Chemistry is the science of change. But why do chemical reactions take place? Why do chemicals react with each other? The answer is in thermodynamics and kinetics, Safety of N-Acetyl-DL-tryptophan, 87-32-1, Name is N-Acetyl-DL-tryptophan, SMILES is O=C(O)C(CC1=CNC2=CC=CC=C12)NC(C)=O, belongs to amides-buliding-blocks compound. In a document, author is Jadresko, Dijana, introduce the new discover.
Antitubercular 7-substituted 2-nitroimidazo[2,1-b]-[1,3]oxazines were previously shown to exhibit potent antileishmanial and antitrypanosomal activities, culminating in a new clinical investigational drug for visceral leishmaniasis (DNDI-0690). To offset development risks, we continued to seek further leads with divergent candidate profiles, especially analogues possessing greater aqueous solubility. Starting from an efficacious monoaryl derivative, replacement of the side chain ether linkage by novel amine, amide, and urea functionality was first explored; the former substitution was well-tolerated in vitro and in vivo but elicited marginal alterations to solubility (except through a less stable benzylamine), whereas the latter groups resulted in significant solubility improvements (up to 53-fold) but an antileishmanial potency reduction of at least 10-fold. Ultimately, we discovered that O-carbamate 66 offered a more optimal balance of increased solubility, suitable metabolic stability, excellent oral bioavailability (100%), and strong in vivo efficacy in a visceral leishmaniasis mouse model (97% parasite load reduction at 25 mg/kg).
A reaction mechanism is the microscopic path by which reactants are transformed into products. Each step is an elementary reaction. In my other articles, you can also check out more blogs about 87-32-1. Safety of N-Acetyl-DL-tryptophan.
Reference:
Amide – Wikipedia,
,Amide – an overview | ScienceDirect Topics