Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Computed Properties of C10H9NO2, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 16136-58-6, in my other articles.
Chemistry is an experimental science, Computed Properties of C10H9NO2, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 16136-58-6, Name is 1-Methyl-1H-indole-2-carboxylic acid
We have previously disclosed the selective ETA receptor antagonist N-(3,4-dimethyl-5-isoxazolyl)-4?-(2-oxazolyl)[1,1?- biphenyl]-2-sulfonamide (1, BMS-193884) as a clinical development candidate. Additional SAR studies at the 2?-position of 1 led to the identification of several analogues with improved binding affinity as well as selectivity for the ETA receptor. Following the discovery that a 3-amino-isoxazole group displays significantly improved metabolic stability in comparison to its 5-regioisomer, the 3-amino-isoxazole group was combined with the optimal 2?-substituent leading to 16a (BMS-207940). Compound 16a is an extremely potent (ETA Ki = 10 pM) and selective (80000-fold for ETA vs ETB) antagonist. It is also 150-fold more potent and >6-fold more selective than 1. The bioavailability of 16a was 100% in rats and the systemic clearance and volume of distribution are higher than that of 1. In rats, intravenous 16a blocks big ET pressor responses with 30-fold greater potency than 1. After oral dosing at 3 mumol/kg, 16a displays enhanced duration relative to 1.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. Computed Properties of C10H9NO2, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 16136-58-6, in my other articles.
Reference:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles