Delving into the Latest Updates on F-10(China Pharmaceutical University) with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

F10

Target

ATPase x Tubulin

Action

inhibitors

Mechanism

ATPase inhibitors(ATPase inhibitors), Tubulin inhibitors

Therapeutic Areas

Neoplasms

Active Indication

Neoplasms

Inactive Indication-

Originator Organization

China Pharmaceutical University

Active Organization

China Pharmaceutical University

Inactive Organization-

License Organization-

Drug Highest PhaseDiscovery

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC20H17BrN2O5

InChIKeyALRSOLQVKXGWII-UHFFFAOYSA-N

CAS Registry-

To continue our development of novel N-phenyltriazinone herbicides, a series of N-phenyltriazinone derivatives containing 5,6-dihydro-4H-1,2-oxazine or oxime fragments were designed and synthesized based on intermediate derivatization approach using ring expansion and ring opening strategies. Nicotiana tabacum PPO (NtPPO) activity assay showed that most of the compounds showed strong inhibition to NtPPO. Among them, compound F10 (K_i = 28.9 nM) exhibits good inhibitory effect on NtPPO comparable to that of triflurazine (K_i = 30.7 nM). Systematic postemergence herbicidal activity evaluation found that F10 had excellent herbicidal activity, with over 90% control effect on six weed species (Echinochloa crusgalli, Eleusine indica, Setaria faberii, Abutilon juncea, Amaranthus retroflexus, and Portulaca oleracea) at 37.5 g a.i./ha. Moreover, it caused only 20-40% damage to rice, maize, peanuts, and wheat at 75-150 g a.i./ha, which was significantly safer than trifludimoxazin (60-100%). Molecular simulations showed that compound F10 formed two hydrogen bonds with Arg98 of NtPPO. Density functional theory (DFT) calculations indicated that F10 showed high chemical reactivity and electronic chemical potential. The present study demonstrates that compound F10 holds significant potential as a promising PPO inhibitor and it offers a novel approach for the development of efficient and broad-spectrum herbicides through an intermediate derivatization strategy.

01 Mar 2025·PEST MANAGEMENT SCIENCE

Sulfone derivatives containing an oxazole moiety as potential antibacterial agents: design, synthesis, antibacterial activity, and mechanism

Article

Author: Chen, Jixiang ; Liu, Xing ; Zou, Yue ; Zhu, Mei ; Zhang, Yong ; Zhu, Zongnan

Abstract:

BACKGROUND:

Bacterial diseases in plants pose a serious threat to crop production, leading to substantial food loss every year. Prolonged and repeated use of a single antibacterial agent can promote resistance in pathogenic bacteria. Therefore, there is an urgent need to develop efficient antibacterial agents for the treatment of bacterial diseases.

RESULTS:

Sulfone derivatives containing an oxazole moiety were designed and synthesized. Subsequently, their biological activities were evaluated. The half‐maximal effective concentration (EC50) value of compound F10 against Xanthomonas oryzae pv. oryzicola (Xoc) was 1.1 mg/L, which was higher than those of commercial antibacterial agents, thiodiazole‐copper (91.5 mg/L) and bismerthiazol (76.0 mg/L). The curative and protective effects of compound F10 against bacterial leaf streak in rice were 43.8% and 48.4%, respectively, at 200 mg/L, which were significantly superior to those of thiodiazole‐copper (25.0% and 25.8%, respectively) and bismerthiazol (31.3% and 38.7%, respectively). Compound F10 inhibits Xoc by increasing the permeability of the cell membrane, inhibiting the production of extracellular polysaccharides, and affecting flagellar movement on the cell membrane. In addition, F10 reduces the pathogenicity of pathogenic bacteria, induces the accumulation of reactive oxygen species (ROS) in pathogenic bacteria, and produces adverse reactions. Compound F10 weakens bacterial pathogenicity by affecting the signal transduction of plant hormones, programmed cell death, and enhancing the ability to resist infection through the autoimmune response of rice.

CONCLUSION:

01 Feb 2025·Recent Patents on Nanotechnology

Formulation Optimization and Characterization of Solid Lipid Nanoparticles of Apixaban

Article

Author: Hegde, Namita ; Mulay, Laukik ; Kanugo, Abhishek

Background::

Unpredictable situations such as clotting of blood, deep vein thrombosis, and pulmonary embolism arise in the body, which is the leading cause of mortality. Such conditions generally arise after surgery as well as after treatment with oral anticoagulant agents. Apixaban is a novel oral anticoagulant widely recommended for the prevention and treatment of strokes and blood clots suffering from nonvalvular atrial fibrillation by suppressing factor Xa. Apixaban has a log P of 2.71 with poor solubility and reported maximum bioavailability of approximately 50%.

Objective::

Hence, the current research mainly focused on the improvement of solubility, bioavailability, and therapeutic efficacy of Apixaban via solid lipid nanoparticles (SLN).

Methods::

The SLN was developed using the hot-homogenization method using a high-pressure homogenizer. The drug-lipid compatibility study was assessed by the FTIR, and the thermal analysis was performed using differential scanning calorimetry (DSC). During the scrutiny of lipids, the highest solubility of Apixaban was estimated in the glyceryl monostearate, hence selected for the formulation. Moreover, the colloidal solution was stabilized by the polyethylene glycol 200. The Design of Expert software (Version 13, Stat-Ease) was implemented for the optimization analysis by considering the 3-independent factors and 2-dependent parameters. The Patents on the SLN are Indian 202321053691, U.S. Patent, 10,973,798B2, U.S. Patent, U.S. Patent 2021/0069121A1, U.S. Patent 2022/0151945A1.

Results::

Box-Behnken design was applied along with ANOVA, which showed a p-value less than 0.05 for the dependent parameters such as particle size and entrapment efficiency (p-value: 0.0476 and 0.0379). The optimized batch F10 showed a particle size of 167.1 nm, -19.5 mV zeta potential, and an entrapment efficiency of 87.32%. The optimized batch F10 was lyophilized and analyzed by Scanning electron microscopy (SEM), which showed a particle size of 130 nm. The solid powder was filled into the capsule for oral delivery.

Conclusion::

The marked improvement in solubility and bioavailability was achieved with F10- loaded Apixaban via Solid lipid nanoparticles. Moreover, the sustained released profile also minimizes the unseen complications that occur due to the clotting of blood.

100 Deals associated with F-10(China Pharmaceutical University)

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