{"id":{"repo_id":"wichita-thes","oai_identifier":"oai:soar.wichita.edu:10057/23434"},"canonical_url":"https://search.dev.ndltd.org/etd/wichita-thes/oai:soar.wichita.edu:10057/23434","repository":{"repo_id":"wichita-thes","name":"Wichita State University","base_url":"https://soar.wichita.edu/oai/request"},"display":{"title":"Design, synthesis and biological evaluation of small molecules with potential antibacterial and antiviral activity","abstract":"In recent years, the ongoing explosion of antibiotic-resistance and viral infections has posed a major threat to global public health and called for the development of new therapeutics. Here, a set of novel compounds are designed, synthesized, and tested for antibacterial and antiviral activities. The synthetic small molecules included in the dissertation are nature-inspired indole derivatives. The indole nucleus is an essential element of several natural and synthetic products with significant biological properties. Recent research has highlighted the effect of indole-based compounds as potential antimicrobial and anticancer candidates. The first part of the dissertation is focused on a set of novel indole derivatives and describes their design, synthesis, and biological evaluation for potential antibiotic activity. Few compounds showed a significant reduction in the growth of standard and drug-resistant strains of gram-positive bacteria. Novel compounds GK517.3 and GK506.2Im inhibited bacterial growth of gram-positive bacteria, S. aureus and E. faecalis at 51.73 and 50.62 mg/mL, respectively and kills 99.9% of bacteria at 103.5 and 101.2 mg/mL, respectively. GK517.3 inhibited the growth of MRSA at 16.17 mg/mL and showed the bactericidal property at 32.35 mg/mL. The encouraging results of the novel indole derivatives pave a way for developing new therapeutic strategies using this unique scaffold to treat antibiotic resistance. The second part of the dissertation includes a novel one-pot synthesis method to furnish b-carboline dimer molecules. For the first time, antiviral activity of b-carboline dimers (GZ440/6) was evaluated against COVID-19 using cell-based assays. The data suggest that the GZ440/6 can inhibit the COVID-19 virus without any cytotoxicity and might include inhibition of virus attachment and/or entry into the cell.","abstract_html":"In recent years, the ongoing explosion of antibiotic-resistance and viral infections has posed a major threat to global public health and called for the development of new therapeutics. Here, a set of novel compounds are designed, synthesized, and tested for antibacterial and antiviral activities. The synthetic small molecules included in the dissertation are nature-inspired indole derivatives. The indole nucleus is an essential element of several natural and synthetic products with significant biological properties. Recent research has highlighted the effect of indole-based compounds as potential antimicrobial and anticancer candidates. The first part of the dissertation is focused on a set of novel indole derivatives and describes their design, synthesis, and biological evaluation for potential antibiotic activity. Few compounds showed a significant reduction in the growth of standard and drug-resistant strains of gram-positive bacteria. Novel compounds GK517.3 and GK506.2Im inhibited bacterial growth of gram-positive bacteria, S. aureus and E. faecalis at 51.73 and 50.62 mg/mL, respectively and kills 99.9% of bacteria at 103.5 and 101.2 mg/mL, respectively. GK517.3 inhibited the growth of MRSA at 16.17 mg/mL and showed the bactericidal property at 32.35 mg/mL. The encouraging results of the novel indole derivatives pave a way for developing new therapeutic strategies using this unique scaffold to treat antibiotic resistance. The second part of the dissertation includes a novel one-pot synthesis method to furnish b-carboline dimer molecules. For the first time, antiviral activity of b-carboline dimers (GZ440/6) was evaluated against COVID-19 using cell-based assays. The data suggest that the GZ440/6 can inhibit the COVID-19 virus without any cytotoxicity and might include inhibition of virus attachment and/or entry into the cell.","abstract_has_math":false,"creators":["Donavalli, Krishna M."],"institution":null,"degree_name":null,"degree_level":null,"degree_discipline":null,"degree_department":null,"school":null,"contributors":[],"advisors":[],"committee_chairs":[],"committee_members":[],"year":2022,"date_issued":"2022-05","date_published":"2022-05","updated_at":"2026-07-24T06:05:25Z","subjects":[],"languages":[],"rights":[],"rights_urls":[],"identifier_entries":[{"key":"dc:identifier","label":"Identifier","values":["hdl:10057/23434"],"render_values":[{"text":"hdl:10057/23434","href":null,"code":true}]}]},"links":{"outbound_url":null,"outbound_label":null,"outbound_source":null},"metadata_groups":[{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date.issued","label":"Date","values":["2022-05"]},{"key":"dc:type","label":"Dc Type","values":["Dissertation"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier","label":"Identifier","values":["hdl:10057/23434"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description.other","label":"Dc Description Other","values":["In recent years, the ongoing explosion of antibiotic-resistance and viral infections has posed a major threat to global public health and called for the development of new therapeutics. Here, a set of novel compounds are designed, synthesized, and tested for antibacterial and antiviral activities. The synthetic small molecules included in the dissertation are nature-inspired indole derivatives. The indole nucleus is an essential element of several natural and synthetic products with significant biological properties. Recent research has highlighted the effect of indole-based compounds as potential antimicrobial and anticancer candidates. The first part of the dissertation is focused on a set of novel indole derivatives and describes their design, synthesis, and biological evaluation for potential antibiotic activity. Few compounds showed a significant reduction in the growth of standard and drug-resistant strains of gram-positive bacteria. Novel compounds GK517.3 and GK506.2Im inhibited bacterial growth of gram-positive bacteria, S. aureus and E. faecalis at 51.73 and 50.62 mg/mL, respectively and kills 99.9% of bacteria at 103.5 and 101.2 mg/mL, respectively. GK517.3 inhibited the growth of MRSA at 16.17 mg/mL and showed the bactericidal property at 32.35 mg/mL. The encouraging results of the novel indole derivatives pave a way for developing new therapeutic strategies using this unique scaffold to treat antibiotic resistance. The second part of the dissertation includes a novel one-pot synthesis method to furnish b-carboline dimer molecules. For the first time, antiviral activity of b-carboline dimers (GZ440/6) was evaluated against COVID-19 using cell-based assays. The data suggest that the GZ440/6 can inhibit the COVID-19 virus without any cytotoxicity and might include inhibition of virus attachment and/or entry into the cell."]},{"key":"dc:title","label":"Title","values":["Design, synthesis and biological evaluation of small molecules with potential antibacterial and antiviral activity"]}]}],"canonical_facts":{"dc:date.issued":["2022-05"],"dc:description.other":["In recent years, the ongoing explosion of antibiotic-resistance and viral infections has posed a major threat to global public health and called for the development of new therapeutics. Here, a set of novel compounds are designed, synthesized, and tested for antibacterial and antiviral activities. The synthetic small molecules included in the dissertation are nature-inspired indole derivatives. The indole nucleus is an essential element of several natural and synthetic products with significant biological properties. Recent research has highlighted the effect of indole-based compounds as potential antimicrobial and anticancer candidates. The first part of the dissertation is focused on a set of novel indole derivatives and describes their design, synthesis, and biological evaluation for potential antibiotic activity. Few compounds showed a significant reduction in the growth of standard and drug-resistant strains of gram-positive bacteria. Novel compounds GK517.3 and GK506.2Im inhibited bacterial growth of gram-positive bacteria, S. aureus and E. faecalis at 51.73 and 50.62 mg/mL, respectively and kills 99.9% of bacteria at 103.5 and 101.2 mg/mL, respectively. GK517.3 inhibited the growth of MRSA at 16.17 mg/mL and showed the bactericidal property at 32.35 mg/mL. The encouraging results of the novel indole derivatives pave a way for developing new therapeutic strategies using this unique scaffold to treat antibiotic resistance. The second part of the dissertation includes a novel one-pot synthesis method to furnish b-carboline dimer molecules. For the first time, antiviral activity of b-carboline dimers (GZ440/6) was evaluated against COVID-19 using cell-based assays. The data suggest that the GZ440/6 can inhibit the COVID-19 virus without any cytotoxicity and might include inhibition of virus attachment and/or entry into the cell."],"dc:identifier":["hdl:10057/23434"],"dc:title":["Design, synthesis and biological evaluation of small molecules with potential antibacterial and antiviral activity"],"dc:type":["Dissertation"]},"updated_at":"2026-07-24T06:05:25Z"}