{"id":{"repo_id":"wichita-thes","oai_identifier":"oai:null:10057/23434"},"canonical_url":"https://search.dev.ndltd.org/etd/wichita-thes/oai:null: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":"Wichita State University","degree_name":null,"degree_level":null,"degree_discipline":null,"degree_department":null,"school":null,"contributors":[],"advisors":["Pugh, Coleen"],"committee_chairs":[],"committee_members":[],"year":2022,"date_issued":"2022-05","date_published":"2022-05","updated_at":"2026-08-21T16:50:43Z","subjects":[],"languages":["en_US"],"rights":["© Copyright 2022 by Krishna Mohan Donavalli All Rights Reserved"],"rights_urls":[],"identifier_entries":[{"key":"dc:identifier.other","label":"Dc Identifier Other","values":["d22002s"],"render_values":[{"text":"d22002s","href":null,"code":true}]}]},"links":{"outbound_url":"https://soar.wichita.edu/handle/10057/23434","outbound_label":"Repository record","outbound_source":"dc:identifier.uri"},"source_record":{"url":"https://soar.wichita.edu/oai/request?verb=GetRecord&metadataPrefix=dim&identifier=oai%3Anull%3A10057%2F23434","prefix":"dim"},"metadata_groups":[{"id":"people","label":"People","entries":[{"key":"dc:contributor.advisor","label":"Advisor","values":["Pugh, Coleen"]},{"key":"dc:creator","label":"Author","values":["Donavalli, Krishna M."]}]},{"id":"academic_context","label":"Academic Context","entries":[{"key":"dc:date.accessioned","label":"Dc Date Accessioned","values":["2022-06-20T14:00:28Z"]},{"key":"dc:date.available","label":"Dc Date Available","values":["2022-06-20T14:00:28Z"]},{"key":"dc:date.issued","label":"Date","values":["2022-05"]},{"key":"dc:publisher","label":"Institution","values":["Wichita State University"]},{"key":"dc:type","label":"Dc Type","values":["Dissertation"]}]},{"id":"language_rights","label":"Language and Rights","entries":[{"key":"dc:language.iso","label":"Language (ISO)","values":["en_US"]},{"key":"dc:rights","label":"Dc Rights","values":["© Copyright 2022 by Krishna Mohan Donavalli All Rights Reserved"]}]},{"id":"identifiers","label":"Identifiers","entries":[{"key":"dc:identifier.other","label":"Dc Identifier Other","values":["d22002s"]},{"key":"dc:identifier.uri","label":"Identifier URI","values":["https://soar.wichita.edu/handle/10057/23434"]}]},{"id":"additional","label":"Additional Metadata","entries":[{"key":"dc:description","label":"Description","values":["Thesis (Ph.D.)-- Wichita State University, College of Liberal Arts and Sciences, Department of Chemistry and Biochemistry"]},{"key":"dc:description.abstract","label":"Abstract","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:contributor.advisor":["Pugh, Coleen"],"dc:creator":["Donavalli, Krishna M."],"dc:date.accessioned":["2022-06-20T14:00:28Z"],"dc:date.available":["2022-06-20T14:00:28Z"],"dc:date.issued":["2022-05"],"dc:description":["Thesis (Ph.D.)-- Wichita State University, College of Liberal Arts and Sciences, Department of Chemistry and Biochemistry"],"dc:description.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. 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