190839-76-0

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 106454-69-7 N-tert-butoxycarbonyl-D-Phenylalaninol 
• 18942-49-9 Boc-D-Phe-OH 
• 126301-19-7 (2R)-2-[(tert-butoxycarbonyl)amino]-3-phenylpropyl methanesulfonate 
• 5267-64-1 (R)-2-amino-3-phenylpropanol 
• 141595-88-2 (R)-tert-butyl (1-bromo-3-phenylpropan-2-yl)carbamate 

Downstream Products

• 185384-16-1 (2R)-2-[(tert-butoxycarbonyl)amino]-3-phenylpropylamine 
• 130406-33-6 (R)-α-(azidomethyl)-2-phenylethanamine 
• 85612-59-5 (R)-3-phenylpropane-1,2-diamine 
• 1357194-37-6 (R)-1-azido-3-phenylpropan-2-amine hydrochloride 
• 185384-18-3 [(R)-1-Benzyl-2-((S)-2-tert-butoxycarbonylamino-3-phenyl-propionylamino)-ethyl]-carbamic acid tert-butyl ester 
• 714909-31-6 (S)-N¹-((R)-2-Amino-3-phenyl-propyl)-3-phenyl-propane-1,2-diamine 

Relevant academic research and scientific papers

PEPTIDE-OLIGOUREA HYBRID COMPOUNDS

The present description relates to peptidomimetic foldamers, and their synthesis. In particular, the description provides peptide-amino urea hybrid peptidomimetic foldamers comprising an alpha amino acid peptide portion and an oligourea portion.

6-O-SUBSTITUTED KETOLIDES HAVING ANTIBACTERIAL ACTIVITY

PROBLEM TO BE SOLVED: To provide 6-O-substituted ketolides with antibacterial activity, having acid stability and enhanced activity toward gram negative bacteria and macrolide resistant gram positive bacteria. SOLUTION: This invention provides 6-O-substituted erythromycin ketolide derivatives such as formula (II) and compositions comprising the compounds. [Y and Z together form a group X; X is ketone, hydroxyimino or the like; or, one of Y and Z is H and the other is hydrogen, hydroxy or the like; Ra is H, hydroxy; Rc is H or a hydroxy protective group; R is a substituted methyl group]. COPYRIGHT: (C)2015,JPOandINPIT

Design, synthesis and SAR studies of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine as aminopeptidase N/CD13 inhibitors

Aminopeptidase N (APN), belonged to metalloproteinase, is an essential peptidase involved in the process of tumor invasion and metastasis. A series of tripeptide analogs with the scaffold 3-phenylpropane-1,2-diamine were designed, synthesized and evaluate

Synthesis and evaluation of inhibitors of cytochrome P450 3A (CYP3A) for pharmacokinetic enhancement of drugs

The HIV protease inhibitor ritonavir (RTV) is also a potent inhibitor of the metabolizing enzyme cytochrome P450 3A (CYP3A) and is clinically useful in HIV therapy in its ability to enhance human plasma levels of other HIV protease inhibitors (PIs). A nov

Discovery of highly potent and selective inhibitors of neuronal nitric oxide synthase by fragment hopping

Selective inhibition of neuronal nitric oxide synthase (nNOS) has been shown to prevent brain injury and is important for the treatment of various neurodegenerative disorders. This study shows that not only greater inhibitory potency and isozyme selectivity but more druglike properties can be achieved by fragment hopping. On the basis of the structure of lead molecule 6, fragment hopping effectively extracted the minimal pharmacophoric elements in the active site of nNOS for ligand hydrophobic and steric interactions and generated appropriate lipophilic fragments for lead optimization. More potent and selective inhibitors with better druglike properties were obtained within the design of 20 derivatives (compounds 7-26). Our structure - based inhibitor design for nNOS and SAR analysis reveal the robustness and efficiency of fragment hopping in lead discovery and structural optimization, which implicates a broad application of this approach to many other therapeutic targets for which known druglike small-molecule modulators are still limited.

Novel 3-phenylpropane-1,2-diamine derivates as inhibitors of aminopeptidase N (APN)

Aminopeptidase N (APN) is an essential peptidase involved in the process of tumor invasion and metastasis. Here we describe a novel class of inhibitor with 3-phenylpropane-1,2-diamine as scaffold to APN. Preliminary activity evaluation with enzyme inhibition studies showed that compound 12i exhibited potent and selective inhibitory activity towards APN with the IC50 value 15.5 ± 1.2 μM.

POTENT AND HIGHLY SELECTIVE HETEROAROMATIC INHIBITORS OF NEURONAL NITRIC OXIDE SYNTHASE

Peptidomimetic compounds as can inhibit neuronal nitric oxide synthase (nNOS) for potential treatment in neurodegenerative diseases, such as but not limited to stroke, Alzheimer's disease, Parkinson's disease, Huntington's disease.

HETEROAROMATIC SELECTIVE INHIBITORS OF NEURONAL NITRIC OXIDE SYNTHASE

Compounds inhibiting neuronal nitric oxide synthase (nNOS) for potential treatment in neurodegenerative diseases, such as stroke, Alzheimer's disease, Parkinson's disease, Huntington's disease, such compounds of a formula.

Macrolide antiinfective agents

The invention is directed towards antibacterial compounds. The invention concerns macrolide antibiotics useful as antiinfective agents.

6-O-substituted ketolides having antibacterial activity

Antimicrobial compounds having the formula STR1 as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.