., I), which were synthesized using Dess-Martin periodinane oxidation Treating of coupled to the resin in the presence of Hunig’s base intermediate acids I with 90% TFA in water gave the desired inhibitors (e. g. II). These compounds were screened directly, without further purification, against four representative recombinant human caspases, as well as in the NT2 cell against camptothecin induced apoptosis. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1COA of Formula: C4H6N2S).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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. 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: C4H6N2S

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

Transforming Benzylic Amines into Diarylmethanes: Cross-Couplings of Benzylic Pyridinium Salts via C-N Bond Activation was written by Liao, Jennie;Guan, Weiye;Boscoe, Brian P.;Tucker, Joseph W.;Tomlin, John W.;Garnsey, Michelle R.;Watson, Mary P.. And the article was included in Organic Letters in 2018.Related Products of 55661-33-1 This article mentions the following:

A nickel-catalyzed cross-coupling of benzylic pyridinium salts with arylboronic acids was developed. Coupled with chemoselective pyridinium formation, this method allows benzyl primary amines to be efficiently converted to di(hetero)arylmethanes, e.g., I. Excellent heteroaryl and functional group tolerance is observed, and a one-pot procedure enables benzylic amines to be converted to diarylmethanes directly. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Related Products of 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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.Related Products of 55661-33-1

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

Development and characterization of 3-(arylsulfamoyl)benzamides as potent and selective SIRT2 inhibitors was written by Khanfar, Mohammad A.;Quinti, Luisa;Wang, Hua;Choi, Soo Hyuk;Kazantsev, Aleksey G.;Silverman, Richard B.. And the article was included in European Journal of Medicinal Chemistry in 2014.Quality Control of Thiazol-2-ylmethanamine This article mentions the following:

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. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Quality Control of Thiazol-2-ylmethanamine).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles are a class of five-membered rings containing nitrogen and sulfur with excellent antitumor, antiviral and antibiotic activities. 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.Quality Control of Thiazol-2-ylmethanamine

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

Matrix Metalloproteinase Inhibitors: A Structure Activity Study was written by Levy, Daniel E.;Lapierre, France;Liang, Weisheng;Ye, Wenqing;Lange, Christopher W.;Li, Xiaoyuan;Grobelny, Damian;Casabonne, Marie;Tyrrell, David;Holme, Kevin;Nadzan, Alex;Galardy, Richard E.. And the article was included in Journal of Medicinal Chemistry in 1998.Name: Thiazol-2-ylmethanamine This article mentions the following:

Modifications around the dipeptide-mimetic core of hydroxamic acid based matrix metalloproteinase inhibitors I [AA = L-Trp, D-Trp, L-Trp(Me), L-3-benzothienylalanine, L-1- and -2-naphthylalanine, L-3- and -8-quinolylalanine, L-4-phenylphenylalanine, L-Phe, L-3- and -4-pyridylalanine, L–tert-leucine, L-abrine; R⁶ = NHMe, NH(CH₂)₄Me, NHCH₂CH₂OH, NHCH₂CH₂NHCO₂CH₂Ph, cyclopropylamino, cyclopentylamino, (S)- and (R)-1-indanylamino, (1R,2S)- and (1S,2R)-2-hydroxy-1-indanylamino, (S)-NHCHMePh, NHCH₂Ph, piperonylamino, 2-, 3-, and 4-pyridylmethylamino, 2-(4-pyridyl)ethylamino, NHCH₂CH₂C₆H₄OH-4, 2-furanylmethylamino, 2-thiazolylmethylamino, 2-benzimidazolylamino, 3-(1-imidazolyl)propylamino, 3-(4-morpholinyl)propylamino; R² = H, OH; R³ = CH₂CHMe₂, Bu, n-hexyl, n-octyl, OCHMe₂, O(CH₂)₄Me] were studied. These variations incorporated a variety of natural, unnatural, and synthetic amino acids in addition to modifications of the P1′ and P3′ substituents. The results of this study indicate the following structural requirements: (1) Two key hydrogen bonds must be present between the enzyme and potent substrates. (2) Potent inhibitors must possess potent zinc-binding functionalities. (3) The potential importance of the hydrophobic group at position R³ as illustrated by its ability to impart greater relative potency against stromelysin when larger hydrophobic groups are used. (4) Requirements surrounding the nature of the amino acid appear to be more restrictive for stromelysin than for neutrophil collagenase, 72 kDa gelatinase, and 92 kDa gelatinase. These requirements may involve planar fused-ring aryl systems and possibly hydrogen-bonding capabilities. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Name: Thiazol-2-ylmethanamine).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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. 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.Name: Thiazol-2-ylmethanamine

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

From dihydroxypyrimidine carboxylic acids to carboxamide HIV-1 integrase inhibitors: SAR around the amide moiety was written by Petrocchi, Alessia;Koch, Uwe;Matassa, Victor G.;Pacini, Barbara;Stillmock, Kara A.;Summa, Vincenzo. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2007.Quality Control of Thiazol-2-ylmethanamine This article mentions the following:

4,5-Dihydroxypyrimidine carboxamides, which evolved from a related series of HCV NS5b polymerase inhibitors, have been optimized to provide selective HIV integrase strand transfer inhibitors. Extensive SAR around the benzylamide moiety led to the identification of the p-fluorobenzylamide compound I as optimal in the enzymic assay. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Quality Control of Thiazol-2-ylmethanamine).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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. 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.Quality Control of Thiazol-2-ylmethanamine

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

Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V₂ receptor agonists was written by Tsukamoto, Issei;Koshio, Hiroyuki;Kuramochi, Takahiro;Saitoh, Chikashi;Yanai-Inamura, Hiroko;Kitada-Nozawa, Chika;Yamamoto, Eisaku;Yatsu, Takeyuki;Shimada, Yoshiaki;Sakamoto, Shuichi;Tsukamoto, Shin-ichi. And the article was included in Bioorganic & Medicinal Chemistry in 2009.Related Products of 55661-33-1 This article mentions the following:

A series of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives was synthesized, and their structure-activity relationships were examined in order to identify potent and selective arginine vasopressin V₂ receptor agonists. Attempts to substitute other chem. groups in place of the 2-pyridilmethyl moiety of 1a led to the discovery that potent V₂ binding affinity could be obtained with a wide range of functional groups. This structural tolerance allowed for the manipulation of other attributes, such as selectivity against V_1a receptor affinity or avoidance of the undesirable inhibition of cytochrome P 450 (CYP), without losing potent affinity for the V₂ receptor. Some representative compounds obtained in this study were also found to decrease urine volume in awake rats. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Related Products of 55661-33-1).

Thiazol-2-ylmethanamine (cas: 55661-33-1) belongs to thiazole derivatives. Thiazoles frequently appear in peptide studies. Thiazoles can also be used as protected formyl groups, which can be released in later stages of complex natural product synthesis. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Related Products of 55661-33-1

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

Antitubercular and Antiparasitic 2-Nitroimidazopyrazinones with Improved Potency and Solubility was written by Ang, Chee Wei;Tan, Lendl;Sykes, Melissa L.;AbuGharbiyeh, Neda;Debnath, Anjan;Reid, Janet C.;West, Nicholas P.;Avery, Vicky M.;Cooper, Matthew A.;Blaskovich, Mark A. T.. And the article was included in Journal of Medicinal Chemistry in 2020.Name: Thiazol-2-ylmethanamine This article mentions the following:

Following the approval of delamanid and pretomanid as new drugs to treat drug-resistant tuberculosis, there is now a renewed interest in bicyclic nitroimidazole scaffolds as a source of therapeutics against infectious diseases. We recently described a nitroimidazopyrazinone bicyclic subclass with promising antitubercular and antiparasitic activity, prompting addnl. efforts to generate analogs with improved solubility and enhanced potency. The key pendant aryl substituent was modified by (i) introducing polar functionality to the methylene linker, (ii) replacing the terminal Ph group with less lipophilic heterocycles, or (iii) generating extended biaryl side chains. Improved antitubercular and antitrypanosomal activity was observed with the biaryl side chains, with most analogs achieved 2- to 175-fold higher activity than the monoaryl parent compounds, with encouraging improvements in solubility when pyridyl groups were incorporated. This study has contributed to understanding the existing structure-activity relationship (SAR) of the nitroimidazopyrazinone scaffold against a panel of disease-causing organisms to support future lead optimization. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Name: Thiazol-2-ylmethanamine).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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 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.Name: Thiazol-2-ylmethanamine

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

Antileukemic agents. 3. Synthesis and antitumor activity of N-(2-chloroethyl)-N-nitrosourea derivatives was written by Nakao, Hideo;Fukushima, Masami;Shimizu, Fusaaki;Arakawa, Masao. And the article was included in Yakugaku Zasshi in 1974.Synthetic Route of C4H6N2S This article mentions the following:

Water-soluble derivatives of N-(2-chloroethyl)-N-nitrosourea RNHCON(NO)CH2CH2Cl (R = pyridylmethyl, pyrimidinylmethyl, quinazolinylmethyl, benzimidazolylethyl, etc.) were prepared and their antitumor activity was tested against leukemia L-1210. Most of these compounds showed a high activity. In the experiment, the researchers used many compounds, for example, Thiazol-2-ylmethanamine (cas: 55661-33-1Synthetic Route of C4H6N2S).

Thiazol-2-ylmethanamine (cas: 55661-33-1) 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. 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.Synthetic Route of C4H6N2S

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