Organic Communications最新文献

An efficient synthesis of quinoxaline derivatives using HCTU as catalyst in DMF 在 DMF 中以 HCTU 为催化剂高效合成喹喔啉衍生物

IF 1.7

Organic Communications Pub Date : 2023-12-13 DOI: 10.25135/acg.oc.160.2308.2876

Nitin A. Sasane, B. Popatkar, G. Meshram

引用次数: 0

Synthesis and bioactivity of 1-substituted tetrahydroisoquinolines derived from phenolic aldehydes 酚醛衍生的 1-取代四氢异喹啉的合成与生物活性

IF 1.7

Organic Communications Pub Date : 2023-11-30 DOI: 10.25135/acg.oc.159.2310.2920

Muamer Dizdar, M. Maksimović, Anela Topčagić, M. Avdic, Danijela Vidic

{"title":"Synthesis and bioactivity of 1-substituted tetrahydroisoquinolines derived from phenolic aldehydes","authors":"Muamer Dizdar, M. Maksimović, Anela Topčagić, M. Avdic, Danijela Vidic","doi":"10.25135/acg.oc.159.2310.2920","DOIUrl":"https://doi.org/10.25135/acg.oc.159.2310.2920","url":null,"abstract":": Phenolic aldehydes and their derivatives found in nature are well-known for their potential biological activity. In this study, four 1-substituted 1,2,3,4-tetrahydroisoquinolines (THIQs) derived from phenolic aldehydes were synthesized by phosphate buffer mediated Pictet-Spengler reaction. All derivatives were chemically and structurally characterized by elemental CHN analysis and spectroscopic methods (IR, HR-ESI-MS, 1 H-and 13 C-NMR). 1-Substituted THIQs derived from 3,4-dihydroxybenzaldehyde and 4-hydroxy-3-methoxybenzaldehyde were described for the first time. In order to cover the diversity of the mechanistic approach, but also to establish the relationship between structure and activity, antioxidant activity was examined by five different in vitro methods, namely: neutralization and reduction of stable free radicals 2,2-diphenyl-1-picrylhydrazyl and radical cation derived from [(2,2´-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)], ferric reducing antioxidant power, oxygen radical absorbance capacity, and ability to chelate Fe(II) ions. In vitro inhibition of acetylcholinesterase (AChE) was examined by the Ellman's colorimetric method, while computer-simulated docking was used to reveal the preferred binding site and major interaction between AChE and THIQs. Antibacterial testing was examined using the agar well method and results were presented in the form of zones of inhibition (mm).","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":"20 3","pages":""},"PeriodicalIF":1.7,"publicationDate":"2023-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"139206312","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}

引用次数: 0

Synthesis and antimicrobial activities of unsymmetrical thioditetrazoles and their precursor thiotetrazoles 不对称硫代四唑及其前体硫代四唑的合成及其抗菌活性

Organic Communications Pub Date : 2023-10-29 DOI: 10.25135/acg.oc.158.2309.2893

Ali Dişli, Doğukan Doyduk, Özge Çağlar Teknikel, Hatice Öğütcü

引用次数: 0

Water extract of onion: chemoselective synthesis of 2-substituted benzimidazole derivatives 洋葱水提物:2取代苯并咪唑衍生物的化学选择性合成

Organic Communications Pub Date : 2023-10-26 DOI: 10.25135/acg.oc.157.2305.2790

Muthu Seenivasa Perumal, Kaliyan Prabakaran, Selvaraj Loganathan, Ayyavu Boomathi, Eswaran Rajendran, Govindaraj Mahalakshmi

引用次数: 0

Erratum to “Facile microwave synthesis of a novel phenothiazine derivative and its cytotoxic activity” [Org. Commun. 13:4 (2020) 175-183] 对 "新型吩噻嗪衍生物的简便微波合成及其细胞毒性活性 "的勘误 [Org.

IF 1.7

Organic Communications Pub Date : 2023-09-29 DOI: 10.25135/acg.oc.148.2303.28001

Cenk A Andac

引用次数: 0

Molecular modeling, synthesis and characterization of FOLR1 specific peptides for tumor targeting activity 肿瘤靶向活性FOLR1特异性肽的分子建模、合成和表征

Organic Communications Pub Date : 2023-09-29 DOI: 10.25135/acg.oc.158.2308.2887

Özgür Yılmaz

引用次数: 0

Synthesis, spectral characterization and biological evaluation of carbamate and sulfonamide derivatives of cis-tramadol 顺曲马多氨基甲酸酯和磺酰胺衍生物的合成、光谱表征及生物学评价

Organic Communications Pub Date : 2023-09-29 DOI: 10.25135/acg.oc.157.2307.2834

Mavallur Varalakshmi, Venkata Lakshmi Reddy Sana, Kiran Yerragudibathal Reddy, Swarupa Chinthala, Venkata Ramana Katla, Chamarthi Naga Raju

引用次数: 0

Asymmetric transfer hydrogenation of a new N-tosyltetrahydrocarbazole-1-one ester with the Noyori-Ikariya catalyst Noyori-Ikariya催化剂催化新型N-tosyltetrahydrocarbazole-1-one酯的不对称转移加氢反应

Organic Communications Pub Date : 2023-09-29 DOI: 10.25135/acg.oc2307.2838

Erkan Ertürk, Ömer Dİlek

引用次数: 0

Synthesis and biological evaluation of [1,2,3]triazolo[4',5':3,4]pyrrolo[1,2-a] indoles: one-pot reaction under microwave irradiation 微波辐照下[1,2,3]三唑[4'，5':3,4]吡咯[1,2-a]吲哚的合成及生物学评价

Organic Communications Pub Date : 2023-09-29 DOI: 10.25135/acg.oc.155.2307.2833

Koppula Shiva Kumar, Abhilasha Dubba

引用次数: 0

Novel oxalamide derivatives for COXs expression and breast cancer: design, synthesis, biological evaluation, and docking studies 用于cox表达和乳腺癌的新型草酰胺衍生物:设计、合成、生物学评价和对接研究

IF 1.7

Organic Communications Pub Date : 2023-08-15 DOI: 10.25135/acg.oc.154.2306.2820

B. Kuzu, C. Hepokur, Ö. Algül

{"title":"Novel oxalamide derivatives for COXs expression and breast cancer: design, synthesis, biological evaluation, and docking studies","authors":"B. Kuzu, C. Hepokur, Ö. Algül","doi":"10.25135/acg.oc.154.2306.2820","DOIUrl":"https://doi.org/10.25135/acg.oc.154.2306.2820","url":null,"abstract":": In the present study, new oxalamide-based compounds were designed from thalidomide and synthesized easily and with high yields (from 69% up to 93%) by a two-step method. The antiproliferative effects of synthesized 6a-d and 7a-d compounds on (ER+) MCF-7 and (ER-) MDA-MB-231 breast cancer cell line and human fibroblast WI-38 healthy cell line were investigated by the MTT method. The results showed that compound 7d was the most potent candidate against both MCF-7 and MDA-MB-231 cell lines with IC 50 = 4.72 µM and 6.37 µM, respectively. To investigate whether antiproliferative effect of the compounds on breast cancer cell lines is dependent on COXs, expressions of COX-1/2 on the MCF-7 cell line were investigated by the Western-Blot technique. Among synthesized compounds, compound 7d increased the expression of both COX-1 and COX-2. The inhibition potential of compounds on COX-1/2 enzymes was investigated by molecular docking compared to inhibitor co-ligand celecoxib in crystal structures of COX-1 (PDB ID: 3KK6) and COX-2 (PDB ID: 3LN1). Docking results indeed showed that compound 7d had a higher binding affinity for both COX-1 and COX-2 active sites. Consequently, the novel oxalamide-based compounds presented here may be important candidate molecules for the development of new COX-dependent antiproliferative agents.","PeriodicalId":19553,"journal":{"name":"Organic Communications","volume":" ","pages":""},"PeriodicalIF":1.7,"publicationDate":"2023-08-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"49016106","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}

引用次数: 0