Browsing Chemistry and Biochemistry by Author "Groutas, William C."

Now showing items 1-20 of 116

    • 1,2,5, thiadiazolidin-3-one 1,1-dioxide derivatives 

      Groutas, William C.; Kuang, Rongze (United States Patent and Trademark Office, 2002-07-16)
      Substituted derivatives of 1,2,5-thiadiazolidin-3-one 1,1-dioxides, oligomers containing them, and methods of using them.

    • 1,2,5-Thiadiazolidin-3-one 1,1 dioxide: a powerful scaffold for probing the S' subsites of (chymo)trypsin-like serine proteases 

      Groutas, William C.; Epp, Jeffrey B.; Kuang, Rongze; Ruan, Sumei; Chong, Lee S.; Venkataraman, Radhika; Tu, Juan; He, Shu; Yu, Hongyi; Fu, Qingfong; Li, Yue He; Truong, Tien M.; Vu, Nga T. (Elsevier, 2001-01-01)
      The 1,2,5-thiadiazolidin-3-one 1,1 dioxide scaffold (I) embodies a motif that allows it to dock to the active site of (chymo)trypsin-like proteases in a predictable and substrate-like fashion. Consequently, inhibitors ...

    • 1,2,5-Thiadiazolidin-3-one 1,1-dioxide-based heterocyclic sulfides are potent inhibitors of human tryptase 

      Wong, Tzutshin; Groutas, Christopher S.; Mohan, Swathi; Lai, Zhong; Alliston, Kevin R.; Vu, Nga T.; Schechter, Norman M.; Groutas, William C. (Elsevier, 2005-04-01)
      We describe herein the design, synthesis, and in vitro biochemical evaluation of a series of potent, time-dependent inhibitors of the mast cell-derived serine protease tryptase. The inhibitors were readily obtained by ...

    • 3-(Alkylthio)-N-hydroxysuccinimide derivatives: potent inhibitors of human leukocyte elastase 

      Groutas, William C.; Venkataraman, Radhika; Brubaker, Michael J.; Epp, Jeffrey B.; Chong, Lee S.; Stanga, Michael A.; McClenahan, Jerald J.; Tagusagawa, F. (Elsevier, 1993-08-07)
      A series of 3-(alkylthio)-N-hydroxysuccinimide derivatives was synthesized and their inhibitory activity towards human leukocyte elastase (HLE) was investigated. The interaction of the compounds having a 3-alkylthioether ...

    • 3C-like protease inhibitors block coronavirus replication in vitro and improve survival in MERS-CoV-infected mice 

      Rathnayake, Athri D.; Zheng, Jian; Kim, Yunjeong; Perera, Krishani Dinali; MacKin, Samantha R.; Meyerholz, David K.; Kashipathy, Maithri M.; Battaile, Kevin P.; Lovell, Scott; Perlman, Stanley; Groutas, William C.; Chang, Kyeong-Ok (NLM (Medline), 2020-08-19)
      Pathogenic coronaviruses are a major threat to global public health, as exemplified by severe acute respiratory syndrome coronavirus (SARS-CoV), Middle East respiratory syndrome coronavirus (MERS-CoV), and the newly emerged ...

    • Affinity chromatography of glucose dehydrogenase 

      Carper, W. Robert; Groutas, William C.; Coffin, D.B. (Springer, 1988-01-15)
      Porcine liver beta-D-glucose dehydrogenase, a multi-functional protein, has been purified to apparent homogeneity. The enzyme has been separated from the endoplasmic reticulum using Triton X-114 and further purified using ...

    • Amino acid-derived 1,2-benzisothiazolinone derivatives as novel small-molecule antifungal inhibitors: identification of potential genetic targets 

      Alex, Deepu; Gay-Andrieu, Francoise; May, Jared; Thampi, Linta; Dou, Dengfeng; Mooney, Aileen; Groutas, William C.; Calderone, Richard (American Society of Microbiology, 2012-09)
      We have identified four synthetic compounds (DFD-VI-15, BD-I-186, DFD-V-49, and DFD-V-66) from an amino acid-derived 1,2-benzisothiazolinone (BZT) scaffold that have reasonable MIC50 values against a panel of fungal ...

    • Amino acid-derived phthalimide and saccharin derivatives as inhibitors of human leukocyte elastase, cathepsin G, and proteinase 3 

      Groutas, William C.; Chong, Lee S.; Venkataraman, Radhika; Kuang, Rongze; Epp, Jeffrey B.; Houser-Archield, Nadene; Huang, He; Hoidal, John R. (Elsevier, 1996-08-15)
      Amino acid-derived phthalimide and saccharin derivatives have been investigated for their inhibitory activity toward the serine proteinases human leukocyte elastase, cathepsin G, and proteinase 3. The saccharin derivatives ...

    • Anti-norovirus therapeutics: a patent review (2010-2015) 

      Kankanamalage, Anushka C. Galasiti; Weerawarna, Pathum M.; Kim, Yunjeong; Chang, Kyeong-Ok; Groutas, William C. (Taylor & Francis Group, 2016-03-03)
      Introduction: Human noroviruses are the primary causative agents of acute gastroenteritis and are a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the ...

    • 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 ...

    • Antifungal drug discovery: the process and outcomes 

      Calderone, Richard; Sun, Nuo; Gay-Andrieu, Francoise; Groutas, William C.; Weerawarna, Pathum M.; Prasad, Sridhar; Alex, Deepu; Li, Dongmei (Future Medicine Ltd, 2014-06)
      New data suggest that the global incidence of several types of fungal diseases have traditionally been under- documented. Of these, mortality caused by invasive fungal infections remains disturbingly high, equal to or ...

    • Antiviral drug discovery: norovirus proteases and development of inhibitors 

      Chang, Kyeong-Ok; Kim, Yunjeong; Lovell, Scott; Rathnayake, Athri D.; Groutas, William C. (MDPI AG, Basel, Switzerland, 2019-02-25)
      Proteases are a major enzyme group playing important roles in a wide variety of biological processes in life forms ranging from viruses to mammalians. The aberrant activity of proteases can lead to various diseases; ...

    • Broad-spectrum antivirals against 3C or 3C-like proteases of picornavirus-like supercluster: picornaviruses, caliciviruses and coronaviruses 

      Chang, Kyeong-Ok; Kim, Yunjeong; Groutas, William C.; Hua, Duy; Saif, Linda J. (United States Patent and Trademark Office, 2016-10-25)
      Antiviral protease inhibitors, including peptidyl aldehydes, peptidyl .alpha.-ketoamides, peptidyl bisulfate salts, and peptidyl heterocycles, are disclosed, along with related antiviral compounds, and methods of using the ...

    • Broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, noroviruses, and coronaviruses 

      Kim, Yunjeong; Lovell, Scott; Tiew, Kok-Chuan; Mandadapu, Sivakoteswara Rao; Alliston, Kevin R.; Battaile, Kevin P.; Groutas, William C.; Chang, Kyeong-Ok (American Society of Microbiology, 2012-08-22)
      Phylogenetic analysis has demonstrated that some positive-sense RNA viruses can be classified into the picornavirus-like supercluster, which includes picornaviruses, caliciviruses, and coronaviruses. These viruses possess ...

    • Broad-spectrum cyclopropane-based inhibitors of coronavirus 3C-like proteases: Biochemical, structural, and virological studies 

      Dampalla, Chamandi S.; Nguyen, Harry Nhat; Rathnayake, Athri D.; Kim, Yunjeong; Perera, Krishani Dinali; Madden, Trent K.; Thurman, Hayden A.; Machen, Alexandra J.; Kashipathy, Maithri M.; Liu, Lijun; Battaile, Kevin P.; Lovell, Scott; Chang, Kyeong-Ok; Groutas, William C. (American Chemical Society, 2022-12-28)
      The advent of SARS-CoV-2, the causative agent of COVID-19, and its worldwide impact on global health, have provided the impetus for the development of effective countermeasures that can be deployed against the virus, ...

    • Broad-spectrum inhibitors against 3C-like proteases of feline coronaviruses and feline caliciviruses 

      Kim, Yunjeong; Shivanna, Vinay; Narayanan, Sanjeev; Prior, Allan M.; Weerasekara, Sahani; Hua, Duy H.; Kankanamalage, Anushka C. Galasiti; Groutas, William C.; Chang, Kyeong-Ok (American Society for Microbiology, 2015-05)
      Feline infectious peritonitis and virulent, systemic calicivirus infection are caused by certain types of feline coronaviruses (FCoVs) and feline caliciviruses (FCVs), respectively, and are important infectious diseases ...

    • Characterization of amino acid substitutions in feline coronavirus 3C-like protease from a cat with feline infectious peritonitis treated with a protease inhibitor 

      Perera, Krishani Dinali; Rathnayake, Athri D.; Liu, Hongwei; Pedersen, Niels C.; Groutas, William C.; Chang, Kyeong-Ok; Kim, Yunjeong (Elsevier, 2019-10)
      Feline infectious peritonitis (FIP) is a highly fatal disease caused by a virulent feline coronavirus in domestic and wild cats. We have previously reported the synthesis of potent coronavirus 3C-like protease (3CLpro) ...

    • Cyclosulfamide-based derivatives as inhibitors of noroviruses 

      Dou, Dengfeng; Mandadapu, Sivakoteswara Rao; Alliston, Kevin R.; Kim, Yunjeong; Chang, Kyeong-Ok; Groutas, William C. (Elsevier, 2011-10-20)
      An optimization campaign focused on improving pharmacological activity and physicochemical properties of a recently-identified class of cyclosulfamide-based norovirus inhibitors has been carried out. Dimeric compound 4 was ...

    • Dengue virus and West Nile virus protease inhibitors 

      Aravapalli, Sridhar (Wichita State University, 2013-05)
      Dengue virus and West Nile virus are important mosquito-borne pathogens of Flaviviridae family affecting millions of people worldwide and causing a severe global healthcare threat. However, currently there are no approved ...

    • Derivatives of 3-alkyl-N-hydroxysuccinimide: probing the effect of structure on bioactivity toward human leukocyte elastase 

      Groutas, William C.; Brubaker, Michael J.; Chong, Lee S.; Epp, Jeffrey B.; Huang, He; Keller, C. E.; McClenahan, Jerry J.; Givens, R. S.; Singh, R.; Zandler, Melvin E. (Harwood Academic Publishers, 1994-02-01)
      A structure-activity relationship study was conducted in order to probe the nature of the interaction between some 3-alkyl-N-hydroxysuccinimide derivatives and human leukocyte elastase. The structural features in substituent ...