Month: November 2022

Ozaki, Masakuni published the artcileIn vivo antibacterial activity of a prodrug of NM394, a thiazetoquinoline carboxylic acid derivative, Recommanded Product: Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate, the main research area is thiazetoquinoline prodrug NM441 NM394 antibacterial.

NM394 (6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-[1,3]-thiazeto[3,2-a]quinoline-3-carboxylic acid) has potent, broad-spectrum antibacterial activity in vitro, but not in vivo. To increase the bioavailability of NM394, various prodrugs were synthesized and tested. One of them, NM441, an N-(5-methyl-2-oxo-1,3-dioxol-4-yl) derivative, showed potent in vivo antibacterial activity. Using thin-layer chromatog.-bioautog., it was confirmed that after oral administration, NM441 was readily absorbed and hydrolyzed to NM394. Other prodrugs of NM394 were only partially metabolized to NM394. In pharmacokinetic studies in mice and monkeys, it was found that the blood levels of NM394 were 7.8 and 5.9 × greater, resp., when NM441 rather than NM394 was administered. These findings suggest that NM441 is an effective prodrug of NM394.

Chemotherapy (Basel) published new progress about Antimicrobial agents. 113028-17-4 belongs to class piperazines, name is Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate, and the molecular formula is C18H20FN3O3S, Recommanded Product: Ethyl 6-fluoro-1-methyl-4-oxo-7-(piperazin-1-yl)-1,4-dihydro-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Ali, Ayad K. published the artcileSignal detection and clarification of peripheral neuropathy and Guillain-Barracue syndrome associated with exposure to systemic fluoroquinolones, Formula: C21H19ClF3N3O3, the main research area is Cipro Levaquin Avelox Noroxin Floxin fluoroquinolone Guillain Barre syndrome.

Aims: Peripheral neuropathy (PN) is an identified risk of systemic antibacterial therapy with fluoroquinolones. The risk and its severity, including the development of Guillain-Barré syndrome (GBS) between individual agents is uncertain. This study examines the association between fluoroquinolones and PN and GBS in cases spontaneously reported to the FDA Adverse Event Reporting System (FAERS). Study Design: Retrospective pharmacovigilance anal. Place and Duration of Study: Cases submitted to FAERS between 1997 and 2012. Methodol.: The MedDRA Preferred Term was used to define PN and GBS. Individual fluoroquinolones were identified by generic names and route of administration. Empirical Bayes Geometric Mean (EBGM) with 95% confidence interval (EB05-EB95) was calculated as disproportionality measure. Safety signals with EB05≥2 was considered a significant disproportional increase in event reporting of at least twice times higher than expected. Results: There were 539 PN reports out of 46,257 adverse event reports submitted for fluoroquinolones. 9% of PN reports were for GBS. Significant disproportionality of PN (EBGM 2.70; EB05-EB95 2.51-2.90) and GBS (EBGM 3.22; EB05-EB95 2.55-4.02) was identified for fluoroquinolones. Signals of PN were detected for ciprofloxacin (EBGM 3.24; EB05-EB95 2.87-3.66) and levofloxacin (EBGM 3.36; EB05-EB95 3.02-3.72). A GBS signal was detected for ciprofloxacin (EBGM 4.15; EB05-EB95 2.94-5.74). GBS and PN resp. ranked 6th and 8th among reported neurol. events. Conclusion: This study reemphasizes the link between fluoroquinolones and PN, and shows potential association with more severe forms of nerve damage, e.g. GBS. Unless the benefit of fluoroquinolone therapy outweighs PN risk, treatment with alternative antibacterial agents is recommended.

British Journal of Pharmaceutical Research published new progress about Antibacterial agents. 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Formula: C21H19ClF3N3O3.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Wang, Ning-Yu published the artcileDesign, synthesis and structure-activity relationship study of piperazinone-containing thieno[3,2-d]pyrimidine derivatives as new PI3Kδ inhibitors, Application In Synthesis of 109384-27-2, the main research area is thienopyrimidine piperazinone preparation SAR non Hodgkin lymphoma PI3K antiproliferative; Antiproliferative activity; PI3Kδ; Piperazinone; SAR; Thieno[3,2-d]pyrimidine.

Two classes of piperazinone-containing thieno[3,2-d]pyrimidines were designed and synthesized as new PI3Kδ inhibitors in this study. Detailed SAR study with respect to the piperazinone substituents at the 6-position of thieno[3,2-d]pyrimidine core demonstrated that piperazinone-containing thieno[3,2-d]pyrimidines would be more potent and selective for PI3Kδ than their piperazine counterparts, which led to the discovery of several potent PI3Kδ inhibitors with comparable or better antiproliferative activity against a panel of non-Hodgkin lymphoma (NHL) cell lines as compared with idelalisib. Our study will promote the development of new PI3Kδ inhibitors based on piperazinone-containing thieno[3,2-d]pyrimidine scaffold.

Bioorganic & Medicinal Chemistry Letters published new progress about Antiproliferative agents. 109384-27-2 belongs to class piperazines, name is 1-Methylpiperazin-2-one hydrochloride, and the molecular formula is C5H11ClN2O, Application In Synthesis of 109384-27-2.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Food and Drug Administration, HHS published the artcileList of drug products that have been withdrawn or removed from the market for reasons of safety or effectiveness, Product Details of C21H19ClF3N3O3, the main research area is drug safety effectiveness standard.

The Food and Drug Administration (FDA) is amending its regulations to include a list of drug products that may not be used for pharmacy compounding under the exemptions under section 503A of the Federal Food, Drug, and Cosmetic Act because they have had their approval withdrawn or were removed from the market because the drug product or its components have been found to be unsafe or not effective. The list has been compiled under the new statutory requirements of the Food and Drug Administration Modernization Act of 1997 (Modernization Act).

Federal Register published new progress about Adrenal cortex (extracts). 105784-61-0 belongs to class piperazines, name is Temafloxacin hydrochloride, and the molecular formula is C21H19ClF3N3O3, Product Details of C21H19ClF3N3O3.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Wang, Guangjun published the artcileAn efficient synthesis of ABT-263, a novel inhibitor of antiapoptotic Bcl-2 proteins, Synthetic Route of 187669-28-9, the main research area is ABT263 Bcl2 protein inhibitor preparation.

ABT-263, a newly developed Bcl-2 inhibitor, was efficiently synthesized. The key intermediates 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl]methyl}piperazin-1-yl)benzoic acid and 4-fluoro-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide were efficiently prepared by a 3-component Mannich reaction and by nucleophilic fluorination of 1-nitro-2-[(trifluoromethyl)sulfonyl]benzene as the key steps, resp. Our work may lay a foundation for a new process development of this promising anticancer drug candidate.

Synthesis published new progress about Bcl-2 proteins Role: NUU (Other Use, Unclassified), USES (Uses) (inhibitors of). 187669-28-9 belongs to class piperazines, name is tert-Butyl 4-(piperazin-1-yl)benzoate, and the molecular formula is C15H22N2O2, Synthetic Route of 187669-28-9.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Hansen, Hanne D. published the artcileSynthesis, radiolabeling and in vivo evaluation of [11C](R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol, a potential PET radioligand for the 5-HT7 receptor, Recommanded Product: tert-Butyl 4-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl)piperazine-1-carboxylate, the main research area is biphenylpiperazine preparation radiolabeling PET imaging serotonin 5HT7 receptor; 5-HT(7) receptor; Arylpiperazine; PET; Radioligand; SB-269970.

In the search for a novel serotonin 7 (5-HT7) receptor PET radioligand we synthesized and evaluated a new series of biphenylpiperazine derivatives in vitro. Among the studied compounds, (R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol, showed the best combination of affinity, selectivity, and lipophilicity, and was thus chosen for carbon-11 labeling and evaluation in pigs. After i.v. injection, compound I entered the pig brain and displayed reversible tracer kinetics. Pretreatment with the 5-HT7 receptor selective antagonist SB-269970 resulted in limited decrease in the binding of I, suggesting that this radioligand is not optimal for imaging the brain 5-HT7 receptor in vivo but it may serve as a lead compound for the design of novel 5-HT7 receptor PET radioligands.

European Journal of Medicinal Chemistry published new progress about 5-HT1A receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study). 1073354-42-3 belongs to class piperazines, name is tert-Butyl 4-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl)piperazine-1-carboxylate, and the molecular formula is C20H32BN3O4, Recommanded Product: tert-Butyl 4-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridin-2-yl)piperazine-1-carboxylate.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

Scattolin, Thomas published the artcileA Nucleophilic Deprotection of Carbamate Mediated by 2-Mercaptoethanol, HPLC of Formula: 187669-28-9, the main research area is carbamate mercaptoethanol nucleophilic deprotection; secondary amine preparation.

Carbamates, typically used for the protection of amines, including Cbz, Alloc, and Me carbamate, was readily deprotected by treatment with 2-mercaptoethanol in the presence of potassium phosphate tribasic in N,N-dimethylacetamide at 75°C. This nucleophilic deprotection protocol was superior to the standard hydrogenolysis or Lewis acid-mediated deprotection conditions for substrates bearing a functionality sensitive to these more traditional methods.

Organic Letters published new progress about Free energy. 187669-28-9 belongs to class piperazines, name is tert-Butyl 4-(piperazin-1-yl)benzoate, and the molecular formula is C15H22N2O2, HPLC of Formula: 187669-28-9.

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics