101666-68-6

Usage

Uses

Used in Pharmaceutical Industry:
N-Desmethyl Clarithromycin is used as an intermediate in the synthesis of Clarithromycin, a widely prescribed macrolide antibiotic. It is utilized for its antimicrobial properties, which are effective against a range of bacterial infections, including respiratory, skin, and soft tissue infections.
Additionally, as a metabolite, N-Desmethyl Clarithromycin may be involved in research and development for understanding the pharmacokinetics and pharmacodynamics of Clarithromycin, potentially leading to improved drug formulations or alternative treatments.
Used in Research and Development:
N-Desmethyl Clarithromycin serves as a crucial compound in the study of drug metabolism and the effects of Clarithromycin on the human body. It aids researchers in understanding the metabolic pathways and helps in the development of new drugs with better efficacy and reduced side effects.
Used in Quality Control:
N-Desmethyl Clarithromycin is used as a reference material for quality control in the pharmaceutical industry. It ensures that the synthesized Clarithromycin meets the required standards and is free from impurities, maintaining the safety and efficacy of the final drug product.

Upstream product

• 81103-11-9 clarithromycin 

Relevant academic research and scientific papers

TRIAZOLE COMPOUNDS AND METHODS OF MAKING AND USING THE SAME

The present invention provides triazole macrocyclic compounds useful as therapeutic agents. More particularly, these compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.

Dicyclic clarithromycin derivative and purpose of dicyclic clarithromycin derivative as tumor cells proliferation inhibitor

The invention belongs to the technical field of medicine, and relates to a dicyclic clarithromycin derivative and a preparation method thereof and an application of the dicyclic clarithromycin derivative as a tumor cells proliferation inhibitor in prepara

Novel desosamine-modified 14- and 15-membered macrolides without antibacterial activity

Novel modifications of the desosamine sugar of 14- and 15-membered antibacterial macrolides, in which the desosamine was fused with N-substituted-1,3-oxazolidin-2-ones, were developed in order to completely suppress antibacterial activity and make them pr

Synthesis and antibacterial activity of desosamine-modified macrolide derivatives

Structural factors behind erm macrolide resistance were studied through synthesis of new macrolide derivates possessing truncated desosamine sugar moieties and subsequent determination of their antibacterial activity. Synthesized compounds with 2′-deoxy a

Novel tandem reaction for the synthesis of Na′-substituted 2-imino-1,3-oxazolidines from vicinal (sec- or tert-)amino alcohol of desosamine

Two one-pot methods, sequential and tandem, for the preparation of Na′-substituted 2-imino-1,3-oxazolidines from the vicinal (sec- or tert)-amino alcohol of desosamine via intermediary alkyl-, aryl-, heteroaryl-, and heteroalkyl-thiourea moieties are described. Particularly interesting is the novel one-pot tandem reaction of the vicinal tert-amino alcohol that involves dealkylation, thiourea formation, and a final cyclization to yield 2-imino-1,3-oxazolidine structures. The yields of both one-pot methods are comparable to the yield of the sequential reaction. A small library of a new class of desosamine-modified 14- and 15-membered macrolides was prepared to demonstrate the variety of substituents that can be easily introduced and thus enable a huge variation of the physicochemical and hence biological properties of these new molecules. Na′-Substituted 2-imino-1,3-oxazolidines have been condensed onto a desosamine amino sugar by two one-pot methods. A novel one-pot tandem reaction of the 2a′,3a′-vicinal tert-amino alcohol of desosamineinvolving dealkylation, thiourea formation, and a final cyclization to yield 2-imino-1,3-oxazolidine structures with a Z configuration around the imine bond has been discovered. Copyright

Non-peptide macrocyclic histone deacetylase inhibitors derived from tricyclic ketolide skeleton

Inhibition of histone deacetylase (HDAC) function is a validated therapeutic strategy for cancer treatment. Of the several structurally distinct small molecule histone deacetylase inhibitors (HDACi) reported, macrocyclic depsipeptides possess the most complex cap groups and have demonstrated excellent HDAC inhibition potency and isoform selectivity. Unfortunately, the development of macrocyclic depsipeptides has been hampered in part because of development problems characteristic of large peptides and the complex reaction schemes required for their synthesis. Herein we report that tricyclic ketolide TE-802 is an excellent mimetic for the peptide backbone of macrocyclic HDACi. Compounds derived from this template are particularly selective against HDACs 1 and 2 with nanomolar inhibitory activity. Interrogation of the association between a subset of these compounds and key HDAC isoforms, using AutoDock, enables a molecular description of the interaction between the HDAC enzyme's outer rim and the inhibitors' macrocyclic cap group that are responsible for compound affinity and presumably isoform selectivity.

Synthesis of an antibacterial compound containing a 1,4-substituted 10-1,2,3-triazole: A scaleable alternative to the click reaction

The copper-catalyzed click reaction of an azide with an alkyne has become a popular method to build up 1,4-substituted 1H-1,2,3- triazoles in medicinal chemistry and this approach was used on a laboratory scale during the preparation of novel macrolide 1. However, the manufacture of the key azide component, as well as its subsequent use in the presence of a copper catalyst on a large scale, was associated with potential safety concerns. Therefore, a sequence was developed in which construction of the 1,4- substituted 1H-1,2,3-triazole in 1 was accomplished via cyclocon - densation of an a,a-dichloro tosyl hydrazone with an amine.

MACROLIDE DERIVATIVES

Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeuti

Non-peptide macrocyclic histone deacetylase inhibitors

Inhibition of histone deacetylase inhibitors (HDACi) hold great promise in cancer therapy because of their demonstrated ability to arrest proliferation of nearly all transformed cell types. Of the several structurally distinct small molecule HDACi reporte

2'-O,3'-N-BRIDGED MACROLIDES

Novel 2 ' -O, 3 ' -/V-bridged macrolides useful in treatment of inflammatory diseases. More particularly, the invention relates to 2 ' -O, 3 ' -/V-bridged 14- membered macrolides and to 2 ' - O, 3 ' -/V-bridged 15-membered azalide macrolides useful in treatment of neutrophil dominated inflammatory diseases resulting from neutrophilic infiltration and/or diseases associated with altered cellular functionality of neutrophils, to intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof.