Electric Literature of C12H13N3O2On May 15, 2015 ,《Synthetic studies of five-membered heteroaromatic derivatives as potassium-competitive acid blockers (P-CABs)》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Arikawa, Yasuyoshi; Hasuoka, Atsushi; Nishida, Haruyuki; Hirase, Keizo; Inatomi, Nobuhiro; Takagi, Terufumi; Tarui, Naoki; Kawamoto, Makiko; Imanishi, Akio; Itoh, Fumio; Kajino, Masahiro. The article conveys some information:
On the basis of a series of novel and potent potassium-competitive acid blockers represented by 1-sulfonylpyrrole derivative I, we prepared several five-membered heterocyclic analogs II [Ht = S, N, O containing heterocycle] and evaluated their H+,K+-ATPase activities in vitro. We also assessed the role of the methylaminomethyl side chain by comparison with methylamino and ethylamino derivatives We observed that the five-membered core ring and its orientation affect inhibitory activity and that the methylaminomethyl moiety is the best side chain. On the basis of potency and ligand-lipophilicity efficiency, compound I remains the most drug-like of the compounds studied to date. This study revealed the factors necessary for potent H+,K+-ATPase inhibition, such as differences in electron d., the properties of the lone pair at each apical position of the heteroaromatic ring, and the geometry of the substituents. After reading the article, we found that the author used Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate(cas: 866837-96-9Electric Literature of C12H13N3O2)
Ethyl 5-amino-1-phenyl-1H-pyrazole-3-carboxylate(cas: 866837-96-9) belongs to anime. Reaction with nitrous acid (HNO2), which functions as an acylating agent that is a source of the nitrosyl group (―NO), converts aliphatic primary amines to nitrogen and mixtures of alkenes and alcohols corresponding to the alkyl group in a complex process. This reaction has been used for analytical determination of primary amino groups in a procedure known as the Van Slyke method.Electric Literature of C12H13N3O2
Referemce:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics