Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies
Two different benzimidazole analogues act as multimodal agent, first one as novel non-peptidic CCK-B receptor antagonist and similarly as potent anti-fungal agent, designated as [Bz-Im]. These compounds were synthesized and characterized by spectroscopic techniques such as FT-IR, NMR, EI-MS and also...
Gespeichert in:
| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2007-05, Vol.17 (10), p.2749-2755 |
|---|---|
| Hauptverfasser: | , , , , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 2755 |
|---|---|
| container_issue | 10 |
| container_start_page | 2749 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 17 |
| creator | Tiwari, Anjani K. Mishra, Anil K. Bajpai, Aruna Mishra, Pushpa Singh, Sweta Sinha, Deepa Singh, V.K. |
| description | Two different benzimidazole analogues act as multimodal agent, first one as novel non-peptidic CCK-B receptor antagonist and similarly as potent anti-fungal agent, designated as [Bz-Im]. These compounds were synthesized and characterized by spectroscopic techniques such as FT-IR, NMR, EI-MS and also evaluated for specific radiopharmaceuticals. Preliminary radiolabeling results with
99mTc and biological evaluation studies showed promising results for further evaluation in vivo. The efficiency of labeling was more than 97% and complex was stable for about 12
h at 30
°C in the presence of serum. Both ligands showed binding to most of the organs, known to express CCK receptors in biodistribution studies. Cholecystokinin (CCK
1 andCCK
2) receptor binding affinities of these analogues are, IC
50, 0.942
±
0.107 for compound C and 0.665
±
0.211 for compound D in rat pancreatic acini. The anti-fungal activity has shown inhibitory activity against
Aspergillus flavus and
Aspergillus niger. These studies have provided a new template for further development of non-peptidic ligands for diagnostic and therapeutic purposes of diseases related with CCK receptors as well as anti-microbes. |
| doi_str_mv | 10.1016/j.bmcl.2007.02.071 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_19913966</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X07002697</els_id><sourcerecordid>19913966</sourcerecordid><originalsourceid>FETCH-LOGICAL-c415t-f7f1e37031b793071d6eabe9230fad79adc1538bde5611104867f21a8df7056b3</originalsourceid><addsrcrecordid>eNp9kE1r3DAURUVpaKZp_0AXxZt2Z-c9y5Zs6KYJ_QiEZJEWCqUIWXpqNdhWItmGzK-vpzOQXVdvc-7lvsPYG4QCAcX5tugG0xclgCygLEDiM7bBSlQ5r6B-zjbQCsibtvpxyl6mtAXACqrqBTtFyUXTtM2GmbvHcfpDyadMjzajRfeznnwYs-Cym7BQn13QuPODt3oXesosRb-sxELZz4tdfjX8-hf0U8qitj6cdz704bc3us_SNFtP6RU7cbpP9Pp4z9j3z5--XX7Nr2-_XF1-vM5NhfWUO-mQuASOnWz5-o0VpDtqSw5OW9lqa7DmTWepFogIVSOkK1E31kmoRcfP2PtD730MDzOlSQ0-Gep7PVKYk8K2Rd4KsYLlATQxpBTJqfvoBx0fFYLaq1VbtVer9moVlGods4beHtvnbiD7FDm6XIF3R0Cn9XsX9Wh8euIayWusYeU-HDhaXSyeokrG02jI-khmUjb4_-34C1oxmBs</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>19913966</pqid></control><display><type>article</type><title>Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies</title><source>MEDLINE</source><source>Access via ScienceDirect (Elsevier)</source><creator>Tiwari, Anjani K. ; Mishra, Anil K. ; Bajpai, Aruna ; Mishra, Pushpa ; Singh, Sweta ; Sinha, Deepa ; Singh, V.K.</creator><creatorcontrib>Tiwari, Anjani K. ; Mishra, Anil K. ; Bajpai, Aruna ; Mishra, Pushpa ; Singh, Sweta ; Sinha, Deepa ; Singh, V.K.</creatorcontrib><description>Two different benzimidazole analogues act as multimodal agent, first one as novel non-peptidic CCK-B receptor antagonist and similarly as potent anti-fungal agent, designated as [Bz-Im]. These compounds were synthesized and characterized by spectroscopic techniques such as FT-IR, NMR, EI-MS and also evaluated for specific radiopharmaceuticals. Preliminary radiolabeling results with
99mTc and biological evaluation studies showed promising results for further evaluation in vivo. The efficiency of labeling was more than 97% and complex was stable for about 12
h at 30
°C in the presence of serum. Both ligands showed binding to most of the organs, known to express CCK receptors in biodistribution studies. Cholecystokinin (CCK
1 andCCK
2) receptor binding affinities of these analogues are, IC
50, 0.942
±
0.107 for compound C and 0.665
±
0.211 for compound D in rat pancreatic acini. The anti-fungal activity has shown inhibitory activity against
Aspergillus flavus and
Aspergillus niger. These studies have provided a new template for further development of non-peptidic ligands for diagnostic and therapeutic purposes of diseases related with CCK receptors as well as anti-microbes.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2007.02.071</identifier><identifier>PMID: 17368898</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>99mTc-labeled ; Animals ; Antibiotics. Antiinfectious agents. Antiparasitic agents ; Antifungal agents ; Antifungal Agents - chemical synthesis ; Antifungal Agents - pharmacology ; Aspergillus flavus ; Aspergillus niger ; Aspergillus niger - drug effects ; Benzimidazole ; Benzimidazoles - chemical synthesis ; Benzimidazoles - pharmacology ; Biodistribution ; Biological and medical sciences ; Contrast media. Radiopharmaceuticals ; Inhibitory Concentration 50 ; Medical sciences ; Microbial Sensitivity Tests ; Neuropharmacology ; Neurotransmitters. Neurotransmission. Receptors ; Non-peptidic ; Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems ; Pharmacology. Drug treatments ; Rabbits ; Radiolabeling ; Radiopharmaceuticals - pharmacology ; Receptor, Cholecystokinin B - antagonists & inhibitors ; Receptors, Cholecystokinin - antagonists & inhibitors ; Spectroscopy</subject><ispartof>Bioorganic & medicinal chemistry letters, 2007-05, Vol.17 (10), p.2749-2755</ispartof><rights>2007 Elsevier Ltd</rights><rights>2007 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-f7f1e37031b793071d6eabe9230fad79adc1538bde5611104867f21a8df7056b3</citedby><cites>FETCH-LOGICAL-c415t-f7f1e37031b793071d6eabe9230fad79adc1538bde5611104867f21a8df7056b3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2007.02.071$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=18735150$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/17368898$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Tiwari, Anjani K.</creatorcontrib><creatorcontrib>Mishra, Anil K.</creatorcontrib><creatorcontrib>Bajpai, Aruna</creatorcontrib><creatorcontrib>Mishra, Pushpa</creatorcontrib><creatorcontrib>Singh, Sweta</creatorcontrib><creatorcontrib>Sinha, Deepa</creatorcontrib><creatorcontrib>Singh, V.K.</creatorcontrib><title>Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Two different benzimidazole analogues act as multimodal agent, first one as novel non-peptidic CCK-B receptor antagonist and similarly as potent anti-fungal agent, designated as [Bz-Im]. These compounds were synthesized and characterized by spectroscopic techniques such as FT-IR, NMR, EI-MS and also evaluated for specific radiopharmaceuticals. Preliminary radiolabeling results with
99mTc and biological evaluation studies showed promising results for further evaluation in vivo. The efficiency of labeling was more than 97% and complex was stable for about 12
h at 30
°C in the presence of serum. Both ligands showed binding to most of the organs, known to express CCK receptors in biodistribution studies. Cholecystokinin (CCK
1 andCCK
2) receptor binding affinities of these analogues are, IC
50, 0.942
±
0.107 for compound C and 0.665
±
0.211 for compound D in rat pancreatic acini. The anti-fungal activity has shown inhibitory activity against
Aspergillus flavus and
Aspergillus niger. These studies have provided a new template for further development of non-peptidic ligands for diagnostic and therapeutic purposes of diseases related with CCK receptors as well as anti-microbes.</description><subject>99mTc-labeled</subject><subject>Animals</subject><subject>Antibiotics. Antiinfectious agents. Antiparasitic agents</subject><subject>Antifungal agents</subject><subject>Antifungal Agents - chemical synthesis</subject><subject>Antifungal Agents - pharmacology</subject><subject>Aspergillus flavus</subject><subject>Aspergillus niger</subject><subject>Aspergillus niger - drug effects</subject><subject>Benzimidazole</subject><subject>Benzimidazoles - chemical synthesis</subject><subject>Benzimidazoles - pharmacology</subject><subject>Biodistribution</subject><subject>Biological and medical sciences</subject><subject>Contrast media. Radiopharmaceuticals</subject><subject>Inhibitory Concentration 50</subject><subject>Medical sciences</subject><subject>Microbial Sensitivity Tests</subject><subject>Neuropharmacology</subject><subject>Neurotransmitters. Neurotransmission. Receptors</subject><subject>Non-peptidic</subject><subject>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</subject><subject>Pharmacology. Drug treatments</subject><subject>Rabbits</subject><subject>Radiolabeling</subject><subject>Radiopharmaceuticals - pharmacology</subject><subject>Receptor, Cholecystokinin B - antagonists & inhibitors</subject><subject>Receptors, Cholecystokinin - antagonists & inhibitors</subject><subject>Spectroscopy</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2007</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1r3DAURUVpaKZp_0AXxZt2Z-c9y5Zs6KYJ_QiEZJEWCqUIWXpqNdhWItmGzK-vpzOQXVdvc-7lvsPYG4QCAcX5tugG0xclgCygLEDiM7bBSlQ5r6B-zjbQCsibtvpxyl6mtAXACqrqBTtFyUXTtM2GmbvHcfpDyadMjzajRfeznnwYs-Cym7BQn13QuPODt3oXesosRb-sxELZz4tdfjX8-hf0U8qitj6cdz704bc3us_SNFtP6RU7cbpP9Pp4z9j3z5--XX7Nr2-_XF1-vM5NhfWUO-mQuASOnWz5-o0VpDtqSw5OW9lqa7DmTWepFogIVSOkK1E31kmoRcfP2PtD730MDzOlSQ0-Gep7PVKYk8K2Rd4KsYLlATQxpBTJqfvoBx0fFYLaq1VbtVer9moVlGods4beHtvnbiD7FDm6XIF3R0Cn9XsX9Wh8euIayWusYeU-HDhaXSyeokrG02jI-khmUjb4_-34C1oxmBs</recordid><startdate>20070515</startdate><enddate>20070515</enddate><creator>Tiwari, Anjani K.</creator><creator>Mishra, Anil K.</creator><creator>Bajpai, Aruna</creator><creator>Mishra, Pushpa</creator><creator>Singh, Sweta</creator><creator>Sinha, Deepa</creator><creator>Singh, V.K.</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>M7N</scope><scope>P64</scope></search><sort><creationdate>20070515</creationdate><title>Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies</title><author>Tiwari, Anjani K. ; Mishra, Anil K. ; Bajpai, Aruna ; Mishra, Pushpa ; Singh, Sweta ; Sinha, Deepa ; Singh, V.K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c415t-f7f1e37031b793071d6eabe9230fad79adc1538bde5611104867f21a8df7056b3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2007</creationdate><topic>99mTc-labeled</topic><topic>Animals</topic><topic>Antibiotics. Antiinfectious agents. Antiparasitic agents</topic><topic>Antifungal agents</topic><topic>Antifungal Agents - chemical synthesis</topic><topic>Antifungal Agents - pharmacology</topic><topic>Aspergillus flavus</topic><topic>Aspergillus niger</topic><topic>Aspergillus niger - drug effects</topic><topic>Benzimidazole</topic><topic>Benzimidazoles - chemical synthesis</topic><topic>Benzimidazoles - pharmacology</topic><topic>Biodistribution</topic><topic>Biological and medical sciences</topic><topic>Contrast media. Radiopharmaceuticals</topic><topic>Inhibitory Concentration 50</topic><topic>Medical sciences</topic><topic>Microbial Sensitivity Tests</topic><topic>Neuropharmacology</topic><topic>Neurotransmitters. Neurotransmission. Receptors</topic><topic>Non-peptidic</topic><topic>Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems</topic><topic>Pharmacology. Drug treatments</topic><topic>Rabbits</topic><topic>Radiolabeling</topic><topic>Radiopharmaceuticals - pharmacology</topic><topic>Receptor, Cholecystokinin B - antagonists & inhibitors</topic><topic>Receptors, Cholecystokinin - antagonists & inhibitors</topic><topic>Spectroscopy</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Tiwari, Anjani K.</creatorcontrib><creatorcontrib>Mishra, Anil K.</creatorcontrib><creatorcontrib>Bajpai, Aruna</creatorcontrib><creatorcontrib>Mishra, Pushpa</creatorcontrib><creatorcontrib>Singh, Sweta</creatorcontrib><creatorcontrib>Sinha, Deepa</creatorcontrib><creatorcontrib>Singh, V.K.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biotechnology and BioEngineering Abstracts</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Tiwari, Anjani K.</au><au>Mishra, Anil K.</au><au>Bajpai, Aruna</au><au>Mishra, Pushpa</au><au>Singh, Sweta</au><au>Sinha, Deepa</au><au>Singh, V.K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2007-05-15</date><risdate>2007</risdate><volume>17</volume><issue>10</issue><spage>2749</spage><epage>2755</epage><pages>2749-2755</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Two different benzimidazole analogues act as multimodal agent, first one as novel non-peptidic CCK-B receptor antagonist and similarly as potent anti-fungal agent, designated as [Bz-Im]. These compounds were synthesized and characterized by spectroscopic techniques such as FT-IR, NMR, EI-MS and also evaluated for specific radiopharmaceuticals. Preliminary radiolabeling results with
99mTc and biological evaluation studies showed promising results for further evaluation in vivo. The efficiency of labeling was more than 97% and complex was stable for about 12
h at 30
°C in the presence of serum. Both ligands showed binding to most of the organs, known to express CCK receptors in biodistribution studies. Cholecystokinin (CCK
1 andCCK
2) receptor binding affinities of these analogues are, IC
50, 0.942
±
0.107 for compound C and 0.665
±
0.211 for compound D in rat pancreatic acini. The anti-fungal activity has shown inhibitory activity against
Aspergillus flavus and
Aspergillus niger. These studies have provided a new template for further development of non-peptidic ligands for diagnostic and therapeutic purposes of diseases related with CCK receptors as well as anti-microbes.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>17368898</pmid><doi>10.1016/j.bmcl.2007.02.071</doi><tpages>7</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2007-05, Vol.17 (10), p.2749-2755 |
| issn | 0960-894X 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_19913966 |
| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | 99mTc-labeled Animals Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal agents Antifungal Agents - chemical synthesis Antifungal Agents - pharmacology Aspergillus flavus Aspergillus niger Aspergillus niger - drug effects Benzimidazole Benzimidazoles - chemical synthesis Benzimidazoles - pharmacology Biodistribution Biological and medical sciences Contrast media. Radiopharmaceuticals Inhibitory Concentration 50 Medical sciences Microbial Sensitivity Tests Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Non-peptidic Peptidergic system (neuropeptide, opioid peptide, opiates...). Adenosinergic and purinergic systems Pharmacology. Drug treatments Rabbits Radiolabeling Radiopharmaceuticals - pharmacology Receptor, Cholecystokinin B - antagonists & inhibitors Receptors, Cholecystokinin - antagonists & inhibitors Spectroscopy |
| title | Synthesis and evaluation of Novel Benzimidazole derivative [Bz-Im] and its radio/biological studies |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-24T22%3A54%3A41IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Synthesis%20and%20evaluation%20of%20Novel%20Benzimidazole%20derivative%20%5BBz-Im%5D%20and%20its%20radio/biological%20studies&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Tiwari,%20Anjani%20K.&rft.date=2007-05-15&rft.volume=17&rft.issue=10&rft.spage=2749&rft.epage=2755&rft.pages=2749-2755&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2007.02.071&rft_dat=%3Cproquest_cross%3E19913966%3C/proquest_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=19913966&rft_id=info:pmid/17368898&rft_els_id=S0960894X07002697&rfr_iscdi=true |