Base Information
- Chemical Name:4-chlorophenylmagnesium bromide
- CAS No.:73-77-8
- Molecular Formula:C6H4BrClMg
- Molecular Weight:215.75796
- Hs Code.:
- Mol file:73-77-8.mol
Synonyms:
Synonyms:
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The research investigates the structure–activity relationship (SAR) of over 50 derivatives of octahydrobenzo[g]quinoline (obeline)-type somatostatin sst1 receptor antagonists, with a focus on modifying the arylpiperazine moiety. The goal was to enhance the sst1 receptor affinities to a subnanomolar level while improving selectivities over the sst2 receptor subtype, without compromising the favorable drug-like properties of the lead molecule. Key chemicals used include various heteroaryl moieties, substituted phenylpiperazines, and cyclic secondary amines. The study found that the best derivatives achieved subnanomolar sst1 affinities and >10,000-fold selectivities over sst2, with promising pharmacokinetic properties. Notably, the introduction of a 4-cyano substituent and a 2-pyridone moiety significantly improved sst1 affinity, while benzothiadiazole derivatives also showed high affinity and selectivity. The research concludes that the arylpiperazine moiety is crucial for optimizing the binding properties of obeline-type sst1 receptor antagonists.
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