Prabhu P. Mohapatra

Chemistry and Biology of Synthetic and Naturally Occurring Antiamoebic Agents

2.2. Schiff Bases and Their Metal Complexes 1904 2.3. Pyrazolines and Their Metal Complexes 1905 2.4. Benzimidazoles and Their Metal Complexes 1906 2.5. Metronidazole Metal Complexes 1908 2.6. Triazines 1910 2.7. Oxime Ethers 1911 2.8. Acetamides 1911 2.9. Carbamates 1912 2.10. Amidines 1913 2.11. Imidazoles 1914 2.12. Bisphosphonates 1914 2.13. Miscellaneous 1915 3. Naturally Occurring Antiamoebic Compounds 1917 3.1. Alkaloids 1917 3.2. Quassinoids 1940 3.3. Flavonoids and Iridoids 1941 3.4. Miscellaneous 1941 4. Drug Targets 1942 5. Conclusion and Future Prospects 1943 6. Abbreviations 1943 7. Acknowledgments 1943 8. References 1943

Synthesis and molecular modeling of antimicrobial active fluoroquinolone-pyrazine conjugates with amino acid linkers

Novel fluoroquinolone-pyrazine conjugates 7a-h with amino acid linkers were synthesized in good yields utilizing benzotriazole chemistry. Antimicrobial bioassay showed that the synthesized bis-conjugates have antimicrobial properties comparable to the parent drugs. Compound 7h showed superior antibacterial activity against Staphylococcus aureus and Streptococcus pyogenes (MIC=74.6 μM and 149.3 μM, respectively). This matched well with the estimated values obtained from 3D-pharmacophore and 2D-QSAR studies (MIC=67 μM and 92.9 μM, respectively).

Synthesis and Characterization of Blowing Agents and Hypergolics

Twelve energetic additives 7–18 were synthesized and evaluated for use as blowing agents. All blowing agent candidates were characterized by NMR spectroscopy, elemental analysis, differential scanning calorimetry, thermogravimetric analysis, and impact sensitivity testing. The X-ray crystal structure of pyrazolium nitrate was also determined. Hypergolic compounds imidazolidine 38a , hexahydropyrimidine 38b , and pyrrolidine derivatives 42 were obtained in improved 80–90% yields by the reduction of the corresponding carbonyl compounds with lithium aluminum hydride in ether under reflux for 12 h. Ignition delays (τexp, μs) were determined for compounds 38a,b and 42 .

Spiroindoles as Potential Pharmacophores

OBJECTIVE The spirooxindole heterocyclic scaffold is found in many natural products and has been identified as an important bioactive agent. BACKGROUND Over the past few decades, various spirooxindole-containing compounds have been reported to possess biological properties and hence found in the structure of many synthetic pharmaceuticals. This mini-review describes the most promising examples of this class of compounds possessing biological activity including anticancer, anti-inflammatory, and antimicrobial activities. CONCLUSION The current review focuses on the biological activity of compounds containing the spirooxindole scaffold.

Curcumin: Not So Spicy After All

BACKGROUND This is a short review on the most recent studies on curcumin and its analogs, including the studies from the laboratories of authors. The diverse medicinal properties of curcumin itself reported in the recent years are reviewed. Although curcumin has shown great potential in treating various diseases, it has not been approved as a clinical drug candidate because of its poor pharmacokinetics. METHOD The recent methods developed to solve this problem are briefly described. CONCLUSION The biological and other properties of synthetic curcumin analogs (diarylheptanoids and diarylpentanoid monocarbonyl derivatives) reported in the recent literature are also presented.