Watanabe, Hitoshi published the artcileSynthesis and pharmacological evaluation of 11-(1,6-dimethyl-1,2,3,6-tetrahydropyridin-4-yl)-5H-dibenzo[b,e][1,4]diazepines with clozapine-like receptor occupancy at dopamine D1/D2 receptor, Category: chlorides-buliding-blocks, the publication is Bioorganic & Medicinal Chemistry Letters (2020), 30(21), 127563, database is CAplus and MEDLINE.
Clozapine-like compound without agranulocytosis risk is need to cure the treatment resistant schizophrenia (TRS). We discovered I as Clozapine-like dopamine D2/D1 receptor selectivity and improved reactive metabolites formation profile by the modification of piperazine moiety in Clozapine. The optimization of I gave compound II to be best compound (approx. 10-fold stronger affinity for D2/D1 receptor and similar D2/D1 selectivity ratio with Clozapine). Clozapine-like D2/D1 receptor occupancy profile was proved by in vivo evaluation. In addition, the reactive metabolites derived agranulocytosis risk of compound II was considered to be lower than Clozapine. The pharmacol. detail of compound II is being investigated to develop it for TRS treatment.
Bioorganic & Medicinal Chemistry Letters published new progress about 60091-87-4. 60091-87-4 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitro Compound,Carboxylic acid,Amine,Benzene, name is 2-((4-Chloro-2-nitrophenyl)amino)benzoic acid, and the molecular formula is C9H10O4, Category: chlorides-buliding-blocks.
Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics