Delving into the Latest Updates on Oxolinic Acid with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

OA, Oxolinic acid (USAN/INN)

+ [2]

Target

Bacterial DNA gyrase

Action

inhibitors

Mechanism

Bacterial DNA gyrase inhibitors(Bacterial DNA gyrase inhibitors)

Therapeutic Areas

Infectious DiseasesUrogenital Diseases

Active Indication

Urinary Tract Infections

Inactive Indication-

Originator Organization-

Active Organization-

Inactive Organization-

License Organization-

Drug Highest PhaseApproved

First Approval Date-

Regulation-

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Structure/Sequence

Molecular FormulaC13H11NO5

InChIKeyKYGZCKSPAKDVKC-UHFFFAOYSA-N

CAS Registry14698-29-4

The aims of this study are: To compare salivary pH changes and stimulation efficacy of two different Gustatory Stimulants of Salivation (GSSS) in patients with Primary Sjögren Syndrome (PSS); To evaluate Primary Sjögren syndrome (PSS) impact and gustatory stimulants of salivary secretion (GSSS) on oral health related quality of life measured by a Portuguese version of Oral Health Impact Profile-14 (OHIP-14) and specific Xerostomia assessment questionnaires.
The Products to be used are the Xeros® Dentaid system and a citric based mouthwash.

Start Date01 Jan 2013

Sponsor / Collaborator

Dentaid SL

[+1]

NCT01620268

/ TerminatedPhase 2

An Open-Label, Phase 2 Study to Treat Patients With Renal Allograft and Polyoma BK Viruria to Prevent Polyoma BK Viremia, Polyoma BK Nephropathy and Renal Allograft Rejection

This study will evaluate the clinical efficacy and safety of a combination of leflunomide and orotic acid in kidney transplant patients with high levels of Polyoma BK viruria for the purpose of preventing Polyoma BK viremia and Nephropathy that could lead to kidney transplant loss from viral damage, acute rejection or both.

Start Date01 Jul 2012

Sponsor / Collaborator

Suzhou Changzheng Cinkate Pharmaceutical Co., Ltd.

NCT00778284

/ CompletedNot Applicable

Comparative, Randomized, Single-Dose, 2-Way Crossover Bioavailability Study of Ranbaxy and GlaxoSmithKline (Augmentin®) 400 mg Amoxicillin (as the Trihydrate)/57 mg Clavulanic Acid (as the Potassium Salt) Chewable Tablets in Healthy Adult Volunteers Following Administration of a Two Tablet Dose Under Fed Conditions

The objective of this study was to compare the single-dose relative bioavailability of Ranbaxy and GlaxoSmithKline (Augmentin®) 400 mg amoxicillin (as the trihydrate) and 57 mg clavulnic acid (as the potassium salt) chewable tablet, following administration of 2 tablet dose under fed conditions

Start Date01 Oct 2002

Sponsor / Collaborator

Ranbaxy Laboratories Ltd.

100 Clinical Results associated with Oxolinic Acid

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100 Translational Medicine associated with Oxolinic Acid

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100 Patents (Medical) associated with Oxolinic Acid

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2,478

Literatures (Medical) associated with Oxolinic Acid

01 May 2025·European Journal of Medicinal Chemistry

Design, synthesis, and antitumor activity of NSDs inhibitors targeting lung squamous cell carcinoma

Article

Author: Jia, Zhenyu ; Sun, Xiaojiao ; Wang, Zhiqi ; Xiu, Siyu ; Liu, Zhenming ; Chi, Xiaowei ; Liu, Huiyu ; Zhang, Liangren ; Shi, Cheng ; Zhang, Xiangyu

Lung squamous cell carcinoma (LUSC), a highly aggressive subtype of lung cancer, presents significant therapeutic challenges due to its complex molecular underpinnings. Recently, NSD3 has been identified as a key driver in the pathogenesis of LUSC, providing a new direction for targeted interventions. Herein, we report the rational design, synthesis, and comprehensive biological evaluation of a series of NSD3 inhibitors, culminating in the identification of compound A8, which demonstrates potent inhibitory activity against NSD3 and LUSC cell proliferation, with an IC₅₀ of 0.355 μM in NCI-H1703 cells, and less toxicity to non-cancerous HEK293T cells. Cellular thermal shift assays confirmed the binding affinity of compound A8 for NSD3, promoting protein stabilization. Mechanistic investigations revealed that compound A8 induces apoptosis in LUSC cells in a dose-dependent manner and exhibits significant antitumor effects in both in vitro and in vivo models. Notably, compound A8 displayed favorable pharmacokinetic properties and efficaciously suppressed tumor growth in an NCI-H520 xenograft mouse model without observable adverse effects. These findings collectively establish compound A8 as a promising candidate for the development of targeted therapies against LUSC, highlighting the therapeutic potential of NSD3 inhibition.

11 Apr 2025·ACS ES&T Water

Riverine Suspended Particulate Matter as a Hotspot of Antibiotics in the Yellow River Delta, China: Occurrence, Distribution, and Main Drivers

Author: Zhang, Yuxuan ; Shi, Bing ; Wang, Huawei ; Yuan, Zhen ; Reguyal, Febelyn ; Zhang, Shuxiang ; Liu, Ruizhi ; Wang, Kun

This study systematically elucidated the spatiotemporal distributions, partitioning behaviors, and environmental risks of 46 antibiotics in water and the suspended particulate matter (SPM) in the Yellow River Delta.Totally, 12 and 18 antibiotics were pervasively detected in water and SPM in two seasons, contributed predominantly by fluoroquinolones and followed by tetracyclines and sulfonamides.The total antibiotic concentrations displayed significant spatial and seasonal variations in water (151-4.72 x 10³ ng/L), with a higher concentration observed in estuaries in spring, resulting from varying consumption patterns, external pollution emissions, and natural attentions.The spatiotemporal trends in SPM (118-8.84 x 10³ ng/g) were parallel with water, indicating SPM served as a critical sink and an internal pollution source of antibiotics, when hydrodynamic conditions changed.The dominant occurrence of fluoroquinolones and several tetracyclines and sulfonamides in SPM suggested that the partitioning coefficient (Kd) was an important indicator to determine antibiotic sorption potentials onto SPM, which were associated with the differences in the physicochem. properties of antibiotics and SPM and water chem.Environmental risk assessment revealed cinoxacin and enoxacin universally exhibited potential risks for the ecosystem and resistance development from medium to high, and special attention should be given to the high joint risks of the co-occurrence of multiple antibiotics in the Yellow River Delta.

01 Apr 2025·Journal of Environmental Management

Hydrological connectivity and dissolved organic matter impacts nitrogen and antibiotics fate in river-lake system before and after extreme wet season

Article

Author: Tang, Wenzhong ; Song, Yuanmeng ; Zhang, Lulu ; Zhao, Yu ; Cui, Jiansheng

The impact and mechanism of hydrological connectivity and dissolved organic matter on the fate of nitrogen and antibiotics are still lack off in a river-lake connected system under climate extreme events. This study examined the fate of NO₃^--N, 38 antibiotics, and dissolved organic matter (DOM) in Baiyangdian Basin, through dry and wet seasonal (after extreme rainfall) samplings at 2023. In the system, NO₃^--N and ∑antibiotics average concentrations were higher in the dry season, while the relative abundance of humic-like components was higher in the wet season. Spatial autocorrelation analysis showed that the high-high clusters of pollutants and DOM components were mainly distributed in rivers, and the temporal difference was significant. MixSIAR and PMF model were respectively applied to nitrogen and antibiotics sources apportionment. The results showed that non-point sources (NPS) of nitrogen and antibiotics exhibited an upward trend, while the point sources decreased from dry to wet seasons. Hydrological connectivity was characterized by using δ¹⁸O-H₂O, which was higher in the wet season. Partial least squares path model revealed that hydrological connectivity directly impacted humic-like components, which were the direct influencing factor of the concentration and NPS for antibiotics and nitrogen in the connected system. Extreme rainfall weaken the impact of hydrological connectivity on the concentration and NPS of pollutants, while enhanced the impact of humic-like components on pollutants NPS. These findings clarified the impact mechanism of hydrological connectivity and DOM on nitrogen and antibiotics fate in the connected system, which plays an important role in future water quality management under extreme events.

100 Deals associated with Oxolinic Acid

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