Synthesis and Biological Activity of Novel 6-Substituted Purine Derivatives

Abstract

A series of 6-substituted purines were synthesized from commercially available 2-amino-6-chloropurine with appropriate reagents, and nine new compounds 7, 8, and 11-17 have been discovered. The compounds synthesized were identified by elemental analysis, 1H NMR, as well as mass spectral data. All the title compounds were screened for their antifungal activities, under the method of the disc diffusion, using three species of fungi — Bacillus subtillis, Aspergillus niger, and Candida tropicalis— and some of the compounds showed promising activities.

ZnO Nanoparticles: A Highly Effective and Readily Recyclable Catalyst for the One-Pot Synthesis of 1,8-dioxo-decahydroacridine and 1,8-dioxooctahydro-xanthene Derivatives

“…Nitrogen-containing heterocyclic compounds are widespread in Nature and their applications in biologically active pharmaceuticals, agrochemicals and functional materials are becoming more and more important [10][11][12]. Therefore, the development of new efficient methods for synthesis of N-heterocycles is one of the major interests of modern synthetic organic chemistry [13][14][15][16]. Recently, the synthesis of 1,8-dioxo-decahydroacridines via three-component coupling of aldehydes, dimedone and amines has been reported using MCRs in the presence of diverse catalysts including ceric ammonium nitrate (CAN) [17], fluorotailed acidic imidazolium salts [18], 1-n-butyl-3-methylimidazolium bromide [bmim]Br [19], 1methylimidazolium triflouroacetate [Hmim]TFA [20], proline [21], amberlyst-15 [22], carbon-based solid acid (CBSA) [23], silica-bonded N-propyl sulfamic acid (SBNPSA) [24], 4-dodecylbenzenesulfonic acid (DBSA) [25] and Zn(OAc) 2 .2H 2 O [26].…”

Development of a Commercial Manufacturing Route to 2-Fluoroadenine, The Key Unnatural Nucleobase of Islatravir

“…We initiated route development with the key fluorination/amination step. Although the isolation of difluoropurine 10 has been reported, our early attempts to prepare 10 revealed that this electron-deficient compound is reactive and undergoes polymerization and degradation under the reaction conditions . Smaller order oligomers of purine species up to tetramers were identified by LCMS.…”

Recent Advances and Developments of in vitro Evaluation of Heterocyclic Moieties on Cancer Cell Lines

“…Purines have also been known as the building blocks of DNA and RNA. They are also found in number of biomolecules including ATP, GTP, NADH, AMP and coenzyme A. Purine derivatives have been known to exhibit anti‐leishmanial, anti‐viral, anti‐fungal, anti‐bacterial and anti‐cancer activities . Pyrimidine analogs have also attracted a considerable attention due to their wide range of biological activities like antitumor, antimycobacterial,antiviral and anti‐inflammatory …”