19790-60-4Relevant articles and documents
Chiral polypropionate subunit by a chemoenzymatic approach
Bonini,Chiummiento,Funicello,Marconi,Righi
, p. 2559 - 2561 (1998)
Enzymatic desymmetrization of meso-4-methyl-3,5-syn-dioxolan- 1,3,5,7- tetrol was found to be highly enantioselective leading to both acetylated enantiomers with high enantiomeric excess.
Asymmetric synthesis of D- and L-2-deoxy-4-thioriboses
Uenishi,Motoyama,Takahashi
, p. 101 - 110 (1994)
Both D- and L-enantiomers of 2-deoxy-4-thioribose derivatives 12 and 17 were prepared stereospecifically in 12 steps from 1,3-propanediol. The key intermediary 2,3-epoxy alcohols, 8 and 15 were obtained with high enantiomeric excess by the Sharpless asymmetric epoxidation using (+)-L- diethyl tartrate and (-)-D-diethyl tartrate.
Synthesis of salicylate and salicylamide alcohols for the preparation of phosphorodiamidates and ifosfamide prodrugs
Pal, Ashutosh
, p. 295 - 301 (2021/05/19)
Prodrugs are derivatives of drugs which gives parent drug or release drug when it breaks inside the body by the presence of suitable enzyme, and then exert desired pharmacological effect. For many years, prodrug strategy has been developed enormously to solve many unwanted drug properties. In drug discovery and development, prodrugs have well-known pharmacokinetic effects of pharmacologically nimble products. Almost 10% of drugs permitted whole world are classified as prodrugs, where the application of a prodrug method during initial stages of development is an emergent fashion. Phosphorodiamidates prodrugs are well known anticancer agents particularly against leucomia. To improve the selectivity of the chemotherapeutic agents and reduce systemic toxicity, I herein report different types of salicylate and salicylamide alcohols for the preparation of phosphorodiamidates and ifosfamide prodrugs.
Pyrazole Agonist of the Apelin Receptor Improves Symptoms of Metabolic Syndrome in Mice
Narayanan, Sanju,Wang, Shaobin,Vasukuttan, Vineetha,Vyas Devambatla, Ravi Kumar,Dai, Donghua,Jin, Chunyang,Snyder, Rodney,Laudermilk, Lucas,Runyon, Scott P.,Maitra, Rangan
, p. 3006 - 3025 (2021/04/06)
Apelin receptor agonism improves symptoms of metabolic syndrome. However, endogenous apelin peptides have short half-lives, making their utility as potential drugs limited. Previously, we had identified a novel pyrazole-based agonist scaffold. Systematic modification of this scaffold was performed to produce compounds with improved ADME properties. Compound 13 with favorable agonist potency (cAMPi EC50 = 162 nM), human liver microsome stability (T1/2 = 62 min), and pharmacokinetic profile in rodents was identified. The compound was tested in a mouse model of diet-induced obesity (DIO) and metabolic syndrome for efficacy. Treatment with 13 led to significant weight loss, hypophagia, improved glucose utilization, reduced liver steatosis, and improvement of disease-associated biomarkers. In conclusion, a small-molecule agonist of the apelin receptor has been identified that is suitable for in vivo investigation of the apelinergic system in DIO and perhaps other diseases where this receptor has been implicated to play a role.