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A housane that our chemists built

Housane-News

A diastereoselective approach to cis- and trans-1,3-disubstituted bicyclo[2.1.0]pentanes (housanes) was recently reported by our chemists in The Journal of Organic Chemistry. The article included preparation of 35 derivatives on up to 100 g scale. Moreover, pKa’s and conformational features of selected examples of housanes (e.g. GABA analogues) were also studied and compared to that of the corresponding 1,3-disubstituted cyclopentanes. For an extended list of novel housanes check the Enamine Store page.

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Paper by Enamine chemists is featured on the JOC cover

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EDF在线老虎机In a recent JOC paper, Enamine chemists reported a comprehensive study of regioselective [3 + 2] cycloaddition reactions – an efficient approach towards 3,5-disubstituted isoxazole building blocks bearing mono-, di- or trifluoromethyl substituents. More than 100 derivatives were obtained on up to 130 g scale, and multigram quantities of representative examples are available from EnamineStore at the isoxazole library.

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EDF在线老虎机Introducing alkyl substituent into the piperidine core goes multigram

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Enamine’s EurJOC paper on the scalable and regioselective preparation of all isomeric (cyclo)alkyl piperidines and the corresponding amino alcohols was featured on the cover of the issue. The multigram quantities of these derivatives are available from EnamineStore at the piperidine library

 

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A New Paper by Enamine’s Scientists: "Synthesis and chemical transformations of diazolyl α,α-difluoroacetates"

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Recent Enamine’s paper disclosed novel heteroaryl difluoroacetates and the corresponding carboxylic acids, amides, nitriles and alcohols as promising building block in drug design. Known literature example of metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitor 1 led to the the corresponding 2,2-difluoro-2-pyridin-2-yl derivative 2, which is not prone to metabolic oxidation at the α-methylene group next to the aromatic moiety.

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A New Review Paper by Enamine’s Scientists: "The Symbiotic Relationship Between Drug Discovery and Organic Chemistry”

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EDF在线老虎机The review mentioned in the title was published in Chemistry – A European journal and emerged from a collaboration of scientists from Enamine Ltd. (including myself) and Duncan Judd from Awridian Ltd. Despite some “symbiotic” hype in the title (as it was pointed out by one of the reviewers), the paper provides a comprehensive overview of concepts which appeared at the edge of these disciplines recently. Initially, we have aimed at tutorial review that might help synthetic chemists to become familiar with state-of-the-art in the field. Thus, genesis of concepts like “…-oriented” syntheses (DOS, LOS, BIOS, FOS, DTS), as well as related “abbreviated” strategies (BBs, FBDD, DEL, REAL) has been discussed, together with recent advances focusing mainly on chemical aspects.

 

However, the paper exceeded the initial “tutorial” goal, and in my opinion, it might be of interest not only to beginners in the field, but also to highly qualified specialists in medicinal chemistry and related sciences. Although we attempted to be as neutral as possible, one might feel that we advocated for the compound selection models taking into account physico-chemical properties of the compounds, and hence concepts like lead-oriented-synthesis (LOS). Despite recent criticism and numerous successful exceptions, we believe that if used properly, such strategies might be step at the right direction for early drug discovery. In particular, LOS-like concepts seem to be dominating for building blocks, and majority of the Enamine’s building block collection have been designed by the corresponding criteria such as “the smaller, the better”.

 

The title picture (which was also used as a frontispiece for the paper) shows one of the most beautiful examples of symbiosis found in Nature – a hummingbird pollinating an ornithophilous flower. These two families co-evolved together, changing their features (i.e. the bill shape of the bird, as well as color spectrum and nectar composition of the plant) to get maximum benefit from their interaction. This is a good illustration of the main concept of the paper: similar symbiotic relationship between synthetic organic chemistry and early drug discovery exists.

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"Hot"​ Research Areas in Drug Discovery -- 2019

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Things like gene editing, stem cells, immunotherapies and new types of biologics are now mega-trends in the pharmaceutical industry, widely covered in media, and I guess there is little doubt that biology is the next big thing in medicine. However, in this post I would like to outline several promising areas in small molecule drug discovery, suggesting a lot of untapped potential and investment prospects in this more “traditional” pharmaceutical research space.

 

1.Targeting ribonucleic acid (RNA)

 

The majority of existing marketed drugs out there are designed to somehow modulate proteins in the body, thereby disrupting a disease progression. However, going one step back and trying to disrupt a pathological process earlier -- right before a protein is actually made in the body -- seems a powerful concept. This can be achieved by influencing ribonucleic acid (RNA), a central actor molecule in the process of gene expression -- the one leading to the formation of proteins as instructed by the human genome.

 

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New Building Blocks For Drug Discovery Are Getting Closer: Gem-difluorocyclopropane-derived Amines

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Modern drug discovery relies heavily on the ability of chemists to produce good starting points for producing high-quality lead compounds. Several concepts were established in the last two decades to aim synthetic organic chemistry onto the proper areas of chemical space, in particular, the so-called lead-oriented approach which describes paradigm shift towards low-molecular-weight, relatively hydrophilic, conformationally restricted, sp3-enriched structures.

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Hunting For New Drug Discovery Ideas In The CLOUD

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Patient diversity and developing drug resistance can undermine the efficiency of existing therapies in a long-term pharmacological treatment of diseases, such as cancer and infections。

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The Next Big Thing In The Life Sciences R&D Market: E-Commerce

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(This post originally )

 

Pioneered by expensive and cumbersome legacy electronic data interchange (EDI) systems, the B2B e-commerce market has been evolving, showing a staggering growth rate with a projected volume of  and  by 2020.

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New Opportunities In Covalent Inhibition: Targeting Lysine

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(This post originally )

 

Notoriously toxic, covalent inhibitors have been nearly excluded from major drug discovery programs in the not so distant past。 Ironically, a great amount of the important drugs exploit covalent inhibition as their mechanism of action (MOA)。 The view on covalent inhibitors is shifting towards a wider consideration, however, inspired by recent successes with EGFR inhibitors for treating cancer and many other promising examples。 A recent publication in provides a chemical proteomic platform for the global and quantitative analysis of lysine residues in native biological systems, offering further insights and ideas in this area。

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Artificial Intelligence In Drug Discovery: A Bubble Or A Revolutionary Transformation?

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(This article originally )

 

Artificial intelligence (AI) has become a hot topic in the area of life sciences lately。 With a growing number of groundbreaking AI in other hi-tech industries -- ranging from self-driving cars to speech and image recognition tools to personal assistants (you know Siri, don’t you?) -- players in the biopharmaceutical industry are to speed up drug discovery, cut R&D costs, decrease failure rates in drug trials and eventually create better medicines。

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Expanding Horizons for Fragment Based Drug Discovery (FBDD)

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Scientists estimated that the human genome encodes above 20,000 different proteins in our body. However, available public databases contain records of known ligands for only about 10% of all proteins. The rest of proteins remains either not yet properly explored, or is labelled “undruggable”.

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