Day: February 13, 2023

Fate of antibiotics in engineered wastewater systems and receiving water environment: A case study on the coast of Hangzhou Bay, China was written by Bao, Yingyu;Li, Feifei;Chen, Lyujun;Mu, Qinglin;Huang, Bei;Wen, Donghui. And the article was included in Science of the Total Environment in 2021.Synthetic Route of C11H12N4O3S This article mentions the following:

The occurrence of man-made antibiotics in natural environment has aroused attentions from both scientists and publics. However, few studies tracked antibiotics from their production site to the end of disposal environment. Taking the coastal region of Hangzhou Bay as the study area, the fate of 77 antibiotics from 6 categories in two-step wastewater treatment plants (WTPs, i.e. pharmaceutical WTP and integrated WTP) was focused; and the antibiotics in both dissolved and adsorbed phases were investigated simultaneously in this study. The ubiquitous occurrence of antibiotics was observed in the two-step WTPs, with antibiotic concentrations following the order of PWTP (LOQ – 1.0 x 105 ng閻犺櫣鏋?1) > IWTPi (for industrial wastewater treatment, LOQ – 3.7 x 103 ng閻犺櫣鏋?1) > IWTPd (for domestic sewage treatment, LOQ – 1.3 x 103 ng閻犺櫣鏋?1). And the types of antibiotics detected in excess sludge and suspended particles were in accordance with those in wastewater. Quinolones were invariably dominant in both dissolved and adsorbed fractions. High removal efficiencies (median values >50.0%) were acquired for the dissolved quinolones (except for DFX), tetracyclines, 閻?lactams, and lincosamides. Anaerobic/anoxic/oxic achieved the highest aqueous removal of antibiotics among the investigated treatment technologies in the three WTPs. PWTP and IWTP removed 9797 and 487 g閻犺櫣妫?1 of antibiotics, resp.; and a final effluent with 126.4 g閻犺櫣妫?1 of antibiotics was discharged into the effluent-receiving area (ERA) of Hangzhou Bay. Source apportionment anal. demonstrated that the effluents of IWTPd and IWTPd contributed resp. 39.3% and 8.9% to the total antibiotics in the ERA. The results illustrate quant. the antibiotic flows from engineered wastewater systems to natural water environment, on the basis of which the improvements of wastewater treatment technologies and discharge management would be put forward. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Synthetic Route of C11H12N4O3S).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. Pyrimidine derivatives also play an important role in drug development, either in concert with other compounds or on their own.Synthetic Route of C11H12N4O3S

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Discovery of dual Axl/VEGF-R2 inhibitors as potential anti-angiogenic and anti-metastatic drugs for cancer chemotherapy was written by Goff, Dane;Zhang, Jing;Heckrodt, Thilo;Yu, Jiaxin;Ding, Pingyu;Singh, Raj;Holland, Sacha;Li, Weiqun;Irving, Mark. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2017.Reference of 35265-83-9 This article mentions the following:

Axl tyrosine kinase has been shown to be involved in multiple pathways contributing to tumor development, angiogenesis, and metastasis. High Axl expression has been observed in many human tumors where it appears to confer aggressive tumor behavior. Here we present several series of dual Axl-VEGF-R2 kinase inhibitors based on extensive optimization of an acyl diaminotriazole. It was hypothesized that dual inhibition of these two receptor tyrosine kinases may have a synergistic affect in inhibiting tumor angiogenesis and metastasis. One of these mols., R916562 showed comparable activity to Sunitinib in two mouse tumor xenograft models and a mouse corneal micropocket model. In the experiment, the researchers used many compounds, for example, 2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9Reference of 35265-83-9).

2,4-Dichloro-7-methylthieno[3,2-d]pyrimidine (cas: 35265-83-9) belongs to pyrimidine derivatives. Heterocyclic compounds bearing the pyrimidine core are of tremendous interest as they constitute an important class of natural and synthetic compounds exhibiting diverse useful biological activities that hold attractive potential for clinical translation as therapeutic agents in alleviation of a myriad of diseases. Pyrimidine derivatives have been used in a wide variety of pharmaceuticals including general anesthetics, anti-epilepsy medication, anti-malaria medication, drugs for treating high blood pressure, and HIV medication.Reference of 35265-83-9

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthesis and bioevaluation of diaryl urea derivatives as potential antitumor agents for the treatment of human colorectal cancer was written by Wu, Chun-Feng;Wang, Qing-Chen;Chen, Rui;Zhou, Hai-Ling;Wu, Ting-Ting;Du, Yao;Zhang, Na-Na;Zhang, Hui-Min;Fan, Zu-Yan;Wang, Li-Li;Hu, Chu-Jiao;Sang, Zhi-Pei;Li, Hong-Liang;Wang, Ling;Tang, Lei;Zhang, Ji-Quan. And the article was included in European Journal of Medicinal Chemistry in 2022.Category: pyrimidines This article mentions the following:

The development of inhibitors targeting the PI3K-Akt-mTOR signaling pathway has been greatly hindered by the on-target AEs, such as hyperglycemia and hepatotoxicities. In this study, a series of diaryl urea derivatives has been designed and synthesized based on clin. candidate gedatolisib, and most of the newly synthesized derivatives showed kinase inhibitory and antiproliferative activities within nanomolar and submicromolar level, resp. The terminal L-proline amide substituted derivative I showed 8.6-fold more potent PI3K浼?inhibitory activity (0.7 nM) and 4.6-fold more potent antiproliferative effect against HCT116 cell lines (0.11娓璏) compared with control gedatolisib. The potential antitumor mechanism and efficacy of I in HCT116 xenograft models have also been evaluated, and found I showed comparable in vivo antitumor activity with gedatolisib. The safety investigations revealed that compound I exhibited more safer profiles in the selectivity of liver cells (selectivity index: >6.6 vs 1.85) and blood glucose regulation than gedatolisib. In addition, the in vitro stability assays also indicated that developed compound I possessed good metabolic stabilities. In the experiment, the researchers used many compounds, for example, 4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0Category: pyrimidines).

4-(2-Chloropyrimidin-4-yl)morpholine (cas: 62968-37-0) belongs to pyrimidine derivatives. The pyrimidine derivatives can easily interact with enzymes, genetic materials, and bio components within the cell. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Category: pyrimidines

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reactivity of pyrimidinylphosphazenes with acetylenic esters: Competitive [4 + 2] and [2 + 2] tandem cycloaddition or retro-cycloaddition approaches was written by Cobo, Justo;Molina, Sebastian;Sanchez, Adolfo;Nogueras, Manuel;Insuasty, Braulio;Orozco-Lopez, Fabian. And the article was included in Journal of Heterocyclic Chemistry in 2022.Related Products of 54030-56-7 This article mentions the following:

In the search for new intermediates for heterocyclic synthesis, the reactivity of 6-iminophosphoranepyrimidines against di-Me acetylenedicarboxylate (DMAD) and Et propiolate as dienophiles, was studied. The presence of a viable 2-azadienic moiety in pyrimidin-4-one rings (oxo derivatives) favored reaction of DMAD by [4 + 2]/retro-[4 + 2] sequence, in addition to the expected [2 + 2] cycloaddition/retrocycloaddn. involving phosphazene moiety. In contrast, pyrimidine derivatives lacking a viable 2-azadienic residue reacted only through phosphazene group by the aforementioned [2 + 2]/retro-[2 + 2] tandem process. Et propiolate (nonsym. dienophile) proved less reactive giving rise to undesired side reactions. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Related Products of 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Related Products of 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Structure-based drug design of 1,3,5-triazine and pyrimidine derivatives as novel FGFR3 inhibitors with high selectivity over VEGFR2 was written by Kuriwaki, Ikumi;Kameda, Minoru;Hisamichi, Hiroyuki;Kikuchi, Shigetoshi;Iikubo, Kazuhiko;Kawamoto, Yuichiro;Moritomo, Hiroyuki;Kondoh, Yutaka;Amano, Yasushi;Tateishi, Yukihiro;Echizen, Yuka;Iwai, Yoshinori;Noda, Atsushi;Tomiyama, Hiroshi;Suzuki, Tomoyuki;Hirano, Masaaki. And the article was included in Bioorganic & Medicinal Chemistry in 2020.Reference of 59864-30-1 This article mentions the following:

Fibroblast growth factor receptor 3 (FGFR3) is an attractive therapeutic target for the treatment of bladder cancer. We identified 1,3,5-triazine derivative 18b and pyrimidine derivative 40a as novel structures with potent and highly selective FGFR3 inhibitory activity over vascular endothelial growth factor receptor 2 (VEGFR2) using a structure-based drug design (SBDD) approach. X-ray crystal structure anal. suggests that interactions between 18b and amino acid residues located in the solvent region (Lys476 and Met488), and between 40a and Met529 located in the back pocket of FGFR3 may underlie the potent FGFR3 inhibitory activity and high kinase selectivity over VEGFR2. In the experiment, the researchers used many compounds, for example, 2,6-Dimethoxypyrimidine-4-carboxylic acid (cas: 59864-30-1Reference of 59864-30-1).

2,6-Dimethoxypyrimidine-4-carboxylic acid (cas: 59864-30-1) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. Therapy for fungal infections is based mainly on four classes of antifungals: azoles, echinocandins, polyenes, and pyrimidine analogs.Reference of 59864-30-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

A facile three-components, one-pot synthesis of pyrimido[4,5-d]pyrimidine-2,5-dione derivatives under microwave-assisted conditions was written by Dabiri, Minoo;Arvin-Nezhad, Hamid;Khavasi, Hamid R.;Bazgir, Ayoob. And the article was included in Journal of Heterocyclic Chemistry in 2007.HPLC of Formula: 54030-56-7 This article mentions the following:

Pyrimido[4,5-d]pyrimidine-2,5-dione derivatives were synthesized in high yields in a novel, 1-pot, and efficient process by condensation of 6-amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one, aldehydes and urea under microwave-assisted conditions. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7HPLC of Formula: 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives. Drugs having the pyrimidine motif have manifested to exhibit gratifying biological activity like anticancer, antiviral, anti-inflammatory, antibacterial, and antihypertensive activities.HPLC of Formula: 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

A novel reaction of 6-aminouracils and isatins was written by Dabiri, Minoo;Azimi, Seyyedeh Cobra;Khavasi, Hamid Reza;Bazgir, Ayoob. And the article was included in Tetrahedron in 2008.Product Details of 54030-56-7 This article mentions the following:

A simple and novel cyclocondensation reaction of 6-aminouracils and isatins for the synthesis of spiro[pyrimido[4,5-b]quinoline-5,5′-pyrrolo[2,3-d]pyrimidine] derivatives, e.g., I, is reported. I was subjected to x-ray anal. In the experiment, the researchers used many compounds, for example, 6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7Product Details of 54030-56-7).

6-Amino-3-methyl-2-(methylthio)pyrimidin-4(3H)-one (cas: 54030-56-7) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. A Cu-catalyzed and 4-HO-TEMPO-mediated [3 + 3] annulation of commercially available amidines with saturated ketones enables an efficient and facile synthesis of structurally important pyrimidines via a cascade reaction of oxidative dehydrogenation/annulation/oxidative aromatization.Product Details of 54030-56-7

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The exposure levels and health risk assessment of antibiotics in urine and its association with platelet mitochondrial DNA methylation in adults from Tianjin, China: A preliminary study was written by Zhang, Jing;Liu, Ziquan;Song, Shanjun;Fang, Junkai;Wang, Lei;Zhao, Lei;Li, Chenguang;Li, Weixia;Byun, Hyang-Min;Guo, Liqiong;Li, Penghui. And the article was included in Ecotoxicology and Environmental Safety in 2022.SDS of cas: 1220-83-3 This article mentions the following:

There has been extensive research on antibiotics exposure in adults by biomonitoring, but the biol. mechanisms and potential risks to human health remain limited. In this study, 102 adults aged 26-44 years in Tianjin were studied and 23 common antibiotics in urine were analyzed by Liquid chromatog.-mass spectrometry (LC-MS). All antibiotics were detected in urine, with an overall detection frequency of 40.4% (the detection frequencies of phenothiazines, quinolones, sulfonamides, tetracyclines, and chloramphenicol were 77%, 54%, 24%, 28%, and 49%, resp.). Ofloxacin and enrofloxacin had the highest detection frequencies (85% and 81%), with median concentrations of 0.26 (IQR: 0.05-1.36) and 0.09 (IQR: 0.03-0.14) ng/mL, resp. Based on health risk assessment, the predicted estimated daily exposures (EDEs) ranged from 0 铻爂/kg/day to 13.98 铻爂/kg/day. The hazard quotient (HQ) values of all the antibiotics except ofloxacin and ciprofloxacin were bellow one, which are considered safe. For all blood samples, the mitochondrial DNA (mtDNA) methylation levels in the MT-ATP6 (ranging between 3.86% and 34.18%) were slightly higher than MT-ATP8 and MT-ND5 (ranging between 0.57% and 9.32%, 1.08% and 19.62%, resp.). Furthermore, mtDNA methylation from MT-ATP6, MT-ATP8 and MT-ND5 were measured by bisulfite-PCR pyrosequencing. The association (P < 0.05) was found between mtDNA methylation level (MT-ATP8 and MT-ND5) and individual antibiotics including chlorpromazine, ciprofloxacin, enrofloxacin, norfloxacin, pefloxacin, sulfaquinoxaline, sulfachloropyridazine, chloramphenicol, and thiamphenicol, indicating that persistent exposure to low-dose multiple antibiotics may affect the mtDNA methylation level and in turn pose health risks. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3SDS of cas: 1220-83-3).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.SDS of cas: 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Photocatalytic degradation of sulfamonomethoxine by mesoporous phosphorus-doped titania under simulated solar light irradiation was written by Li, Jiang;Su, Qi;Yuan, Huayu;Zhang, Lin;Hou, Li’an;Wang, Yuehu;Liu, Baojun;Wang, Bing;Li, Yancheng. And the article was included in Chemosphere in 2021.Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide This article mentions the following:

Photocatalytic degradation of sulfamonomethoxine (SMM) by mesoporous phosphorus-doped TiO2 (P-TiO₂) was studied under simulated solar light irradiation The morphol. structure and chem. composition of P-TiO₂ were analyzed by XRD, SEM, HRTEM, BET, XPS and FTIR. Using the central composite design (CCD) of response surface methodol. (RSM), the degradation of SMM was investigated with a range of antibiotic concentrations (4-8 mg L^-1), catalyst dosages (400-900 mg L^-1), P doping amounts (5-15 wt%) and irradiation time (90-150 min). The Ti-O-P bond formed during the calcination of TiO₂, thereby generating plate-like P-TiO₂, where P was uniformly distributed. Phosphorus doping can stabilize anatase TiO₂, which has a larger sp. surface area and a lower average particle and pore size than bare TiO₂. The result obtained from the RSM model showed a significant correlation between the predicted values and the exptl. results of SMM degradation (P < 0.05). Under the optimal exptl. conditions (antibiotic concentration = 6 mg/L, catalyst dosage = 800 mg/L, P doping = 5 wt% and irradiation time = 90 min), the degradation rate of SMM was 99.51%, and the TOC was 50%. Toxicity showed a considerable reduction towards Vibrio-qinghaiensis sp.-Q67 after SMM photocatalytic degradation Through free radical capture experiments, LC-MS detection and DFT calculations, the possible photocatalytic degradation mechanism of SMM using P-TiO₂ as the catalyst was revealed. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. Pyrimidines are isomeric with two other forms of diazines: pyridazine, with the nitrogen atoms in the 1 and 2 positions; and pyrazine, with the nitrogen atoms in the 1 and 4 positions. As nucleotides in DNA and RNA, pyrimidine nucleotide derivatives have a wide range of biological applications. For example, pyrimidine derivatives are useful in DNA repair studies involving cancer and epigenetics.Application In Synthesis of 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Hydrophilic crosslinking agent-incorporated magnetic imprinted materials with enhanced selectivity for sulfamethazine adsorption was written by Cui, Yahan;Lin, Jiasheng;Xu, Yang;Li, Qiaoyan;Chen, Yanhua;Ding, Lan. And the article was included in Separation and Purification Technology in 2021.Recommanded Product: 1220-83-3 This article mentions the following:

In this study, magnetic molecularly imprinted polymers (MMIPs) with enhanced selectivity were synthesized using sulfamethazine (SMZ) as template mol. and hydrophilic triethylene glycol dimethacrylate as cross-linker. Compared with that of imprinted polymers (MMIPs@EGDMA) prepared with commonly used ethylene glycol dimethacrylate, MMIPs with increased hydrophilicity could achieve efficient adsorption and preferred binding ability for template SMZ (selectivity factor increased from 0.9 of MMIPs@EGDMA to 1.9) in the presence of structural analogs with significant similarities (i.e. sulfamonomethoxine). Under the optimal extraction conditions, the developed MMIPs-MSPE-HPLC-DAD method showed wide linear range (1.6-250娓璯/L), low detection limit (0.44娓璯/L) and satisfactory precision (RSD < 7%). The proposed strategy offers a potential and simple way to obtain imprinted polymers with high recognition capability, providing a perspective method in the accurate determination of SMZ in environmental water. In the experiment, the researchers used many compounds, for example, 4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3Recommanded Product: 1220-83-3).

4-Amino-N-(6-methoxypyrimidin-4-yl)benzenesulfonamide (cas: 1220-83-3) belongs to pyrimidine derivatives. The pyrimidine nitrogenous bases are derived from the organic compound pyrimidine through the addition of various functional groups. We all know its importance to life – pyrimidine and purine bases are included in the structure of DNA and RNA.Recommanded Product: 1220-83-3

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia