Pub Date : 2020-12-12DOI: 10.25135/acg.bmcr.22.20.07.1706
Nebih Lolak, Muhammed Tuneğ, Asli E Dogan, M. Boğa, Suleyman Akocak
A series of twenty 1,3,5-triazine-substituted ureido benzenesulfonamides 2 (a-e) and 3 (a-o) were re-synthesized and assayed for antioxidant properties by using several different methods including 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay, 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radical decolarization assay, metal chelating and cupric reducing antioxidant capacity (CUPRAC) methods. The inhibitory effects of compounds on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes have been also demonstrated. All compounds showed a greater antioxidant capacity against ABTS assay by having a more potent activity than the standards BHT, BHA and α-TOC. In general, all compounds were non susceptible to against AChE enzyme. On the other hand, several lead compounds were obtained from the current series against BChE enzyme. More specifically, compound 3m showed great inhibition profile against BChE with % inhibition value of 93.77, which is better than the standard drug galantamine (% inhibition value of 87.86).
重新合成了20种1,3,5-三嗪取代的脲基苯磺酰胺2 (A -e)和3 (A -o)，并采用1,1-二苯基-2-吡啶酰肼(DPPH)自由基清除法、2,2 ' -氮基-双-(3-乙基苯并噻唑-6-磺酸)(ABTS)阳离子自由基脱色法、金属螯合法和铜还原抗氧化能力(CUPRAC)法测定了它们的抗氧化性能。化合物对乙酰胆碱酯酶(AChE)和丁基胆碱酯酶(BChE)也有抑制作用。所有化合物均比BHT、BHA和α-TOC具有更强的抗氧化能力。总的来说，所有化合物对乙酰胆碱酯酶均不敏感。另一方面，从目前的系列中获得了几个针对BChE酶的先导化合物。其中，化合物3m对BChE的抑制率为93.77 %，优于标准药物加兰他明(87.86 %)。
{"title":"Synthesis and biological evaluation of 1,3,5-triazine-substituted ureido benzenesulfonamides as antioxidant, acetylcholinesterase and butyrylcholinesterase inhibitors","authors":"Nebih Lolak, Muhammed Tuneğ, Asli E Dogan, M. Boğa, Suleyman Akocak","doi":"10.25135/acg.bmcr.22.20.07.1706","DOIUrl":"https://doi.org/10.25135/acg.bmcr.22.20.07.1706","url":null,"abstract":"A series of twenty 1,3,5-triazine-substituted ureido benzenesulfonamides 2 (a-e) and 3 (a-o) were re-synthesized and assayed for antioxidant properties by using several different methods including 1,1-diphenyl-2-picryl hydrazyl (DPPH) free radical scavenging assay, 2,2′-azino-bis-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) cation radical decolarization assay, metal chelating and cupric reducing antioxidant capacity (CUPRAC) methods. The inhibitory effects of compounds on acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes have been also demonstrated. All compounds showed a greater antioxidant capacity against ABTS assay by having a more potent activity than the standards BHT, BHA and α-TOC. In general, all compounds were non susceptible to against AChE enzyme. On the other hand, several lead compounds were obtained from the current series against BChE enzyme. More specifically, compound 3m showed great inhibition profile against BChE with % inhibition value of 93.77, which is better than the standard drug galantamine (% inhibition value of 87.86).","PeriodicalId":8932,"journal":{"name":"Bioorganic and Medicinal Chemistry Reports","volume":"17 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81472521","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2018-12-31DOI: 10.25135/bmcr.10.18.12.1104
B. Kuzu, Nurettin Menges
{"title":"Analyzing of Some Drugable Properties of Hydrazono-pyridazinones","authors":"B. Kuzu, Nurettin Menges","doi":"10.25135/bmcr.10.18.12.1104","DOIUrl":"https://doi.org/10.25135/bmcr.10.18.12.1104","url":null,"abstract":"","PeriodicalId":8932,"journal":{"name":"Bioorganic and Medicinal Chemistry Reports","volume":"72 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86303702","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2018-12-31DOI: 10.25135/BMCR.15.18.12.1124
B. Dur, R. Ozen, Furkan Ayaz
{"title":"Citric acid synthesis efficiency of Aspergillus niger in carob molasses based media","authors":"B. Dur, R. Ozen, Furkan Ayaz","doi":"10.25135/BMCR.15.18.12.1124","DOIUrl":"https://doi.org/10.25135/BMCR.15.18.12.1124","url":null,"abstract":"","PeriodicalId":8932,"journal":{"name":"Bioorganic and Medicinal Chemistry Reports","volume":"9 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84201309","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2018-12-31DOI: 10.25135/bmcr.09.18.01.001
Oztekin Algul
{"title":"Welcome to the first issue of BioorgMedChemRep for 2018!","authors":"Oztekin Algul","doi":"10.25135/bmcr.09.18.01.001","DOIUrl":"https://doi.org/10.25135/bmcr.09.18.01.001","url":null,"abstract":"","PeriodicalId":8932,"journal":{"name":"Bioorganic and Medicinal Chemistry Reports","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77216628","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2018-12-31DOI: 10.25135/BMCR.12.18.11.1035
Esen Yıldız Bekfelavi, Pınar Çevik, Ö. Yılmaz, N. S. Kus, G. Coral, A. Çelik
{"title":"The synthesis of two novel bicyclic haloketones and measurement of their biological activity","authors":"Esen Yıldız Bekfelavi, Pınar Çevik, Ö. Yılmaz, N. S. Kus, G. Coral, A. Çelik","doi":"10.25135/BMCR.12.18.11.1035","DOIUrl":"https://doi.org/10.25135/BMCR.12.18.11.1035","url":null,"abstract":"","PeriodicalId":8932,"journal":{"name":"Bioorganic and Medicinal Chemistry Reports","volume":"66 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81460197","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2018-12-31DOI: 10.25135/BMCR.11.18.09.899
Furkan Ayaz
Especially in elderly women osteoporosis leads to decline in the strength of the bone tissue by erosion of its mass. Weakened bone tissue is more prone to breaks. Patients mostly realize this situation after having a bone breakage especially with the wrist and hip fractures. There has not been an effective way of improving this debilitating condition. A new approach aiming to regulate the activities of the immune system cells in order to reverse osteoporosis and push the tissue for the formation of the bone structure gained attention due to its promising potential. In this review, I will be focusing on this approach by regulation of the macrophage activity, the major immune cell type that is involved in the bone formation. Immunomodulation of the macrophages enable formation and healing of the bone tissue in the patients and conducting more studies in this area would certainly improve the quality of the applicable medicines.
{"title":"Immunomodulation of macrophages for bone formation","authors":"Furkan Ayaz","doi":"10.25135/BMCR.11.18.09.899","DOIUrl":"https://doi.org/10.25135/BMCR.11.18.09.899","url":null,"abstract":"Especially in elderly women osteoporosis leads to decline in the strength of the bone tissue by erosion of its mass. Weakened bone tissue is more prone to breaks. Patients mostly realize this situation after having a bone breakage especially with the wrist and hip fractures. There has not been an effective way of improving this debilitating condition. A new approach aiming to regulate the activities of the immune system cells in order to reverse osteoporosis and push the tissue for the formation of the bone structure gained attention due to its promising potential. In this review, I will be focusing on this approach by regulation of the macrophage activity, the major immune cell type that is involved in the bone formation. Immunomodulation of the macrophages enable formation and healing of the bone tissue in the patients and conducting more studies in this area would certainly improve the quality of the applicable medicines.","PeriodicalId":8932,"journal":{"name":"Bioorganic and Medicinal Chemistry Reports","volume":"67 1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83075341","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2018-12-31DOI: 10.25135/BMCR.10.18.12.110486
Z. Kudaş
{"title":"Electrochemical studies of regorafenib in non-aqueous media","authors":"Z. Kudaş","doi":"10.25135/BMCR.10.18.12.110486","DOIUrl":"https://doi.org/10.25135/BMCR.10.18.12.110486","url":null,"abstract":"","PeriodicalId":8932,"journal":{"name":"Bioorganic and Medicinal Chemistry Reports","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2018-12-31","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84232870","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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