An Expedient Route to Imidazo[1,4]diazepin-7-ones via A Post-Ugi Gold-Catalyzed Heteroannulation

A novel diversity-oriented post-Ugi/gold(I)-catalyzed heteroannulation process for the synthesis of imidazo[1,4]diazepin-7-ones is elaborated. The scope and limitations of the protocol are discussed

Facile, catalyst-free, microwave-assisted access toward the synthesis of 2-aryl/alkyl-3-(1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)-2, 3-dihydroquinazolin-4(1<i>H</i>)-ones

<p>An efficient, catalyst-free, microwave-assisted approach has been developed for the synthesis of 2-aryl/alkyl-3-(1<i>H</i>-benzo[<i>d</i>]imidazol-2-yl)-2,3-dihydroquinazolin-4(1<i>H</i>)-one derivatives by condensing 2-aminobenzamides with various aliphatic, aromatic, and heterocyclic aldehydes. This catalyst-free approach exhibited good functional group compatibility and produced the desired products in good to excellent yields in just 10–20 min. This approach can be seen as a better alternative of the metal-catalyzed protocols used for the synthesis of this class of compounds. The formation of desired compound has also been confirmed by X-ray analysis.</p

Microwave-Assisted, Metal-Free, Base-Mediated C–N Bond Formation/Cleavage: Synthesis of Benzimidazo[1,2‑<i>a</i>]quinazoline Derivatives

A novel, rapid, and efficient microwave-assisted, metal-free, base-mediated approach has been developed for the construction of benzimidazo­[1,2-<i>a</i>]­quinazolines from readily available building blocks. This synthetic strategy affords a diverse range of benzimidazo­[1,2-<i>a</i>]­quinazoline derivatives in moderate to good yields

Glycine-Terminated Dendritic Amphiphiles for Nonviral Gene Delivery

Development of nonviral vectors for the successful application of gene therapy through siRNA/DNA transfection of cells is still a great challenge in current research., In the present study, we have developed multivalent polyglycerol dendron based amphiphiles with well-defined molecular structures that express controlled glycine arrays on their surfaces. The structure–activity relationships with respect to the siRNA complexation, toxicity, and transfection profiles were studied with synthesized amphiphilic polycations. Our findings revealed that a second-generation amphiphilic dendrimer (G2-octaamine, <b>4</b>) that has eight amine groups on its surface and a hydrophobic C-18 alkyl chain at the core of the dendron, acts as an efficient vector to deliver siRNA and achieve potent gene silencing by investigating the knockdown of luciferase and GAPDH gene activity in HeLa cells. Interestingly, the amphiphilic vector is nontoxic even at higher ratio of N/P 100. To the best of our knowledge this is the first example of successful in vitro siRNA transfection using dendritic amphiphiles. We believe that this supramolecular complex may serve as a new promising alternative for nonviral siRNA delivery systems and will be investigated for in vivo siRNA delivery in the future

Synthesis and anti-inflammatory activity evaluation of novel triazolyl-isatin hybrids

<p>New isatin-triazole based hybrids have been synthesized and evaluated for their inhibitory activity of TNF-α induced expression of Intercellular Adhesion Molecule-1 (ICAM-1) on the surface of human endothelial cells. Structure-activity relationship (SAR) studies revealed that the presence of the electron-attracting bromo substituent at position-5 of the isatin moiety played an important role in enhancing the anti-inflammatory potential of the synthesized compounds. Z-1-[3-(1<i>H</i>-1,2,4-Triazol-1-yl)propyl]-5-bromo-3-[2-(4-methoxyphenyl)hydrazono]indolin-2-one (<b>19</b>) with an IC₅₀ = 20 μM and 89% ICAM-1 inhibition with MTD at 200 μM was found to be the most potent of all the synthesized derivatives. Introduction of 1,2,4-triazole ring and electron-donating methoxy group on the phenylhydrazone moiety resulted in four-fold increase of the anti-inflammatory activity.</p