Electric Literature of 111769-27-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.111769-27-8, Name is (R)-Tetrahydrofuran-3-amine 4-methylbenzenesulfonate, molecular formula is C11H17NO4S. In a Article,once mentioned of 111769-27-8
A series of 5?-carbamoyl and 5?-thionocarbamoyl derivatives of 2?-C-methyl analogues of the A1 adenosine receptor (A1AR) full agonists N6-cyclopentyladenosine (CPA), 2-chloro-N6-cyclopentyladenosine (CCPA), N6-[3-(R)-tetrahydrofuranyl]adenosine (tecadenoson), and 2-chloro analogue (2-Cl-tecadenoson) was synthesized and evaluated for their affinity for adenosine receptor subtypes from bovine, porcine, and human species. In the N6-cyclopentylamino series, the 5?-substituted derivatives showed a reduced affinity at the bovine A1AR compared to the parent compounds; however, the selectivity for A1 versus A2A receptor was retained or increased. The corresponding N6-3-(R)-tetrahydrofuranylamino analogues displayed a very low affinity toward the bovine A1AR. The 5?-methylthionocarbamoyl derivative of 2?-Me-CCPA showed the best affinity at porcine A1AR with a Ki value of 13 nM. At human AR subtypes tecadenoson derivatives showed 2.3- to 5-fold lower affinity at A1AR and very low affinity at the other subtypes (A2A, A2B, and A3) compared to the corresponding N6-cyclopentyl analogues. The 5?-carbamoyl and 5?-thionocarbamoyl derivatives of 2?-Me-CCPA 3, 4, 7 and tecadenoson derivative 12 were found to be partial A1 agonists at the porcine receptor. Docking studies explained the lower affinity of N6-3-(R)-tetrahydrofuranyl-substituted compounds at bovine A1AR compared to that of N6-cyclopentyl analogues, showing that the oxygen of the tetrahydrofuranyl ring establishes unfavorable electrostatic interactions with the CO oxygen of Asn254. The low binding affinity of the 2?-C-methyl-N6-3-(R)-tetrahydrofuranyl adenosine analogues at human A1AR may be ascribed to the presence of unfavorable interactions between the hydrophilic tetrahydrofuranyl ring and the surrounding hydrophobic residues Leu250 (TM6) and Ile274 (TM7).
We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 111769-27-8, and how the biochemistry of the body works.Electric Literature of 111769-27-8
Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem