PMID- 18409015
OWN - NLM
STAT- MEDLINE
DCOM- 20081001
LR  - 20211020
IS  - 1381-1991 (Print)
IS  - 1381-1991 (Linking)
VI  - 12
IP  - 1
DP  - 2008 Feb
TI  - Emerging approaches for the syntheses of bicyclic imidazo[1,2-x]-heterocycles.
PG  - 1-15
LID - 10.1007/s11030-008-9072-1 [doi]
AB  - Imidazo-[1,2-x]heterocycles are versatile building blocks for use in both a 'drug 
      hunters' quest to discover new leads and a chemical biologists search for 
      effective molecular tools in 'cell perturbation' studies. At the front end of the 
      drug discovery flow chart, the last 5-10 years have witnessed the discovery of 
      new high-throughput methodologies which very quickly have enabled access to 
      virtual libraries of these chemo-types in the realm of 10(7) derivatives. 
      Interestingly, these often neglected cores in patent cooperation treaty (PCT) 
      applications appear in several highly effective marketed drugs, completing the 
      medicinal chemists search for clinical success. Such rigid chemo-types, all 
      containing a bridgehead nitrogen atom, are thus poised for an ever increasing 
      impact on the discovery and development of new molecular therapeutics. The 
      following mini-review will briefly cover therapeutic utility, chemical 
      methodologies and automation developed to enable preparation of arrays of these 
      chemo-types in a high-throughput manner. Synthetic emphasis is placed on a 
      3-component-3-center isocyanide based multi-component reaction (IMCR), which 
      spans solution, solid phase, flourous and microwave assisted organic synthesis.
FAU - Hulme, Christopher
AU  - Hulme C
AD  - Division of Medicinal Chemistry & Organic Chemistry, BIO5 Institute, University 
      of Arizona, Tucson, Arizona, USA. hulme@pharmacy.arizona.edu
FAU - Lee, Yeon-Sun
AU  - Lee YS
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20080412
PL  - Netherlands
TA  - Mol Divers
JT  - Molecular diversity
JID - 9516534
RN  - 0 (Bridged Bicyclo Compounds, Heterocyclic)
RN  - 0 (Imidazoles)
SB  - IM
MH  - Automation
MH  - Bridged Bicyclo Compounds, Heterocyclic/*chemical synthesis/chemistry/therapeutic 
      use
MH  - Drug Design
MH  - Imidazoles/*chemical synthesis/chemistry/therapeutic use
RF  - 61
EDAT- 2008/04/15 09:00
MHDA- 2008/10/02 09:00
CRDT- 2008/04/15 09:00
PHST- 2007/10/15 00:00 [received]
PHST- 2008/02/24 00:00 [accepted]
PHST- 2008/04/15 09:00 [pubmed]
PHST- 2008/10/02 09:00 [medline]
PHST- 2008/04/15 09:00 [entrez]
AID - 10.1007/s11030-008-9072-1 [doi]
PST - ppublish
SO  - Mol Divers. 2008 Feb;12(1):1-15. doi: 10.1007/s11030-008-9072-1. Epub 2008 Apr 
      12.