Delving into the Latest Updates on Tydock Pharma Srl with Synapse

Overview

Author: Kuzikov, Maria ; Santarem, Nuno ; Freitas-Junior, Lucio ; Lane, Thomas R. ; Ekins, Sean ; Foil, Daniel H. ; Wittig, Ulrike ; Mueller, Wolfgang ; Ellinger, Bernhard ; Gul, Sheraz ; Costi, Maria Paola ; Zorn, Kimberley M. ; Reinshagen, Jeanette ; Cordeiro da Silva, Anabela ; Luciani, Rosaria ; Tonelli, Michele ; Venturelli, Alberto ; B Moraes, Carolina ; Ferrari, Stefania ; Santucci, Matteo ; Quotadamo, Antonio ; Linciano, Pasquale

Broad-spectrum anti-infective chemotherapy agents with activity against Trypanosomes, Leishmania, and Mycobacterium tuberculosis species were identified from a high-throughput phenotypic screening program of the 456 compounds belonging to the Ty-Box, an in-house industry database. Compound characterization using machine learning approaches enabled the identification and synthesis of 44 compounds with broad-spectrum antiparasitic activity and minimal toxicity against Trypanosoma brucei, Leishmania Infantum, and Trypanosoma cruzi. In vitro studies confirmed the predictive models identified in compound 40 which emerged as a new lead, featured by an innovative N-(5-pyrimidinyl)benzenesulfonamide scaffold and promising low micromolar activity against two parasites and low toxicity. Given the volume and complexity of data generated by the diverse high-throughput screening assays performed on the compounds of the Ty-Box library, the chemoinformatic and machine learning tools enabled the selection of compounds eligible for further evaluation of their biological and toxicological activities and aided in the decision-making process toward the design and optimization of the identified lead.

01 Aug 2019·Journal of Pharmaceutical and Biomedical AnalysisQ3 · MEDICINE

A new strategy based on microwave-assisted technology for the extraction and purification of beeswax policosanols for pharmaceutical purposes and beyond

Q3 · MEDICINE

Article

Author: Brighenti, Virginia ; Venturelli, Alberto ; Mascolo, Danilo ; Pellati, Federica

Policosanols (PCs) are a mixture of long chain primary aliphatic alcohols mainly known for their ability to reduce cholesterol level. Due to this property, there is an increasing interest in the extraction process of these compounds. In this context, beeswax, a natural product produced by honey bees of the genus Apis, is a promising source for their extraction and purification. The present research work was aimed at the development of a new procedure for the extraction and purification of PCs from yellow beeswax by using microwave-assisted technology, which hitherto has never been applied to this mixture. The developed process comprises three main steps: 1) microwave-assisted trans-esterification; 2) microwave-assisted hydrolysis; 3) final purification by means of preparative liquid chromatography. The final step is responsible for the increased purity of PCs, thanks to the removal of undesired compounds, such as natural paraffins. The predominant alcohols investigated in this work are tetracosanol (C₂₄OH), hexacosanol (C₂₆OH), octacosanol (C₂₈OH), triacontanol (C₃₀OH) and dotriacontanol (C₃₂OH). Compound identification was performed using GC-EI-MS, while GC-FID analysis was chosen for the quantification of the main fatty alcohols present in the product. This new method represents a useful tool for the production of PCs from beeswax to be used in pharmaceuticals and nutraceuticals for human use, feed and veterinary supplements.

24 Apr 2019·ChemistrySelect

Optimization of N‐alkylation in the Synthesis of Methotrexate and Pteridine‐based Derivatives Under Microwave‐Irradiation

Author: Costi, Maria Paola ; Quotadamo, Antonio ; Venturelli, Alberto ; Linciano, Pasquale

AbstractMethotrexate (MTX) and its pteridine‐based derivatives represent an attractive chemotype for the development of bioactive molecules. However, the synthesis of pteridines suffers from several drawbacks. Here we describe a new efficient and improved microwave‐assisted lab‐scale process for the preparation of MTX and congeners. Starting from the commercially available 2,4‐diamino‐6‐(hydroxymethyl)pteridine (Pt‐OH), MTX was obtained with an overall 94% yield through a three steps procedure. The crucial yield‐limiting and time‐consuming step of SN2 substitution between halogenated pteridine and nucleophilic aromatic amine was taken. The innovative process, conducted under microwave irradiation, improved yield and purity, and in particular reduced the reaction time from days to 20 minutes. The optimized protocol was successfully applied to the synthesis of diverse pteridine‐based derivatives and to the preparation in gram‐scale of antiparasitic MTX derivatives for in vivo studies. This new optimized synthetic procedure therefore represents a worthy alternative to the current protocols for the preparation of pteridine‐based derivatives.

100 Deals associated with Tydock Pharma Srl

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100 Translational Medicine associated with Tydock Pharma Srl

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Pipeline

Pipeline Snapshot as of 20 May 2025

The statistics for drugs in the Pipeline is the current organization and its subsidiaries are counted as organizations,Early Phase 1 is incorporated into Phase 1, Phase 1/2 is incorporated into phase 2, and phase 2/3 is incorporated into phase 3

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