DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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Figure 2. a. Fragment-based screening: Small and structurally diverse molecules (circles represent functional groups) are screened for a biological target, and they are combined and modified to generate drug-like compounds. b. Diversity-oriented synthesis: Large collections of structurally diverse and complex molecules are made using a short number of reactions. The resulting compounds are optimized to produce the drug-like compounds. | Credit: P. J. Hajduk,W. R. J. D. Galloway & D. R. Spring Nature, 2011, 470, 42–43. DOI: 10.1038/470042a
The discovery and development of new drugs is a long and expensive process, and despite of it, essential to face present and new diseases. For small molecules, which account for the majority of the marketed drugs, the discovery process generally involves finding a starting point termed hit or lead compound. These molecules have biological activity but need to be optimized to enhance their potency and selectivity (i.e. minimize the toxicity) and improve pharmacokinetic parameters making them suitable to go to the next stage, the pre-clinical tests……….http://mappingignorance.org/2014/07/04/lead-oriented-synthesis-new-concept-aid-drug-discovery-process/
Author
pablo ortiz
PhD at Rijksuniversiteit Groningen
Experience
PhD Student, Rijksuniversiteit Groningen
October 2013 – Present
Asymmetric organometallic catalysis focused on tertiary alcohols and amines
Harutyunyan research group
Master Thesis Project
University of the Basque Country
February 2013 – September 2013 (8 months)Vitoria-Gasteiz Area, Spain
Estereoselective synthesis of quaternary alpha-aminophosphonic acid derivatives (organocatalysis)
Locum pharmacist
Community pharmacy
August 2012 – August 2012 (1 month)La Rioja, Spain
Pre-registration pharmacist
NHS Trust
January 2012 – June 2012 (6 months)Southport, England
In-patient and out-patient dispensing
Clinical pharmacy
Medicines information
Anticoagulant management
Aseptic preparation of medicines
Clinical audit of antimicrobial use
Publications
Tertiary α-diarylmethylamines derived from diarylketimines and organomagnesium reagents(Link)
Chem. Commun. 2015, 51, 703-706.
November 13, 2014
Organomagnesium reagents enable swift and versatile derivatisation of diarylimines to the corresponding α-substituted diarylmethylamines in excellent yields, through fast and clean reactions. Where it occurs, 1,2-reduction can be circumvented using readily accessible dialkylmagnesium reagents.
Asymmetric Synthesis of Functionalized Tetrasubstituted α-Aminophosphonates through Enantioselective Aza-Henry Reaction of Phosphorylated Ketimines(Link)
J. Org. Chem., 2015, 80, 156–164
November 2014
Bifunctional Cinchona alkaloid thioureas efficiently catalyze asymmetric nucleophilic addition of nitromethane to ketimines derived from α-aminophosphonic acids to afford tetrasubstituted α-amino-β-nitro-phosphonates.
Catalytic Asymmetric Alkylation of Aryl Heteroaryl Ketones(Link)
Eur. J. Org. Chem., 2015, 72–76.
November 2014
Tertiary diarylmethanols are highly bioactive structural motifs. A new strategy to access chiral tertiary diarylmethanols through copper-catalyzed direct alkylation of (di)(hetero)aryl ketones by using Grignard reagents was developed. The low reactivity and the similarity of the enantiotopic faces of bis-aromatic ketones were partially overcome, which resulted in moderate to good yields and…more
Synthesis of Tetrasubstituted α-Aminophosphonic Acid Derivatives from Trisubstituted α-Aminophosphonates(Link)
Eur. J. Org. Chem., 2013: 7095–7100
September 2013
Education
Universidad del País Vasco/Euskal Herriko Unibertsitatea
Master’s degree, Synthetic and Industrial Chemistry, 9.2
2012 – 2013
- (Open)1 course
Universidad del País Vasco/Euskal Herriko Unibertsitatea
Bachelor’s degree, Pharmacy, Extraordinary Degree Award, 9.06
2007 – 2012
- (Open)1 honor or award
- (Open)2 courses
Courses
Universidad del País Vasco/Euskal Herriko Unibertsitatea
- How to write and publish a research article
- X Pharmaceutical Chemistry Sessions: New strategies for the design and synthesis of drugs
Universidad del País Vasco/Euskal Herriko Unibertsitatea
- II Organic Chemistry Synthesis and Catalysis Workshop: Methods and strategies in synthesis
GRONINGEN, NETHERLANDS
stadtmitte groningen niederlande stadtwanderung
New Drug Approvals 