AMRI Global

Albany, NY, United States

AMRI Global

Albany, NY, United States
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Ho G.D.,Merck Research Laboratory | Tulshian D.,Merck Research Laboratory | Bercovici A.,Merck Research Laboratory | Tan Z.,Merck Research Laboratory | And 12 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. Compound 41 displayed anti-nociceptive efficacy in the rat CFA pain model at 100 mpk oral dosing. © 2014 Elsevier Ltd. All rights reserved.


PubMed | Cardiorenal Group, Merck Research Laboratory, In Vivo Pharmacology Group and AMRI Global
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2014

A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. Compound 41 displayed anti-nociceptive efficacy in the rat CFA pain model at 100 mpk oral dosing.


Grant
Agency: GTR | Branch: EPSRC | Program: | Phase: Training Grant | Award Amount: 5.27M | Year: 2014

The traditional PhD programme begins with a student seeking out a PhD position early on in their final year of undergraduate study. The time elapsed between a student choosing their project and actually starting is generally between 6-8 months - can a student really be sure that the right choice has been made under these circumstances? This choice is probably the most important decision an aspiring professional researcher can make, yet students can make ill informed, naive or simply unsuitable PhD choices based on their perceived interests and limited research experience. Bristol Chemical Synthesis (BCS) is a Centre for Doctoral Training (CDT) that offers a different and much enhanced PhD training experience to the traditional path. Crucially, students join the Centre in October but do not choose their PhD research project until 7-months later. Students spend these 7-months completing a unique, multifaceted training period called Postgraduate Advanced Chemical Techniques (PACT). The over-arching goal of PACT is to equip the students with the tools required to make the best-informed PhD project choice, to develop a creative attitude towards problem solving and to build self-confidence with presentations and by speaking publicly. PACT also provides a formal assessment mechanism before students progress to their PhD projects. Brainstorming involves the students generating ideas on outline research proposals which they then present to the staff members in a lively and engaging feedback session, which invariably sees new and student-driven ideas emerge. By encouraging teamwork and presentation skills, as well as allowing students to become fully engaged with the projects and staff, brainstorming ensures that students take control of a PhD proposal before they start - Partners not Slaves is our vision. Research Broadening Sabbaticals comprise three successive 7-week lab rotations designed to include a period of known work, enabling the student to practice new skills required for further research. Rotations are important in giving students the opportunity to learn new techniques beyond their undergraduate experience, providing them with time to consider and reflect on their choice of PhD by offering tasters in different areas of synthetic chemistry. Dynamic Laboratory Manual (DLM) enabled experiments allow students to experience an interactive, virtual version of an essential experimental technique. Pioneered at the undergraduate level at Bristol, DLMs consist of a mixture of simulations, videos, tutorials and quizzes to allow the student to gain a full understanding of a technique and learn from mistakes quickly, effectively and safely before entering the lab. Chemical Synthesis is an area upon which much of modern society relies as it enables the customised fabrication of products that are the essential materials of our daily lives. Examples are wide and diverse from vital life saving drugs to the chromic materials that make your iPad screen change in an instant. There are 15 key UK industry sectors in which chemistry is an essential component, employing over 5 million people and contributing £258bn (21%) to the UKs GDP. Pharma, agrochem, petrochem, fine & bulk chemical manufacturing and CRO industries are major players in these industries and UK competitiveness here is unsustainable without the continued supply of highly trained & skilled chemical synthesis PhD graduates. Our Centre will train the next generation of synthetic chemistry architects equipped to solve the diverse molecular problems of the future.


Voss M.E.,AMRI Global | Rainka M.P.,AMRI Global | Fleming M.,AMRI Global | Peterson L.H.,AMRI Global | And 6 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2012

The structure-activity relationships of new Aurora A/B kinase inhibitors derived from the previously identified kinase inhibitor 12 are described. Introduction of acetic acid amides onto the pyrazole of compound 12 was postulated to influence Aurora A/B selectivity and improve the profile against off-target kinases. The SAR of the acetic acid amides was explored and the effect of substitution on enzyme inhibition as well as mechanism-based cell activity was studied. Additionally, several of the more potent inhibitors were screened for their off-target kinase selectivity. © 2012 Elsevier Ltd. All rights reserved.


PubMed | AMRI Global
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2012

The structure-activity relationships of new Aurora A/B kinase inhibitors derived from the previously identified kinase inhibitor 12 are described. Introduction of acetic acid amides onto the pyrazole of compound 12 was postulated to influence Aurora A/B selectivity and improve the profile against off-target kinases. The SAR of the acetic acid amides was explored and the effect of substitution on enzyme inhibition as well as mechanism-based cell activity was studied. Additionally, several of the more potent inhibitors were screened for their off-target kinase selectivity.

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