The azaindole chemical scaffold is represented in many biologically active natural products and synthetic derivatives. Recently, this chemical scaffold yielded several therapeutic agents for a variety of diseases. Due to the interesting biochemical and biophysical properties of various isomeric azaindoles, numerous investigators have designed and implemented novel synthetic methods for azaindole core units in the past few decades. By using these novel strategies, a number of diversely substituted azaindoles including bioactive natural products, key intermediates and drug candidates have been produced. Herein, we have reviewed the novel synthetic strategies developed for azaindoles since 2011 and highlight their attractive reaction mechanisms, advantages and their limitations. This review may offer potential solutions to develop novel and facile methodologies for the azaindole derivatives of biological interest.

Recent developments in the synthesis of azaindoles from pyridine and pyrrole building blocks

Azaindole therapeutic agents.

https://link.springer.com/content/pdf/10.1186/s43094-020-00042-0.pdf

Amelioration of lipophilic compounds in regards to bioavailability as self-emulsifying drug delivery system (SEDDS)

Azaindoles and azaindolines are important core structures in pharmaceuticals and natural products, which have found wide applications in the field of medicinal chemistrty. In this study, we developed a novel...

Alkali-Amide Controlled Selective Synthesis of 7-Azaindole and 7-Azaindoline through Domino Reactions of 2-Fluoro-3-methylpyridine and Aldehydes

Using in situ Raman spectroscopy to study the drug precipitation inhibition and supersaturation mechanism of Vitamin E TPGS from self-emulsifying drug delivery systems (SEDDS)

Azaindoles have been accepted as important structures having various biological activities in medicinal chemistry in novel drug discovery. Various azaindole derivatives have been used commercially and newer analogues are synthesized continuously. As in literature, azaindole is a very potent moiety, its derivatives displayed a number of biological activities such as kinase inhibitors, cytotoxic agents, anti-angiogenic activity, CRTh2 receptor antagonists, melanin agonists, nicotine agonists, effectiveness in alzheimer disease, cytokinin analogs, Orai inhibitors in asthma and chemokine receptor- 2 (CCR2) antagonists. This review consists of biological activities of various azaindole analogs, reported so far, and their structure activity relations, along with future perspectives in this field.

7-Azaindole Analogues as Bioactive Agents and Recent Results

Oral route still remains the favorite route of drug administration in many diseases because it is very suitable for drug delivery and non invasive. Till today it attracts to many researchers for investigation in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bio-availability due to less water solubility and permeability of the drug across the biological membrane. This may arise high inter and intra subject variability due to lack of dose proportionality and therapeutic failure. It is estimated that 40% of new active constituents which are investigated recently show poor water solubility due to their lipophilic nature.  The improvement of bio-availability of these drugs with such properties presents one of the greatest challenges in drug formulations. Several technologies are used for overcome these problems including micronization, solid dispersions, cyclodextrins complex formation and different lipid based drug delivery systems. Self-emulsifying drug delivery system is one the most important and advanced technology for enhancing the oral bio-availability as well reducing in dose. This system also gained attraction for enabling more consistent drug absorption, selective targeting of drugs in GIT, and protection of drugs from the inner environment of gut.

http://www.arjournals.org/index.php/ijdd/article/viewFile/717/pdf

Self Emulsifying Drug Delivery System: A Gentle Approach for drug delivery

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7-Azaindole Analogues as Bioactive Agents and Recent Results

Self Emulsifying Drug Delivery System: A Gentle Approach for drug delivery