The antimicrobial effectiveness of five phenothiazine derivatives, namely A, B, C, D and E, was examined against three Gram-pos. and three Gram-neg. bacteria, as well as seven fungal species.Anal. of the gathered data revealed that all derivatives exhibited strong antibacterial properties.However, their performance as antifungal agents were comparatively less effective which may be attributed to cell structure of fungi.Notably, in several instances, the activity of the phenothiazine derivatives surpassed that of the reference drug penicillin 10.Furthermore, mol. docking studies provided addnl. evidence of the ability of these four derivatives to bind with the target enzyme PBP2a.The docking scores obtained ranged from -11.27 to -15.90 Kcal/mol.According to pharmacokinetics and ADME study, all phenothiazine derivatives A-E, as well as Penicillin 10, have a bioavailability higher than zero, ranging between 0.17 and 0.55.Phenothiazine derivative A is similar to the reference drug penicillin 10, indicating that it is the most bioactive.

17 Jan 2025·The Journal of Organic Chemistry

O₂-Mediated Cu-Catalyzed Dehydrogenative Phenothiazination

Article

Author: Patureau, Frederic W. ; Xiao, Fang ; Oppel, Iris M. ; Ebel, Ben ; Wang, Xingben

In contrast to what one can be led to believe upon inspecting some of the recent literature, the dehydrogenative phenothiazination reaction does not require onerous technologies, complicated setups, or advanced catalysts in order to be mild and sustainable. We demonstrate this herein with a most facile, cost-effective, and sustainable Cu(II) catalyzed method, under 1 atm of O₂ at room temperature in methanol, providing broad scope and high yields. These new results further set the dehydrogenative phenothiazination reaction among the green and practical coupling concepts of chemistry.

31 Dec 2024·Journal of Enzyme Inhibition and Medicinal Chemistry

Synthesis and biological evaluation of ortho -phenyl phenylhydroxamic acids containing phenothiazine with improved selectivity for class IIa histone deacetylases

Article

Author: Hsu, Kai-Cheng ; Huang, Wei-Jan ; Chu, Jung-Chun ; Huang, Yu-Wen ; Hu, Jing-Lan ; Yen, Shih-Chung ; Lin, Tony Eight ; Weng, Jing-Ru ; Huang, Yun-Yi

Class IIa histone deacetylases (HDACs) have been linked to tumorigenesis in various cancers. Previously, we designed phenylhydroxamic acid LH4f as a potent class IIa HDAC inhibitor. However, it also unselectively inhibited class I and class IIb HDACs. To enhance the compound's selectivity towards class IIa HDACs, the ortho-phenyl group from the selective HDAC7 inhibitor 1 is incorporated into ortho position of the phenylhydroxamic acid in LH4f. Compared to LH4f, most resulting compounds displayed substantially improved selectivity towards the class IIa HDACs. Notably, compound 7 g exhibited the strongest HDAC9 inhibition with an IC₅₀ value of 40 nM. Molecular modelling further identified the key interactions of compound 7 g bound to HDAC9. Compound 7 g significantly inhibited several human cancer cells, induced apoptosis, modulated caspase-related proteins as well as p38, and caused DNA damage. These findings suggest the potential of class IIa HDAC inhibitors as lead compounds for the development of cancer therapeutics.

100 Deals associated with ML-171

R&D Status

10 top R&D records.

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Discovery	Italy	University of Salerno	31 Aug 2023

Clinical Result

Indication

Phase

Evaluation

View All Results

Translational Medicine

Boost your research with our translational medicine data.

view full example data

Deal

Boost your decision using our deal data.

view full example data

Core Patent

Boost your research with our Core Patent data.

view full example data

Clinical Trial

Identify the latest clinical trials across global registries.

view full example data

Approval

Accelerate your research with the latest regulatory approval information.

view full example data

Regulation

Understand key drug designations in just a few clicks with Synapse.

view full example data

Chat with Hiro

Get started for free today!

Accelerate Strategic R&D decision making with Synapse, PatSnap’s AI-powered Connected Innovation Intelligence Platform Built for Life Sciences Professionals.

Start your data trial now!

Synapse data is also accessible to external entities via APIs or data packages. Empower better decisions with the latest in pharmaceutical intelligence.

Bio

Bio Sequences Search & Analysis

Chemical

Chemical Structures Search & Analysis


No Data

ML-171

Overview

Basic Info

Structure/Sequence

Related

R&D Status

Clinical Result

Translational Medicine

Deal

Core Patent

Clinical Trial

Approval

Regulation