Tag: 100-200

Studies towards the total synthesis of epothilones: asymmetric synthesis of the key fragments was written by Schinzer, Dieter;Limberg, Anja;Boehm, Oliver M.. And the article was included in Chemistry – A European Journal in 1996.Product Details of 74704-39-5 The following contents are mentioned in the article:

Three key intermediates, the C(1)-C(6) and C(7)-C(12) fragments and a side chain fragment of epothilones A and B were prepared This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Product Details of 74704-39-5).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) 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 δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Product Details of 74704-39-5

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

Pseudomonas aeruginosa porphobilinogen synthase assembly state regulators: hit discovery and initial SAR studies was written by Reitz, Allen B.;Ramirez, Ursula D.;Stith, Linda;Du, Yanming;Smith, Garry R.;Jaffe, Eileen K.. And the article was included in ARKIVOC (Gainesville, FL, United States) in 2010.Reference of 74704-39-5 The following contents are mentioned in the article:

Porphobilinogen synthase (PBGS) catalyzes the first common step in the biosynthesis of the essential heme, chlorophyll and vitamin B₁₂ heme pigments. PBGS activity is regulated by assembly state, with certain oligomers exhibiting biol. activity and others either partially or completely inactive, affording an innovative means of allosteric drug action. Pseudomonas aeruginosa PBGS is functionally active as an octamer, and inactive as a dimer. We have identified a series of compounds that stabilize the inactive P. aeruginosa dimer by a computational prescreen followed by native PAGE gel mobility shift anal. From those results, we have prepared related thiadiazoles and evaluated their ability to regulate P. aeruginosa PBGS assembly state. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Reference of 74704-39-5).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) 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. 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.Reference of 74704-39-5

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

Discovery of the First Potent and Selective Inhibitors of Human dCTP Pyrophosphatase 1 was written by Llona-Minguez, Sabin;Hoeglund, Andreas;Jacques, Sylvain A.;Johansson, Lars;Calderon-Montano, Jose Manuel;Claesson, Magnus;Loseva, Olga;Valerie, Nicholas C. K.;Lundbaeck, Thomas;Piedrafita, Javier;Maga, Giovanni;Crespan, Emmanuele;Meijer, Laurent;Burgos Moron, Estefania;Baranczewski, Pawel;Hagbjoerk, Ann-Louise;Svensson, Richard;Wiita, Elisee;Almloef, Ingrid;Visnes, Torkild;Jeppsson, Fredrik;Sigmundsson, Kristmundur;Jensen, Annika Jenmalm;Artursson, Per;Jemth, Ann-Sofie;Stenmark, Paal;Warpman Berglund, Ulrika;Scobie, Martin;Helleday, Thomas. And the article was included in Journal of Medicinal Chemistry in 2016.Quality Control of 4-(Bromomethyl)-2-methylthiazole The following contents are mentioned in the article:

The dCTPase pyrophosphatase 1 (dCTPase) regulates the intracellular nucleotide pool through hydrolytic degradation of canonical and noncanonical nucleotide triphosphates (dNTPs). DCTPase is highly expressed in multiple carcinomas and is associated with cancer cell stemness. Here the authors report on the development of the first potent and selective dCTPase inhibitors that enhance the cytotoxic effect of cytidine analogs in leukemia cells. Boronate I displays a promising in vitro ADME profile, including plasma and mouse microsomal half-lives, aqueous solubility, cell permeability and CYP inhibition, deeming it a suitable compound for in vivo studies. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Quality Control of 4-(Bromomethyl)-2-methylthiazole).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. The thiazole ring is notable as a component of the vitamin thiamine (B1). 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.Quality Control of 4-(Bromomethyl)-2-methylthiazole

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

Multi-step application of immobilized reagents and scavengers: A total synthesis of epothilone C was written by Storer, R. Ian;Takemoto, Toshiyasu;Jackson, Philip S.;Brown, Dearg S.;Baxendale, Ian R.;Ley, Steven V.. And the article was included in Chemistry – A European Journal in 2004.Recommanded Product: 4-(Bromomethyl)-2-methylthiazole The following contents are mentioned in the article:

The total synthesis of the cytotoxic antitumor natural product epothilone C has provided a stage for the exploitation and further development of immobilized reagent methods. A stereoselective convergent synthetic strategy was applied, incorporating polymer-supported reagents, catalysts, scavengers and catch-and-release techniques to avoid frequent aqueous work-up and chromatog. purification The enantioselective preparation of 3 key fragments heptanone I, (S)-2-methyl-6-heptenal, and thiazole II along with their elaboration via diastereoselective coupling into epothilone C is presented. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Recommanded Product: 4-(Bromomethyl)-2-methylthiazole).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) 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 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.Recommanded Product: 4-(Bromomethyl)-2-methylthiazole

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

Structure activity studies of the serine-AIB dipeptide domain in 2,3-dihydroisothiazole based growth hormone secretagogues was written by Evers, Britta;Ruehter, Gerd;Berg, Martina;Dodge, Jeffrey A.;Hankotius, Dirk;Hary, Ulrike;Jungheim, Louis N.;Mest, Hans-Juergen;de la Nava, Eva-Maria Martin;Mohr, Michael;Muehl, Brian S.;Petersen, Soenke;Sommer, Birgit;Riedel-Herold, Grit;Tebbe, Mark J.;Thrasher, Kenneth J.;Voelkers, Silke. And the article was included in Bioorganic & Medicinal Chemistry in 2005.Related Products of 74704-39-5 The following contents are mentioned in the article:

A series of growth hormone secretagogues (GHSs) based on 2,3-dihydroisothiazole has been synthesized in the search for a potential treatment of growth hormone deficiency or frailty in the elderly. This paper describes the evaluation of the SAR of the benzyl-D-Ser-aminoisobutyric acid dipeptide fragment. Introduction of substituents in the peptide backbone and in the Ph ring has been investigated, as well as replacements for the benzyl group and for the AIB residue. A number of modifications resulted in enhanced potency over the parent benzyl-D-Ser-AIB derivative This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Related Products of 74704-39-5).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) 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.Related Products of 74704-39-5

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

Palladium-Catalyzed Regioselective C-H Heteroarylation of Pyridotriazoles was written by Rawat, Deepa;Semwal, Rashmi;Adimurthy, Subbarayappa. And the article was included in ChemistrySelect in 2022.Formula: C7H4FNS The following contents are mentioned in the article:

An efficient and regioselective palladium-catalyzed C-H heteroarylation of [1,2,3]triazolo[1,5-a]pyridines with benzo[b]thiophenes and benzothiazoles was described. A series of C-7 arylated [1,2,3]triazolo[1,5-a]pyridines were obtained in moderate to good yields with exclusive regioselectivity and good functional group tolerance. DBU (1,8-Diazabicyclo(5.4.0)undec-7-ene) as a base and Ag₂CO₃ as oxidant were the best combination for the transformation and avoided the pre-functionalized substrates. Control experiments suggested that the reaction proceeds through ionic pathway. This study involved multiple reactions and reactants, such as 7-Fluorobenzo[d]thiazole (cas: 214855-12-6Formula: C7H4FNS).

7-Fluorobenzo[d]thiazole (cas: 214855-12-6) 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.Formula: C7H4FNS

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

Phthalazinone Pyrazoles as Potent, Selective, and Orally Bioavailable Inhibitors of Aurora-A Kinase was written by Prime, Michael E.;Courtney, Stephen M.;Brookfield, Frederick A.;Marston, Richard W.;Walker, Victoria;Warne, Justin;Boyd, Andrew E.;Kairies, Norman A.;von der Saal, Wolfgang;Limberg, Anja;Georges, Guy;Engh, Richard A.;Goller, Bernhard;Rueger, Petra;Rueth, Matthias. And the article was included in Journal of Medicinal Chemistry in 2011.Electric Literature of C5H6BrNS The following contents are mentioned in the article:

The inhibition of Aurora kinases in order to arrest mitosis and subsequently inhibit tumor growth via apoptosis of proliferating cells has generated significant discussion within the literature. We report a novel class of Aurora kinase inhibitors based upon a phthalazinone pyrazole scaffold. The development of the phthalazinone template resulted in a potent Aurora-A selective series of compounds (typically >1000-fold selectivity over Aurora-B) that display good pharmacol. profiles with significantly improved oral bioavailability compared to the well studied Aurora inhibitor VX-680. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Electric Literature of C5H6BrNS).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) belongs to thiazole derivatives. Thiazole is a five-membered, unsaturated, planar, π-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.Electric Literature of C5H6BrNS

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

Total Syntheses of Epothilones B and D was written by Jung, Jae-Chul;Kache, Rajashaker;Vines, Kimberly K.;Zheng, Yan-Song;Bijoy, Panicker;Valluri, Muralikrishna;Avery, Mitchell A.. And the article was included in Journal of Organic Chemistry in 2004.Recommanded Product: 4-(Bromomethyl)-2-methylthiazole The following contents are mentioned in the article:

A convergent, total synthesis of epothilones B (I; X = O) and D (I; X = bond) is described. The key steps are Normant coupling to establish the desired (Z)-stereochem. at C12-C13, Wadsworth-Emmons olefination, diastereoselective aldol condensation of aldehyde II with the enolate of keto acid derivatives to form the C6-C7 bond, selective deprotection, and macrolactonization. This study involved multiple reactions and reactants, such as 4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5Recommanded Product: 4-(Bromomethyl)-2-methylthiazole).

4-(Bromomethyl)-2-methylthiazole (cas: 74704-39-5) 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. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Recommanded Product: 4-(Bromomethyl)-2-methylthiazole

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

TBHP/AIBN-Mediated Synthesis of 2-Amino-thiazoles from Active Methylene Ketones and Thiourea under Metal-free Conditions was written by Sun, Jiyun;Ge, Huaibin;Zhen, Xiaohua;An, Xuechan;Zhang, Guangtao;Zhang-Negrerie, Daisy;Du, Yunfei;Zhao, Kang. And the article was included in Tetrahedron in 2018.Product Details of 303994-99-2 The following contents are mentioned in the article:

A new oxidative system of tert-Bu hydroperoxide (TBHP)/azodiisobutyronitrile (AIBN) was used for the first time for a convenient, metal-free synthesis of substituted 2-aminothiazoles from active methylene ketone derivatives and thiourea. The reaction was postulated to proceed via an oxidative cyclization initiated by a radical process and followed by a condensation reaction. This study involved multiple reactions and reactants, such as 2-Amino-4-(tert-butyl)thiazole-5-carbonitrile (cas: 303994-99-2Product Details of 303994-99-2).

2-Amino-4-(tert-butyl)thiazole-5-carbonitrile (cas: 303994-99-2) 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. 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.Product Details of 303994-99-2

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

Design, synthesis, and structure-activity relationship studies of benzothiazole derivatives as antifungal agents was written by Zhao, Shizhen;Zhao, Liyu;Zhang, Xiangqian;Liu, Chunchi;Hao, Chenzhou;Xie, Honglei;Sun, Bin;Zhao, Dongmei;Cheng, Maosheng. And the article was included in European Journal of Medicinal Chemistry in 2016.HPLC of Formula: 479028-67-6 The following contents are mentioned in the article:

A series of compounds with benzothiazole and amide-imidazole scaffolds were designed and synthesized to combat the increasing incidence of drug-resistant fungal infections. The antifungal activity of these compounds was evaluated in vitro, and their structure-activity relationships (SARs) were evaluated. The synthesized compounds showed excellent inhibitory activity against Candida albicans and Cryptococcus neoformans. The most potent compounds I (R¹ = 6-Br, 6-CF₃; R² = ipr, ibu) exhibited potent activity, with min. inhibitory concentration (MIC) values in the range of 0.125-2 μg/mL. Preliminary mechanism studies revealed that the compound I (R¹ = 6-Br, R² = ibu) might act by inhibiting the CYP51 of Candida albicans. The SARs and binding mode established in this study are useful for further lead optimization. This study involved multiple reactions and reactants, such as 6-Fluorobenzo[d]thiazole-2-carboxylic acid (cas: 479028-67-6HPLC of Formula: 479028-67-6).

6-Fluorobenzo[d]thiazole-2-carboxylic acid (cas: 479028-67-6) 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 δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current.Various laboratory methods exist for the organic synthesis of thiazoles. For example, 2,4-dimethylthiazole is synthesized from thioacetamide and chloroacetone.HPLC of Formula: 479028-67-6

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