Browsing CHEM Faculty Scholarship by Author "Aravapalli, Sridhar"

Now showing items 1-7 of 7

    • Antifungal activity of a series of 1,2-benzisothiazol-3(2H)-one derivatives 

      Dou, Dengfeng; Alex, Deepu; Du, Bingfan; Tiew, Kok-Chuan; Aravapalli, Sridhar; Mandadapu, Sivakoteswara Rao; Calderone, Richard; Groutas, William C. (Elsevier, 2011-10-01)
      A series of broad-spectrum antifungal agents based on the 1,2-benzisothiazol-3(2H)-one scaffold is reported. Preliminary structure-activity relationship studies have established the importance of the presence of the ...

    • Design, synthesis and characterization of novel 1,2-benzisothiazol-3(2H)-one and 1,3,4-oxadiazole hybrid derivatives: Potent inhibitors of Dengue and West Nile virus NS2B/NS3 proteases 

      Lai, Huiguo; Dou, Dengfeng; Aravapalli, Sridhar; Teramoto, Tadahisa; Lushington, Gerald H.; Mwania, Tom M.; Alliston, Kevin R.; Eichhorn, David M.; Padmanabhan, Radhakrishnan; Groutas, William C. (PERGAMON-ELSEVIER SCIENCE LTD, 2013-01)
      1,2-Benzisothiazol-3(2H)-ones and 1,3,4-oxadiazoles individually have recently attracted considerable interest in drug discovery, including as antibacterial and antifungal agents. In this study, a series of functionalized ...

    • Design, synthesis, and evaluation of inhibitors of Norwalk virus 3C protease 

      Tiew, Kok-Chuan; He, Guijia; Aravapalli, Sridhar; Mandadapu, Sivakoteswara Rao; Gunnam, Mallikarjuna Reddy; Alliston, Kevin R.; Lushington, Gerald H.; Kim, Yunjeong; Chang, Kyeong-Ok; Groutas, William C. (Elsevier, 2011-09-15)
      The first series of peptidyl aldehyde inhibitors that incorporate in their structure a glutamine surrogate has been designed and synthesized based on the known substrate specificity of Norwalk virus 3C protease. The ...

    • Inhibition of noroviruses by piperazine derivatives 

      Dou, Dengfeng; He, Guijia; Mandadapu, Sivakoteswara Rao; Aravapalli, Sridhar; Kim, Yunjeong; Chang, Kyeong-Ok; Groutas, William C. (Elsevier, 2012-01)
      There is currently an unmet need for the development of small-molecule therapeutics for norovirus infection. The piperazine scaffold, a privileged structure embodied in many pharmacological agents, was used to synthesize ...

    • Inhibitors of Dengue Virus and West Nile Virus proteases based on the aminobenzamide scaffold 

      Aravapalli, Sridhar; Lai, Huiguo; Teramoto, Tadahisa; Alliston, Kevin R.; Lushington, Gerald H.; Ferguson, Eron L.; Padmanabhan, Radhakrishnan; Groutas, William C. (Elsevier, 2012-05-10)
      Dengue and West Nile viruses (WNV) are mosquito-borne members of flaviviruses that cause significant morbidity and mortality. There is no approved vaccine or antiviral drugs for human use to date. In this study, a series ...

    • Macrocyclic Inhibitors of 3C and 3C-like Proteases of Picornavirus, Norovirus, and Coronavirus 

      Mandadapu, Sivakoteswara Rao; Weerawarna, Pathum M.; Prior, Allan M.; Uy, Roxanne Adeline Z.; Aravapalli, Sridhar; Alliston, Kevin R.; Lushington, Gerald H.; Kim, Yunjeong; Hua, Duy H.; Chang, Kyeong-Ok; Groutas, William C. (Elsevier, 2013-05-16)
      The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective ...

    • Potent inhibition of Norwalk virus by cyclic sulfamide derivatives 

      Dou, Dengfeng; Tiew, Kok-Chuan; He, Guijia; Mandadapu, Sivakoteswara Rao; Aravapalli, Sridhar; Alliston, Kevin R.; Kim, Yunjeong; Chang, Kyeong-Ok; Groutas, William C. (Elsevier, 2011-10-15)
      A new class of compounds that exhibit anti-norovirus activity in a cell-based system and embody in their structure a cyclosulfamide scaffold has been identified. The structure of the initial hit (compound 2a, ED(50) 4 µM, ...