Month: January 2023

Structure-activity study of diuretic azanaphthalene derivatives was written by Mizuta, Eiji;Nishikawa, Kohei;Omura, Kiyoshi;Oka, Yoshikazu. And the article was included in Chemical & Pharmaceutical Bulletin in 1976.HPLC of Formula: 322-46-3 This article mentions the following:

Regression anal. by the Free-Wilson technique was applied to estimate the contribution of substituents on azanaphthalene skeletons to diuretic activity of pyrimido[4,5-d]pyridazine and pyrido[3,4-d]pyridazine derivatives In the former group, one of the most preferable compounds was DS-210 [2-phenyl-5,8-dimorpholinopyrimido[4,5-d]pyridazine](I) [33222-18-3] and that in the latter group proved to be DS-511 (1,4-dimorpholine-7-phenylpyrido[3,4-d]pyridazine)(II) [39632-88-7]. Subsequently, electron d. distributions on a variety of azanaphthalene skeletons were calculated by extended Huckel Theory calculation Linear multiple regression anal. to find a correlation between diuretic activity and electron d. at some positions of azanaphthalene skeletons suggested that the diuretic activity might be influenced largely by electronic structures at the ring junction. In the experiment, the researchers used many compounds, for example, Pyrido[2,3-b]pyrazine (cas: 322-46-3HPLC of Formula: 322-46-3).

Pyrido[2,3-b]pyrazine (cas: 322-46-3) belongs to pyrazine derivatives. Pyrazine is an N-heterocyclic moiety, and it can be easily prepared from ethylenediamine and 1,2-diketone, α-hydroxyketone, α-methyl ketone. A large number of pyrazine derivatives are known for their antitumor, antibiotic, anticonvulsant, antituberculosis, and diuretic activities.HPLC of Formula: 322-46-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Development of subnanomolar radiofluorinated (2-pyrrolidin-1-yl)imidazo[1,2-b]pyridazine pan-Trk inhibitors as candidate PET imaging probes was written by Bernard-Gauthier, Vadim;Bailey, Justin J.;Aliaga, Arturo;Kostikov, Alexey;Rosa-Neto, Pedro;Wuest, Melinda;Brodeur, Garrett M.;Bedell, Barry J.;Wuest, Frank;Schirrmacher, Ralf. And the article was included in MedChemComm in 2015.Recommanded Product: 1150566-27-0 This article mentions the following:

Dysregulation of tropomyosin receptor kinases (TrkA/B/C) expression and signalling is recognized as a hallmark of numerous neurodegenerative diseases including Parkinson’s, Huntington’s and Alzheimer’s disease. TrkA/B/C is known to drive tumorogensis and metastatic potential in a wide range of neurogenic and non-neurogenic human cancers. The development of suitable positron emission tomog. (PET) radioligands would allow an in vivo exploration of this versatile potential therapeutic target. Herein, the rational remodeling of the amide moiety of a 6-(2-(3-fluorophenyl)pyrrolidin-1-yl)imidazo[1,2-b]pyridazine-3-amide lead structure to accommodate efficient fluorine-18 labeling led to the identification of a series of fluorinated Trk inhibitors with picomolar IC₅₀. The ensuing representative radiolabeled inhibitors [¹⁸F]16 ([¹⁸F]-(±)-IPMICF6) and [¹⁸F]27 ([¹⁸F]-(±)-IPMICF10) constitute novel lead radioligands with about 2- to 3- orders of magnitude increased TrkB/C potencies compared to previous lead tracers and display favorable selectivity profiles and physicochem. parameters for translation into in vivo PET imaging agents. In the experiment, the researchers used many compounds, for example, Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0Recommanded Product: 1150566-27-0).

Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. Pyrazine-based skeletons were incorporated into agents targeting a range of ailments. Many derivatives were synthesized and evaluated as potential cancer treatments.Recommanded Product: 1150566-27-0

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Derisking the Cu-Mediated ¹⁸F-Fluorination of Heterocyclic Positron Emission Tomography Radioligands was written by Taylor, Nicholas J.;Emer, Enrico;Preshlock, Sean;Schedler, Michael;Tredwell, Matthew;Verhoog, Stefan;Mercier, Joel;Genicot, Christophe;Gouverneur, Veronique. And the article was included in Journal of the American Chemical Society in 2017.HPLC of Formula: 1150566-27-0 This article mentions the following:

The compatibility of various heterocycles, particularly nitrogen heterocycles, towards the copper-mediated ¹⁸F-fluorination of aryl pinacolboronates with ¹⁸F-fluoride was determined using fluorination reactions of a model substrate in the presence of exogenous heterocycles and the fluorination reactions of substrates possessing heterocycles with fluorination on an attached aromatic ring or directly attached to the heterocycle of interest. Using this information, syntheses of seven ¹⁸F-labeled structurally complex pharmaceutically relevant heterocycle-containing mols. were designed and executed. The method may be useful in designing syntheses of other radiolabeled compounds and delineating the scope of utility of other radiolabeling methods. In the experiment, the researchers used many compounds, for example, Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0HPLC of Formula: 1150566-27-0).

Ethyl 6-chloroimidazo[1,2-b]pyridazine-3-carboxylate (cas: 1150566-27-0) belongs to pyrazine derivatives. Pyrazinesare six-membered aromatic heterocyclic organic compounds with two nitrogen atoms at 1,4-positions. Pyrazine is a weaker base (pKb = 13.4) than pyridine (pKb = 8.8), pyrimidine (pKb = 12.7). Pyrazines are chemical compounds (technically called “methoxypyrazines”) found in grape skin and stems that are responsible for many “green” flavors in wine. Levels of pyrazines are dependent on viticultural practices, climate, and grape variety.HPLC of Formula: 1150566-27-0

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Detection and Imaging of Aβ1-42 and Tau Fibrils by Redesigned Fluorescent X-34 Analogues was written by Zhang, Jun;Sandberg, Alexander;Konsmo, Audun;Wu, Xiongyu;Nystroem, Sofie;Nilsson, K. Peter R.;Konradsson, Peter;Le Vine, Harry III;Lindgren, Mikael;Hammarstroem, Per. And the article was included in Chemistry – A European Journal in 2018.SDS of cas: 148231-12-3 This article mentions the following:

The authors revisited the Congo red analog 2,5-bis(4′-hydroxy-3′-carboxy-styryl)benzene (X-34) to develop this highly fluorescent amyloid dye for imaging Alzheimer’s disease (AD) pathol. comprising Aβ and Tau fibrils. A selection of ligands with distinct optical properties were synthesized by replacing the central benzene unit of X-34, with other heterocyclic moieties. Full photophys. characterization was performed, including recording absorbance and fluorescence spectra, Stokes shift, quantum yield and fluorescence lifetimes. All ligands displayed high affinity towards recombinant amyloid fibrils of Aβ1-42 (13-300 nM K_d) and Tau (16-200 nM K_d) as well as selectivity towards the corresponding disease-associated protein aggregates in AD tissue. These ligands efficiently displaced X-34, but not Pittsburgh compound B (PiB) from recombinant Aβ1-42 amyloid fibrils, arguing for retained targeting of the Congo red type binding site. The authors foresee that the X-34 scaffold offers the possibility to develop novel high-affinity ligands for Aβ pathol. found in human AD brain in a different mode compared with PiB, potentially recognizing different polymorphs of Aβ fibrils. In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3SDS of cas: 148231-12-3).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. Pyrazines are chemical compounds (technically called “methoxypyrazines”) found in grape skin and stems that are responsible for many “green” flavors in wine. Levels of pyrazines are dependent on viticultural practices, climate, and grape variety.SDS of cas: 148231-12-3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Pyridopyrazines was written by Zhang, J.. And the article was included in Science of Synthesis, Knowledge Updates in 2010.Synthetic Route of C7H5N3 This article mentions the following:

This manuscript is an update of the original Science of Synthesis chapter and includes methods for the preparation of pyrido[2,3-b]pyrazine derivatives and pyrido[3,4-b]pyrazine derivatives described in the literature up to 2010. Methods proceeding by a condensation of pyridinediamine derivatives with carbonyl compounds and the application of (halo)pyrido[2,3-b]pyrazines by palladium-catalyzed cross-coupling reactions are covered. In the experiment, the researchers used many compounds, for example, Pyrido[2,3-b]pyrazine (cas: 322-46-3Synthetic Route of C7H5N3).

Pyrido[2,3-b]pyrazine (cas: 322-46-3) belongs to pyrazine derivatives. Pyrazine is an N-heterocyclic moiety, and it can be easily prepared from ethylenediamine and 1,2-diketone, α-hydroxyketone, α-methyl ketone. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging.Synthetic Route of C7H5N3

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

High-Performance and Light-Emitting n-Type Organic Field-Effect Transistors Based on Dithienylbenzothiadiazole and Related Heterocycles was written by Kono, Takahiro;Kumaki, Daisuke;Nishida, Jun-ichi;Sakanoue, Tomo;Kakita, Motoyasu;Tada, Hirokazu;Tokito, Shizuo;Yamashita, Yoshiro. And the article was included in Chemistry of Materials in 2007.Computed Properties of C8H4Br2N2 This article mentions the following:

Authors developed new semiconductors composed of donor-acceptor compounds including electron accepting benzothiazole and related heterocycles. The FET devices based on them showed high n-type performance. Using the benzothiazole unit, the threshold voltage was reduced to 3 CM^-1. The devices showed n-type light emitting FET characteristics, where the emission intensity was strongly dependent on the gate voltage. In the experiment, the researchers used many compounds, for example, 5,8-Dibromoquinoxaline (cas: 148231-12-3Computed Properties of C8H4Br2N2).

5,8-Dibromoquinoxaline (cas: 148231-12-3) belongs to pyrazine derivatives. Pyrazine is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. A number of pyrazine-based derivatives were used as dyes or fluorescent probes.Computed Properties of C8H4Br2N2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Ligustrazine Derivatives. Part 8: Design, Synthesis, and Preliminary Biological Evaluation of Novel Ligustrazinyl Amides as Cardiovascular Agents was written by Li, Zhenyu;Yu, Fang;Cui, Lei;Chen, Wenmin;Wang, Shouxun;Zhan, Peng;Shen, Yuemao;Liu, Xinyong. And the article was included in Medicinal Chemistry (Sharjah, United Arab Emirates) in 2014.Application In Synthesis of (3,5,6-Trimethylpyrazin-2-yl)methanol This article mentions the following:

A series of novel Ligustrazinyl amides was designed, synthesized and evaluated for their protective effect on the injured vascular endothelial cells. The preliminary results demonstrated that some compounds possessed more potent activities than that of Ligustrazine in stimulating replication of the injured human umbilical vascular endothelial cells (HUVECs) that is damaged by hydrogen peroxide. Among the active compounds, compounds 8i, 8t and 8u exhibited the highest potency with low EC50 values of 0.037, 0.070 and 0.055 mM, resp. Structure-activity relationships were briefly discussed. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Application In Synthesis of (3,5,6-Trimethylpyrazin-2-yl)methanol).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazines are volatile compounds that are used in the cosmetic, food, flavor, and fragrance industries. A large number of pyrazine derivatives are known for their antitumor, antibiotic, anticonvulsant, antituberculosis, and diuretic activities.Application In Synthesis of (3,5,6-Trimethylpyrazin-2-yl)methanol

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

New amiloride analog as hapten to raise anti-amiloride antibodies was written by Kleyman, Thomas R.;Rajagopalan, Raghavan;Cragoe, Edward J. Jr.;Erlanger, Bernard F.;Al-Awqati, Qais. And the article was included in American Journal of Physiology in 1986.Name: Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate This article mentions the following:

A new amiloride analog amiloride-caproic acid, was synthesized, coupled to albumin, and used as a hapten to raise anti-amiloride antibodies in rabbits. The antibodies were affinity purified with an amiloride affinity column and characterized. Binding studies using [³H]benzamil showed a dissociation constant of 0.8 nM. Amiloride and amiloride-caproate inhibited [³H]benzamil binding; ε-guanidinocaproic acid showed no inhibition. Anti-amiloride antibodies reversed the inhibition by amiloride of Na transport across the toad urinary bladder. Anti-amiloride antibodies and an amiloride affinity column should provide useful tools for the characterization of the epithelial Na channel. In the experiment, the researchers used many compounds, for example, Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate (cas: 1458-01-1Name: Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate).

Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate (cas: 1458-01-1) belongs to pyrazine derivatives. Pyrazine is an N-heterocyclic moiety, and it can be easily prepared from ethylenediamine and 1,2-diketone, α-hydroxyketone, α-methyl ketone. Pyrazines are chemical compounds (technically called “methoxypyrazines”) found in grape skin and stems that are responsible for many “green” flavors in wine. Levels of pyrazines are dependent on viticultural practices, climate, and grape variety.Name: Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Protective effects of 2-hydroxymethyl-3,5,6-trimethylpyrazine on vascular endothelial cells injured by hydrogen peroxide was written by Li, Chaowu;Liu, Xinyong;Zhang, Rui;Xu, Wenfang;Li, Zhong;Wang, Defeng. And the article was included in Shandong Daxue Xuebao, Yixueban in 2003.Application In Synthesis of (3,5,6-Trimethylpyrazin-2-yl)methanol This article mentions the following:

The protective effects of 2-hydroxymethyl-3,5,6-trimethylpyrazine (HTMP) on human umbilical vein endothelial cells (HUVECs) injured by H₂O₂ were studied. HUVECs viability was assessed by Me thiazolyl tetrazolium assay and tetramethylpyrazine (TMP) was used as a controlled drug. HTMP (0.1-1.5 mM) highly stimulated the proliferation of normal HUVECs, and protected the injured HUVECs against suppression induced by H₂O₂, which had more potency than the pos. drug TMP. The exptl. data suggested that HTMP exerted protective action on injured HUVECs and had a great significance for repairing the injured endothelium in treatment of cardiovascular diseases. In the experiment, the researchers used many compounds, for example, (3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3Application In Synthesis of (3,5,6-Trimethylpyrazin-2-yl)methanol).

(3,5,6-Trimethylpyrazin-2-yl)methanol (cas: 75907-74-3) belongs to pyrazine derivatives. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging. Pyrazine and a variety of alkylpyrazines are flavor and aroma compounds found in baked and roasted goods. Tetramethylpyrazine (also known as ligustrazine) is reported to scavenge superoxide anion and decrease nitric oxide production in human Granulocytes.Application In Synthesis of (3,5,6-Trimethylpyrazin-2-yl)methanol

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Pyrazine diuretics. II. N-amidino-3-amino-5-substituted 6-halopyrazinecarboxamides was written by Cragoe, Edward J. Jr.;Woltersdorf, Otto W. Jr.;Bicking, John B.;Kwong, Sara F.;Jones, James Holden. And the article was included in Journal of Medicinal Chemistry in 1967.Computed Properties of C6H7ClN4O2 This article mentions the following:

The synthesis of a series of N-amidino-3-amino-5-substituted-6-halopyrazinecarboxamides (I) is described In rats and dogs, these compounds cause diuresis and saluresis while K excretion is unaffected or repressed Compounds with a variety of 5 substituents including hydroxy, alkoxy, mercapto, alkylmercapto, amino, and substitute amino were prepared The latter 2 tupes embrace compounds with the highest activity. Several routes for the synthesis of Me 3-amino-5,6-dichloropyrazinoate, a key intermediate, are presented. 23 references. In the experiment, the researchers used many compounds, for example, Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate (cas: 1458-01-1Computed Properties of C6H7ClN4O2).

Methyl 3,5-diamino-6-chloropyrazine-2-carboxylate (cas: 1458-01-1) belongs to pyrazine derivatives. Pyrazine is a symmetrical molecule with point group D2h. Pyrazine is less basic than pyridine, pyridazine and pyrimidine. Pyrazine heterocycles and their benzo derivatives possess many interesting properties, including chemical reactivity profiles, and have diverse applications in total synthesis, medicine, chemical biology, materials, dyes, and imaging.Computed Properties of C6H7ClN4O2

Referemce:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem