Room temperature ligand-free Cu2O-H2O2 catalyzed tandem oxidative synthesis of quinazoline-4(3H)-one and quinazoline derivatives.

An efficient and simple copper catalytic system has been developed for the synthesis of medicinally important 2-substituted quinazoline-4(3H)-ones from 2-aminobenzonitrile and benzyl alcohol derivatives and additionally 2-substituted quinazolines from 2-aminobenzylamine and benzaldehyde derivatives. Mild oxidant H2O2 was utilized, providing excellent product yields. The molecular structure of one of the compounds was substantiated through SC-XRD. The versatility of the protocol was demonstrated through gram-scale syntheses.

[DDQM][HSO4]/TBHP as a Multifunctional Catalyst for the Metal Free Tandem Oxidative Synthesis of 2-Phenylquinazolin-4(3H)-ones.

A bifunctional ionic liquid (IL) [DDQM][HSO4] has been designed and explored as a three-way catalyst for the synthesis of 2-phenylquinazolin-4(3H)-ones from anthranilamide and benzyl alcohol in 3.5 min incorporating microwave irradiation. Photochemically the reaction proceeds for 4 h at room temperature and thermally for 8 h at 120 °C. Further IL-assisted metal, solvent, and base free in situ oxidation of benzyl alcohols to aldehydes shows its task specificity. The multifunctionality of the IL was reestablished with the synthesis of two Wnt pathway antagonists.

Design and Synthesis of Quinazolinone-Triazole Hybrids as Potent Anti-Tubercular Agents.

A straightforward and convenient methodology has been developed for the reaction of 2-aminobenzamide and carbonyls affording 2,3-dihydroquinazolin-4(1H)-ones using aqueous solution of [C12Py][FeCl3Br]. The developed methodology was applied for the synthesis of 25 quinazolinone-triazole hybrids followed by evaluation of their in vitro anti-tubercular (TB) activity. The results revealed that 8 quinazolinone-triazole hybrids displayed promising activity having MIC values of 0.78-12.5 µg/mL. The compound 3if with MIC 0.78 µg/mL was found to be the lead nominee among the series, better than Ethambutol, a first line anti-TB drug and comparable with Rifampicin. The active compounds with MIC values ≤ 6.25 µg/mL were subjected to in vitro cytotoxicity and found nontoxic. In drug-drug interaction, compounds 3ia and 3ii interacted synergistically with all the three anti-TB drugs, INH, RFM, and EMB. Other 3 compounds interacted either in synergistic or additive manners. Important information on the binding interaction of the target compounds with the active sites of 1DQY Antigen 85C from Mycobacterium tuberculosis and Enoyl acyl carrier protein reductase (InhA) enzymes was obtained from molecular docking studies. Screening of the drug-likeness properties and bioactivity score indicates that synthesized molecules could be projected as potential drug candidates. Based on the current study, quinazolinone-triazole hybrids framework can be useful in drug development for TB.

Anomalous structural behavior and antiferroelectricity in BiGdO3: detailed temperature and high-pressure study.

A comprehensive temperature and high-pressure investigation on BiGdO3is carried out by means of dielectric constant, piezoelectric current, polarization-electric field loop, Raman scattering and x-ray diffraction measurements. Temperature dependent dielectric constant and dielectric loss show two anomalies at about 290 K (Tr) and 720 K (TC). The latter anomaly is most likely due to antiferroelectric to paraelectric transition as hinted by piezoelectric current and polarization-electric field loop measurements at room temperature, while the former anomaly suggests reorientation of polarization. A small deviation from linear behaviour of both the Raman modes due to structural modification in the vicinity ofTC; and sharp decrease in integrated intensities of these two modes aboveTCprovide further proof for the above antiferroelectric to paraelectric transition. Cubic to monoclinic structural transition is observed at about 10 GPa in high-pressure x-ray diffraction studies accompanied by anisotropic lattice parameter changes and large unit cell volume collapse during the transition. This structural transition is corroborated by anomalous softening and large increase in full width half maximum of M2(640 cm-1) Raman mode above 10 GPa. We speculate that enhancement of large structural distortion and large reduction inc/aratio above 10 GPa might be associated with antiferroelectric to ferroelectric transition in the system.

Recent advances in the synthesis of Quinazoline analogues as Anti-TB agents.

Quinazoline analogues are one of the important nitrogen containing heterocycles that have significant bioactivity as well as found in a plethora of natural products. Tuberculosis is one of the serious universal health threats caused by Mycobacteriumtuberculosis (MTB) and primarily affects the lungs. Due to their significant bioactivity and natural occurrences of quinazolines, researchers are trying to synthesize new quinazoline analogues which may have significant potency against tuberculosis. This particular review summarizes recent development of different types of quinazoline bearing analogues as anti-tubercular (anti-TB) agents and their synthesis with structure-activity relationship.

Studies on peptidyl nucleoside antibiotics: synthesis and antifungal evaluation of pyranosyl nucleoside analogs of nikkomycin.

BACKGROUND: The Streptomyces-derived nikkomycins are a unique class of peptidyl nucleoside natural products, with potent antifungal activity against a variety of pathogenic fungi. RESULTS: In continuation of our structure-activity relationship studies on the nikkomycins, this paper describes the strategic design, synthesis and biological evaluation of a 'doubly modified' generation of nikkomycin analogs. The structural modifications included a ring-expanded carbohydrate core and a simplified peptidyl side chain. Biological screening of these novel analogs against clinical isolates of various human pathogenic fungi indicated that the described modifications of the structural features of nikkomycin could be a potentially beneficial strategy towards optimizing the antifungal potency of this class of peptidyl nucleoside antibiotics. CONCLUSION: Continued investigation of the pyranosyl nikkomycin analogs is warranted to fully explore and optimize the structural features of this novel lead for the desired development of a new class of therapeutically useful antifungal drugs.