Pharmaron’s Post

Join us for our next virtual chemistry lecture on Thursday, July 4, 2024, at 9:15 am (China Standard Time). 𝗦𝗲𝗹𝗲𝗰𝘁𝗶𝘃𝗲 𝗙𝘂𝗻𝗰𝘁𝗶𝗼𝗻𝗮𝗹𝗶𝘇𝗮𝘁𝗶𝗼𝗻 𝗼𝗳 𝗣𝘆𝗿𝗶𝗱𝗶𝗻𝗲𝘀, 𝗗𝗶𝗮𝘇𝗶𝗻𝗲𝘀 𝗮𝗻𝗱 𝗣𝗵𝗮𝗿𝗺𝗮𝗰𝗲𝘂𝘁𝗶𝗰𝗮𝗹𝘀 𝘃𝗶𝗮 𝗨𝗻𝗰𝗼𝗻𝘃𝗲𝗻𝘁𝗶𝗼𝗻𝗮𝗹 𝗜𝗻𝘁𝗲𝗿𝗺𝗲𝗱𝗶𝗮𝘁𝗲𝘀 Prof. Andy McNally Department of Chemistry Colorado State University Register for the webinar: https://lnkd.in/dKdJXAdc Pyridines and diazines are ubiquitous in pharmaceuticals and agrochemicals, yet there are limits in synthetic methods that can directly functionalize the C–H bonds in these structures. In this lecture, Prof. Andy McNally will show two distinct approaches, using phosphorus and ring-opened intermediates, that enable selective functionalization of these heterocycles into a range of valuable derivatives. A range of C–C and C–Heteroatom bond formations are viable, and the chemistry functions on structures typically encountered in drug discovery programs. Prof. McNally's lab has also performed mechanistic and computational studies of the regioselectivity of these reactions and the phosphorus ligand-coupling processes involved.

Excited to announce the publication of our review article in RSC Advances. This article, titled "Exploring the latest trends in chemistry, structure, coordination, and diverse applications of 1-acyl-3-substituted thioureas: a comprehensive review" is focused on providing an overall picture of research conducted in the field of acyl thioureas in previous two years. Grateful for the support and collaboration from my co-authors and mentors. Looking forward to engaging with fellow researchers and professionals who are passionate about organic synthesis focused on biological applications. Read the full article here: https://lnkd.in/dWbNPh37 #Research #Publication #OrganicChemistry #Pharmaceuticals #ScientificCommunity

Publication of the Day 📚 "Chemo-, regio- and enantioselective hydroformylation of trisubstituted cyclopropenes: access to chiral quaternary cyclopropanes" from Nature Communications (open access !). 📌 Method Explanation ⚗ This study presents an innovative method for the chemo-, regio-, and enantioselective hydroformylation of trisubstituted cyclopropenes. Serious mechanistics studies have been done as well alongside other post reaction extra synthetic steps. Advantages of the Method ➕ -Chemo-, regio-, and enantioselectivity - Versatile Applications : The chiral quaternary cyclopropanes produced are crucial intermediates for complex molecule synthesis, particularly in medicinal chemistry. - This hydroformylation process is efficient and can be applied to a wide range of trisubstituted cyclopropenes, showcasing its versatility and practicality. At NUVISAN The Science CRO, our team of synthetic chemists is equipped with a deep understanding of cutting-edge methodologies and decades of experience to provide unparalleled support in API synthesis and analytical troubleshooting. #Chemistry #OrganicChemistry #Hydroformylation #Cyclopropanes #Pharmaceuticals #Research #Nuvisan #DrugDevelopment

Drugging more enzymes in KRas's family Researchers discover a druggable cryptic pocket in guanosine triphosphate-binding proteins However, the present study is still biased toward chemical space optimized to target K-Ras(G12C). New chemical space and the discovery of novel types of reversible high-affinity scaffolds for other GTPases requires a concerted medicinal chemistry campaign that lies beyond the scope of this initial study. https://lnkd.in/gZA3tdMB https://lnkd.in/gTVWJ6iJ

Chemistry can be complex but even so its elegance has always fascinated me. I have recently started an Instagram account celebrating the ingenuity and the hard work of the researchers involved in developing the syntheses in both an academic or industrial environment. Each week on (Synthesis) Monday, a new project will be shown and its features highlighted. This week's contribution comes from the Merck process chemistry department, in which their approach to the anti-migraine API Ubrogepant is discussed. Come check out the Art of Synthesis! https://lnkd.in/e8ht3tUe #OrganicChemistry #Chemistry #Synthesis #Science #Research #organicsynthesis #SynthesisMonday #ProcessDevelopment #ProcessChemistry #API #Pharma #Merck

Clickable Polysaccharides: Click Chemistry behind Biomedical Polysaccharides . Mohammad Reza Saeb Department of Pharmaceutical Chemistry, Gdański Uniwersytet Medyczny (Medical University of Gdańsk), Poland . Mohsen Khodadadi Yazdi, S. Mohammad Sajadi, Farzad Seidi, Navid Rabiee, Yousef Fatahi, Mohammad Rabiee, Payam Zarrintaj, Krzysztof Formela, Mohammad Reza Saeb, Sidi A. Bencherif . In chemical synthesis, "Click Chemistry" is a class of simple, atom-economy reactions commonly used for joining two molecular entities of choice. As a powerful method, it allows for specific and controllable bio-orthogonal reactions to make complex molecular structures with a high level of specificity, selectivity, and yield under mild conditions. Several innovative target-oriented polysaccharides are obtained via "Click Chemistry", which are thoroughly summarized, reviewed and discussed in this paper, published in Progress in Polymer Science (PPS). PPS is a peer-reviewed scientific journal publishing review articles on topics broadly related to polymer chemistry. The 2022 impact factor of this journal was 27.1, ranking it the highest in the subject category "Polymer Science". . #Biomaterials #clickchemistry #biomedicalengineering #tissueengineering #drugdelivery #polysaccharide #cellgrowth #mohammadrezasaeb #polymer

Thrilled to announce the publication of the first article in our special issue honoring the 75th birthday of Prof. B. C. Ranu. This paper, titled "Metal-Free Synthesis of C-3-Alkoxycarbonylated 2H-Indazoles Using Alkyl Carbazates," (https://lnkd.in/gBeeAcmV) authored by a talented team led by Dr. Alakananda Hajra, this work describes a novel, environmentally friendly approach to the direct C-3 functionalization of indazoles - an important class of heterocycles with broad pharmaceutical applications. Using a simple, metal-free protocol, the researchers were able to access a diverse array of C-3 carboxylic ester-derived indazoles in good to excellent yields. This is just the first of many insightful contributions that will be featured in this special issue. If you have been working in green chemistry, there is still time to submit your manuscript. The deadline for submissions is June 30, 2024. Don't miss out on this opportunity to be part of this commemorative volume. Submit your paper today! https://lnkd.in/dNUPm7KY #Synlett #SpecialIssue #BirthdayHonor #OrganicChemistry #Indazoles #FunctionalMaterials

Discover Novel Bioactive Compounds with Enamine’s Pseudo-Natural Products! Dive into the groundbreaking research on pseudo-natural products (PNPs) published in the RSC Medicinal Chemistry journal. This pivotal study, "Identification of Readily Available Pseudo-Natural Products," by Axel Pahl, Oleksandr Grygorenko, Ivan Kondratov, and Herbert Waldmann, reveals how Enamine’s extensive library of synthetic small molecules offers a treasure trove of structurally unique PNPs.  ▪ Vast Collection: Immediate access to diverse PNPs combining natural product fragments in novel ways; ▪ Advanced Tools: Utilized an improved NPFC tool to classify and analyze PNPs, revealing significant bioactivity potential; ▪ Efficient Discovery: Enamine’s library accelerates the discovery of novel chemotypes, providing a cost-effective alternative to traditional synthesis. Enamine’s PNPs can revolutionize drug discovery, enhancing the potential for finding new bioactive compounds and supporting innovative research. Read more https://lnkd.in/d4KSz6CU More about Enamine Compound Libraries https://lnkd.in/dbjfQaz8

Happy to share my another published research article in Royal Society of Chemistry (Analyst) entitled " A copper metal–organic framework-based electrochemical sensor for identification of glutathione in pharmaceutical samples" The article details how Mof materials can be sensibly used, particularly through the use of electrochemical techniques. These techniques are well-known today due to their selectivity, sensitivity, repeatability, and—perhaps most astonishing of all—low detection limits. For a deeper understanding of these and other qualities, please read the article, which provides a brief description of the technique. Authors: Dr. Reshma Kaimal , Ashutosh Dubey , Jerry. J. Wu, @Abdullah Al Sauwaileh, Sambandam Anandan . My speciale thanks to Dr. Reshma Kaimal and Sambandam Anandan for all the support and guidance during my master's thesis project #mof #metalorganicframeworks #electrochemistry #research #researchanddevelopment #researchpaper #researchopportunity #researchpublication #researchcollaboration #researchwriting #materialsscience #materialsresearch #materialcharacterization #materials #sensing #phdposition #phdstudent #phdresearch #phdopportunity #phdscholarship #phdjobs #phdprogram #europe #europetravel #phdsupport #abroadeducation #abroadstudies #abroadstudyvisa #abroadjobs #glutathione #electrodes #batteries #supercapacitors #batterytechnology #phdposition #phdopportunity #phdscholarship

Protein #NMR, isotope labeling and chemical shift calculations form the basis for a rapid and efficient structure optimization process of initial low-affinity binders. A recent research article published in the Journal of Medicinal Chemistry presents the latest findings from a collaborative project involving the University of Vienna, Boehringer Ingelheim, and MAG-LAB, with financial support from the Christian Doppler Society. This innovative method employs protein NMR spectroscopy, combined with aliphatic residue methyl labeling to directly measure CH-hydrogen bonding interactions. The resulting data on ligand-protein complex geometries helps to understand the residual mobility of ligands within their binding pockets, indirectly reflecting binding energies. These insights enable medicinal chemists to make well-informed decisions during accelerated structure optimization processes, even in the absence of protein-ligand cocrystal structures. Read the full story in the open access article: https://lnkd.in/dNfVS8fu