Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials
Nowadays, the growth of drug-resistant microbial strains (MDRs) is a serious public health threat worldwide. Moreover, tens of millions of people are annually diagnosed with cancer worldwide, and more than half of patients ultimately die. In the present study, a new series of 2-(4-substituted-thiazo...
| Main Authors: | , , , |
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| Format: | Article |
| Language: | English |
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Elsevier
2020-05-01
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| Series: | Arabian Journal of Chemistry |
| Subjects: | |
| Online Access: | http://www.sciencedirect.com/science/article/pii/S1878535220300824 |
| _version_ | 1811324987119763456 |
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| author | Essam M. Hussein Munirah M. Al-Rooqi Amal A. Elkhawaga Saleh A. Ahmed |
| author_facet | Essam M. Hussein Munirah M. Al-Rooqi Amal A. Elkhawaga Saleh A. Ahmed |
| author_sort | Essam M. Hussein |
| collection | DOAJ |
| description | Nowadays, the growth of drug-resistant microbial strains (MDRs) is a serious public health threat worldwide. Moreover, tens of millions of people are annually diagnosed with cancer worldwide, and more than half of patients ultimately die. In the present study, a new series of 2-(4-substituted-thiazol-2-ylamino)acetamides and N-(4-substituted-thiazol-2-yl)acetamides incorporating sulfonamide moieties were designed, synthesized, well-characterized and successfully evaluated for their antimicrobial activity against multidrug resistant strains and screened for cytotoxic activity against normal lung fibroblast (WI-38), human lung carcinoma (A549), and human breast carcinoma (MDA-MB-231) cell lines. Fluorescence-activated cell sorting (FACS) analysis and molecular modeling study were performed to identify the mode of action of the novel synthesized compounds and their binding interactions with the active sites of dihydrofolate reductase enzyme (DHFR). |
| first_indexed | 2024-04-13T14:25:16Z |
| format | Article |
| id | doaj.art-7557127f32c345cb8b51ecba92f7b67d |
| institution | Directory Open Access Journal |
| issn | 1878-5352 |
| language | English |
| last_indexed | 2024-04-13T14:25:16Z |
| publishDate | 2020-05-01 |
| publisher | Elsevier |
| record_format | Article |
| series | Arabian Journal of Chemistry |
| spelling | doaj.art-7557127f32c345cb8b51ecba92f7b67d2022-12-22T02:43:21ZengElsevierArabian Journal of Chemistry1878-53522020-05-0113553455362Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentialsEssam M. Hussein0Munirah M. Al-Rooqi1Amal A. Elkhawaga2Saleh A. Ahmed3Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia; Chemistry Department, Faculty of Science, Assiut University, 71516 Assiut, Egypt; Corresponding authors at: Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia.Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi ArabiaDepartment of Medical Microbiology & Immunology, Faculty of Medicine Assiut University, 71516 Assiut, EgyptDepartment of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia; Chemistry Department, Faculty of Science, Assiut University, 71516 Assiut, Egypt; Corresponding authors at: Department of Chemistry, Faculty of Applied Science, Umm Al-Qura University, 21955 Makkah, Saudi Arabia.Nowadays, the growth of drug-resistant microbial strains (MDRs) is a serious public health threat worldwide. Moreover, tens of millions of people are annually diagnosed with cancer worldwide, and more than half of patients ultimately die. In the present study, a new series of 2-(4-substituted-thiazol-2-ylamino)acetamides and N-(4-substituted-thiazol-2-yl)acetamides incorporating sulfonamide moieties were designed, synthesized, well-characterized and successfully evaluated for their antimicrobial activity against multidrug resistant strains and screened for cytotoxic activity against normal lung fibroblast (WI-38), human lung carcinoma (A549), and human breast carcinoma (MDA-MB-231) cell lines. Fluorescence-activated cell sorting (FACS) analysis and molecular modeling study were performed to identify the mode of action of the novel synthesized compounds and their binding interactions with the active sites of dihydrofolate reductase enzyme (DHFR).http://www.sciencedirect.com/science/article/pii/S1878535220300824SulfonamideAnticancerAntimicrobialFluorescence-activated cell sorting (FACS)ThiazoleMultidrug resistant strains |
| spellingShingle | Essam M. Hussein Munirah M. Al-Rooqi Amal A. Elkhawaga Saleh A. Ahmed Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials Arabian Journal of Chemistry Sulfonamide Anticancer Antimicrobial Fluorescence-activated cell sorting (FACS) Thiazole Multidrug resistant strains |
| title | Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials |
| title_full | Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials |
| title_fullStr | Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials |
| title_full_unstemmed | Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials |
| title_short | Tailoring of novel biologically active molecules based on N4-substituted sulfonamides bearing thiazole moiety exhibiting unique multi-addressable biological potentials |
| title_sort | tailoring of novel biologically active molecules based on n4 substituted sulfonamides bearing thiazole moiety exhibiting unique multi addressable biological potentials |
| topic | Sulfonamide Anticancer Antimicrobial Fluorescence-activated cell sorting (FACS) Thiazole Multidrug resistant strains |
| url | http://www.sciencedirect.com/science/article/pii/S1878535220300824 |
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