Yamamoto, Takeshi published the artcileQuantitative structure-activity relationship study of N-(3-Oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carbonyl)guanidines as potent Na/H exchange inhibitors, Safety of Ethyl 2-mercaptopropanoate, the publication is Chemical & Pharmaceutical Bulletin (2000), 48(6), 843-849, database is CAplus and MEDLINE.
The authors have previously reported that N-(4-isopropyl-2,2-dimethyl-3-oxo-3,4-dihydro-2H-benzo[1,4]oxazine-6-carbonyl)guanidine methanesulfonate salt (KB-R9032) is a potent and highly water-soluble Na/H exchange inhibitor. In a series of studies on Na/H exchange inhibitors, the authors designed and synthesized N-(3-oxo-3,4-dihydro-2H-benzo[1,4]thiazine-6-carbonyl)guanidines (I, R1 = H, R2 = H or Me and R3 = H, Me, Et, iso-Pr, Pr, Bu or pentyl) as more potent inhibitors with high water-solubility The design strategy for I was based on a quant. structure-activity relation (QSAR) study, involving the proportional relation between the biol. activity and hydrophobicity of the ring structure of N-(2H-benzo[1,4]oxazine-6-carbonyl)guanidines (II). As expected, I showed more potent activity than II. It was found by using the QSAR anal. that I were about five-fold more potent than II. The increase in potency of I well agreed with the authors previous QSAR anal. result. The most potent derivative was the methanesulfonate salt of the 4-iso-Pr derivative of I (IC50=0.0091 μM). In addition to the in vitro study, the 4-iso-Pr derivative of I showed significant protective activity against ventricular fibrillation in a rat acute myocardial infarction model.
Chemical & Pharmaceutical Bulletin published new progress about 19788-49-9. 19788-49-9 belongs to esters-buliding-blocks, auxiliary class Thiol,Aliphatic hydrocarbon chain,Ester, name is Ethyl 2-mercaptopropanoate, and the molecular formula is C19H21N3O3S, Safety of Ethyl 2-mercaptopropanoate.
Referemce:
https://en.wikipedia.org/wiki/Ester,
Ester – an overview | ScienceDirect Topics