Month: April 2022

Recommanded Product: 118994-89-1. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: Ethyl oxazole-5-carboxylate, is researched, Molecular C6H7NO3, CAS is 118994-89-1, about Synthesis and evaluation of anthelmintic and cytotoxic properties of [2,5′]bis-1,3-azole analogs of bengazoles.

Using different heterocycle formation methodologies (Deoxo-Fluor, DAST, POCl3, TosMIC), [2,5′]bis-1,3-azoles were prepared as stable analogs of bengazoles, a family of potent anthelmintic marine natural products. The cytotoxic activity of these heterocycles and their precursors on HCT-15 cells and the effect on the L4 larvae of Nippostrongylus brasiliensis were evaluated.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Synthetic Route of C5H5FN2. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 5-Amino-2-fluoropyridine, is researched, Molecular C5H5FN2, CAS is 1827-27-6, about Soluble-type small-molecule CD4 mimics as HIV entry inhibitors. Author is Kobayakawa, Takuya; Konno, Kiju; Ohashi, Nami; Takahashi, Kohei; Masuda, Ami; Yoshimura, Kazuhisa; Harada, Shigeyoshi; Tamamura, Hirokazu.

Several small mol. CD4 mimics have been reported previously as HIV-1 entry inhibitors, which block the interaction between the Phe43 cavity of HIV-1 gp120 and the host CD4. Known CD4 mimics such as NBD-556 possess significant anti-HIV activity but are less soluble in water, perhaps due to their hydrophobic aromatic ring-containing structures. Compounds with a pyridinyl group in place of the Ph group in these mols. have been designed and synthesized in an attempt to increase the hydrophilicity. Some of these new CD4 mimics, containing a tetramethylpiperidine ring show significantly higher water solubility than NBD-556 and have high anti-HIV activity and synergistic anti-HIV activity with a neutralizing antibody. The CD4 mimic that has a cyclohexylpiperidine ring and a 6-fluoropyridin-3-yl ring has high anti-HIV activity and no significant cytotoxicity. The present results will be useful in the future design and development of novel soluble-type mol. CD4 mimics.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Safety of 4-Aminopyrimidine. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 4-Aminopyrimidine, is researched, Molecular C4H5N3, CAS is 591-54-8, about Design, synthesis and biological evaluation of pyrazole-aromatic containing carboxamides as potent SDH inhibitors.

To continue studies on discovery of new potent antifungal leads, 43 novel pyrazole-aromatic containing carboxamides were rationally designed and synthesized. Bioassays indicated that most target compounds displayed good in vitro antifungal activities against Botrytis cinerea, Rhizoctonia cerealis and Sclerotinia sclerotiorum and in vivo antifungal activity against R. solani. Compound I exhibited the most significant in vitro activity against R. cerealis (EC50 = 0.93μg/mL) with about 2-fold more potent than a previously reported lead compound N-(3-bromophenyl)-2-[3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl]-4-thiazolecarboxamide (EC50 = 2.01μg/mL), and about 11-fold more potent than the pos. control/com. succinate dehydrogenase inhibitor thifluzamide (EC50 = 23.09μg/mL). Structure-activity relationship anal. and mol. docking simulations indicated that the presence of difluoromethyl pyrazole-(m-benzene)carboxamide scaffold obviously increased the antifungal activity. The further enzymic bioassay showed that both thifluzamide and compound I displayed excellent SDH inhibitory effects, and fluorescence quenching anal. suggested that they may share the same target SDH.

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Pyrazine – Wikipedia,
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So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Lee, H. H.; Palmer, B. D.; Wilson, W. R.; Denny, W. A. researched the compound: 4-Bromo-1-methyl-2-nitro-1H-imidazole( cas:121816-79-3 ).SDS of cas: 121816-79-3.They published the article 《Synthesis and hypoxia-selective cytotoxicity of a 2-nitroimidazole mustard》 about this compound( cas:121816-79-3 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: chloroethylaminonitroimidazole preparation hypoxia selective cytotoxicity; nitroimidazole mustard preparation hypoxia selective cytotoxicity; imidazole chloroethylaminonitro preparation hypoxia selective cytotoxicity. We’ll tell you more about this compound (cas:121816-79-3).

A four-step synthesis of 5-[N,N-bis(2-chloroethyl)amino]-1-methyl-2-nitroimidazole from 1-methyl-2-nitroimidazole is described. This compound showed similar hypoxia-selective cytotoxicity to the dinitrobenzamide mustard SN 23862 in UV4 cells (ca. 40-fold), and superior selectivity (>7-fold) in repair-competent AA8 cells.

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Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Most of the compounds have physiologically active properties, and their biological properties are often attributed to the heteroatoms contained in their molecules, and most of these heteroatoms also appear in cyclic structures. A Journal, Tianjin Keji Daxue Xuebao called Effect of DL-ATC on the production of L-cysteine with enzymatic method by Pseudomonas sp. TS1138, Author is Li, Mei; Huang, Lei; Huai, Li-hua; Chen, Ning, which mentions a compound: 2150-55-2, SMILESS is O=C(C1N=C(N)SC1)O, Molecular C4H6N2O2S, COA of Formula: C4H6N2O2S.

L-cysteine is an elementary S-containing amino acid, which has been widely used in medicines, food additives, and cosmetics. Effect of DL-ATC on the conditions of enzyme production process by Pseudomonas sp. TS1138 and enzymic transformation of L-cysteine was discussed. The results show that DL-ATC add in the medium has an inducible impact on enzyme production On account of the interaction of the L-cysteine yield and conversion ratio of DL-ATC, the optimal concentration of DL-ATC is confirmed at about 9 g/L-1. The L-cysteine yield is increased by 56.25% with the DL-ATC interval feeding method.

Compound(2150-55-2)COA of Formula: C4H6N2O2S received a lot of attention, and I have introduced some compounds in other articles, similar to this compound(2-Amino-4,5-dihydrothiazole-4-carboxylic acid), if you are interested, you can check out my other related articles.

Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Shinozuka, Tsuyoshi; Kobayashi, Hiroyuki; Suzuki, Sayaka; Tanaka, Kyosuke; Karanjule, Narayan; Hayashi, Noriyuki; Tsuda, Toshifumi; Tokumaru, Eri; Inoue, Masahiro; Ueda, Kiyono; Kimoto, Hiroko; Domon, Yuki; Takahashi, Sakiko; Kubota, Kazufumi; Yokoyama, Tomihisa; Shimizugawa, Akiko; Koishi, Ryuta; Fujiwara, Chie; Asano, Daigo; Sakakura, Tomoko; Takasuna, Kiyoshi; Abe, Yasuyuki; Watanabe, Toshiyuki; Kitano, Yutaka published the article 《Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor》. Keywords: neuropathic pain safety GSH preclin CYP3A4 sodium channels inhibitor.They researched the compound: 4-Aminopyrimidine( cas:591-54-8 ).Electric Literature of C4H5N3. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:591-54-8) here.

A highly potent, selective NaV1.7 inhibitor, DS-1971a(I), has been discovered. Exploration of the left-hand Ph ring of sulfonamide derivatives (I and II) led to the discovery of novel series of cycloalkane derivatives with high NaV1.7 inhibitory potency in vitro. As the right-hand heteroaromatic ring affected the mechanism-based inhibition liability of CYP3A4, replacement of this moiety resulted in the generation of 4-pyrimidyl derivatives Addnl., GSH adducts formation, which can cause idiosyncratic drug toxicity, was successfully avoided by this modification. An addnl. optimization led to the discovery of DS-1971a. In preclin. studies, DS-1971a demonstrated highly potent selective in vitro profile with robust efficacy in vivo. DS-1971a exhibited a favorable toxicol. profile, which enabled multiple-dose studies of up to 600 mg bid or 400 mg tid (1200 mg/day) administered for 14 days to healthy human males. DS-1971a is expected to exert potent efficacy in patients with peripheral neuropathic pain, with a favorable safety profile.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《Kinetics of the cyanide-cystine reaction》. Authors are Gawron, Oscar; Fernando, Joseph.The article about the compound:2-Amino-4,5-dihydrothiazole-4-carboxylic acidcas:2150-55-2,SMILESS:O=C(C1N=C(N)SC1)O).Computed Properties of C4H6N2O2S. Through the article, more information about this compound (cas:2150-55-2) is conveyed.

The kinetics of the cystine-cyanide reaction was studied in 0.04M KOH at pH 12.5 by a spectrophotometric method. The reaction was bimol., with cyclization of the thiocyanato product much faster than the reverse reaction. Activation parameters at 35° were: Ea, 16.8 kcal./mole; ΔH*, 16.1 kcal./mole; and ΔS*, -7.4 e.u. The entropy of activation was about the same as that for the cyanide-S8 reaction but about 20 e.u. less than that for the cystine-SO3–reaction; this indicated the activated complex for cystine-SO3– is more crowded than that for cystine-CN-.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

In organic chemistry, atoms other than carbon and hydrogen are generally referred to as heteroatoms. The most common heteroatoms are nitrogen, oxygen and sulfur. Now I present to you an article called 2-Iminothiazolidine-4-carboxylic acid produces hippocampal CA1 lesions independent of seizure excitation and glutamate receptor activation, published in 1997, which mentions a compound: 2150-55-2, mainly applied to iminothiazolidinecarboxylate hippocampus CA1 lesion glutamate receptor, Electric Literature of C4H6N2O2S.

In this study, the ability of either 2-iminothiazolidine-4-carboxylic acid (2-ICA), glutamate, proline or NMDA (N-methyl-D-aspartate) injected i.c.v. to produce hippocampal lesions sensitive to glutamate antagonists was compared in mice. Hippocampal CA1 damage was observed 5-days following either a seizure (3.2 μmol) or subseizure (1.0 μmol) dose of 2-ICA. Glutamate (3.2 μmol) or proline (10 μmol) also produced hippocampal damage; glutamate damage was primarily to the CA1 subfield, whereas proline damaged neurons throughout the entire hippocampal formation. NMDA (3.2 nmol) caused seizure activity in all animals with a 50% lethality. No hippocampal damage was observed in surviving mice. Neither MK-801 (dizocilpine maleate) nor CNQX (6-cyano-7-nitroquinoxaline-2,3-dione) pretreatment prevented hippocampal lesions produced by 2-ICA. In contrast, MK-801 significantly reduced the frequency of mice displaying glutamate hippocampal lesions, but failed to block seizures produced by glutamate. MK-801 also protected neurons in the CA2-3 zone and the dentate gyrus, but not in the CA1 region of proline-injected mice. Finally, pretreatment with the mixed metabotropic glutamate receptor (mGluR)1/mGluR2 antagonist-agonist (S)-4-carboxy-3-hydroxyphenylglycine (CHPG) prevented hippocampal damage produced by the mGluR 1 agonist (RS)-3,5-dihydroxyphenylglycine (DHPG), but did not protect against 2-ICA hippocampal lesions. These results show that 2-ICA hippocampal CA1 damage is not mediated through ionotropic or metabotropic glutamate receptors. 2-ICA hippocampal damage may represent a neurotoxicity that is distinct from excitotoxic-mediated cell death.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Related Products of 2150-55-2. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 2-Amino-4,5-dihydrothiazole-4-carboxylic acid, is researched, Molecular C4H6N2O2S, CAS is 2150-55-2, about Identification of bioconversion product from DL-ATC and optimization of reaction conditions in Pseudomonas sp. F12. Author is Fan, Cui-li; Li, Zhi-min; Ye, Qin.

The objective if this work was to identify the bioconversion product from DL-2-amino-Δ2-thiazoline-4-carboxylic acid (DL-ATC) and enhance L-cysteine yield from it. Reaction mixture was analyzed by HPLC and LC-MS; comparison among different reaction conditions of L-cysteine decomposition was performed. Contrast to standard L-cysteine, the results of HPLC and LC-MS indicated that it was L-cysteine; a small amount of hydrogen sulfide produced from degradation of L-cysteine inhibited L-cysteine desulfhydrase dramaticly in air-free condition which contributed the highest amount of L-cysteine arrived 46.2 mmol/L with a yield of 94%, in contrast to that of 31.6% under initial condition. Pseudomonas sp. F12 equipped with the ability of converting DL-ATC to L-cysteine; it was beneficial for L-cysteine accumulation in air-free condition.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem

Matralis, Alexios N.; Malik, Adnan; Penzo, Maria; Moreno, Inmaculada; Almela, Maria J.; Camino, Isabel; Crespo, Benigno; Saadeddin, Anas; Ghidelli-Disse, Sonja; Rueda, Lourdes; Calderon, Felix; Osborne, Simon A.; Drewes, Gerard; Boesche, Markus; Fernandez-Alvaro, Elena; Martin Hernando, Jose Ignacio; Baker, David A. published an article about the compound: 4-Aminopyrimidine( cas:591-54-8,SMILESS:C1=CN=CN=C1N ).Application of 591-54-8. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:591-54-8) through the article.

One of the attractive properties of artemisinins is their extremely fast-killing capability, quickly relieving malaria symptoms. Nevertheless, the unique benefits of these medicines are now compromised by the prolonged parasite clearance times and the increasing frequency of treatment failures, attributed to the increased tolerance of Plasmodium falciparum to artemisinin. This emerging artemisinin resistance threatens to undermine the effectiveness of antimalarial combination therapies. Herein, we describe the medicinal chem. efforts focused on a cGMP-dependent protein kinase (PKG) inhibitor scaffold, leading to the identification of novel chem. entities with very potent, similar to artemisinins, fast-killing potency against asexual blood stages that cause disease, and activity against gametocyte activation that is required for transmission. Furthermore, we confirm that selective PKG inhibitors have a slow speed of kill, while chemoproteomic anal. suggests for the first time serine/arginine protein kinase 2 (SRPK2) targeting as a novel strategy for developing antimalarial compounds with extremely fast-killing properties.

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Reference:
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem