Fang, Yuanying Zhang, Shaokun Li, Min Xiong, Lijuan Tu, Liangxing Xie, Saisai Jin, Yi Liu, Yanhua Yang, Zunhua Liu, Ronghua
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Published in
Journal of enzyme inhibition and medicinal chemistry
GPR119 is a promising target for discovery of anti-type 2 diabetes mellitus agents. We described the optimisation of a novel series of pyrimido[5,4-b][1,4]oxazine derivatives as GPR119 agonists. Most designed compounds exhibited good agonistic activities. Among them, compound 10 and 15 demonstrated the potent EC50 values (13 and 12 nM, respectively...
Ali, M Barakat, Assem El-Faham, Ayman Al-Rasheed, Hessa H Dahlous, Kholoud Al-Majid, Abdullah Mohammed Sharma, Anamika Yousuf, Sammer Sanam, Mehar Ul-Haq, Zaheer
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Published in
Journal of enzyme inhibition and medicinal chemistry
A new series of thiobarbituric (thiopyrimidine trione) enamine derivatives and its analogues barbituric acid derivatives was synthesised, characterised, and screen for in vitro evaluation of α-glucosidase enzyme inhibition and anti-glycation activity. This series of compounds were found to inhibit α-glucosidase activity in a reversible mixed-type m...
Pustenko, Aleksandrs Nocentini, Alessio Balašova, Anastasija Krasavin, Mikhail Žalubovskis, Raivis Supuran, Claudiu T
Published in
Journal of enzyme inhibition and medicinal chemistry
A series of 3H-1,2-benzoxathiepine 2,2-dioxides incorporating 7-acylamino moieties were obtained by an original procedure starting from 5-nitrosalicylaldehyde, which was treated with propenylsulfonyl chloride followed by Wittig reaction of the bis-olefin intermediate. The new derivatives, belonging to the homosulfocoumarin chemotype, were assayed a...
Kim, Suwon Jo, Seri Kim, Mi-Sun Shin, Dong Hae
Published in
Journal of enzyme inhibition and medicinal chemistry
Frequent occurrences of multi-drug resistance of pathogenic Gram-negative bacteria threaten human beings. The CMP-2-keto-3-deoxy-d-manno-octulosonic acid biosynthesis pathway is one of the new targets for antibiotic design. 2-Keto-3-deoxy-d-manno-octulosonate cytidylyltransferase (KdsB) is the key enzyme in this pathway. KdsB proteins from Burkhold...
Song, Yoojin Park, Sun You Wu, Zhexue Liu, Kwang-Hyeon Seo, Young Ho
Published in
Journal of enzyme inhibition and medicinal chemistry
Chlorambucil is a nitrogen mustard-based DNA alkylating drug, which is widely used as a front-line treatment of chronic lymphocytic leukaemia (CLL). Despite its widespread application and success for the initial treatment of leukaemia, a majority of patients eventually develop acquired resistance to chlorambucil. In this regard, we have designed an...
Hou, Zhuang Li, Chuanchao Liu, Yichuang Zhang, Miao Wang, Yitong Fan, Zhanfang Guo, Chun Lin, Bin Liu, Yang
Published in
Journal of enzyme inhibition and medicinal chemistry
A series of new carbohydrate-based sulphonamide derivatives were designed, synthesised by employing the so-call 'sugar-tail' approach. The compounds were evaluated in vitro against a panel of CAs. Compared to their parent compound p-sulfamoylbenzoic acid, these compounds showed nearly 100-fold improvement in their binding affinities against hCA II ...
Guillon, Jean Cohen, Anita Boudot, Clotilde Valle, Alessandra Milano, Vittoria Das, Rabindra Nath Guédin, Aurore Moreau, Stéphane Ronga, Luisa Savrimoutou, Solène
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Published in
Journal of enzyme inhibition and medicinal chemistry
A series of new 2,4-bis[(substituted-aminomethyl)phenyl]quinoline, 1,3-bis[(substituted-aminomethyl)phenyl]isoquinoline, and 2,4-bis[(substituted-aminomethyl)phenyl]quinazoline derivatives was designed, synthesised, and evaluated in vitro against three protozoan parasites (Plasmodium falciparum, Leishmania donovani, and Trypanosoma brucei brucei). ...
Durgun, Mustafa Türkeş, Cüneyt Işık, Mesut Demir, Yeliz Saklı, Ali Kuru, Ali Güzel, Abdussamat Beydemir, Şükrü Akocak, Suleyman Osman, Sameh M
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Published in
Journal of enzyme inhibition and medicinal chemistry
Sulphonamides are biologically important compounds with low toxicity, many bioactivities and cost-effectiveness. Eight sulphonamide derivatives were synthesised and characterised by FT-IR, 13C NMR, 1H NMR, LC-MS and elemental analysis. Their inhibitory effect on AChE, and carbonic anhydrase I and II enzyme activities was investigated. Their antioxi...
Dizdaroglu, Yazgı Albay, Canan Arslan, Tayfun Ece, Abdulilah Turkoglu, Emir A Efe, Asiye Senturk, Murat Supuran, Claudiu T Ekinci, Deniz
Published in
Journal of enzyme inhibition and medicinal chemistry
In this study, newly synthesised compounds 6, 8, 10 and other compounds (1-5, 7 and 9) and their inhibitory properties against the human isoforms hCA I and hCA II were reported for the first time. Compounds 1-10 showed effective inhibition profiles with KI values in the range of 5.13-16.9 nM for hCA I and of 11.77-67.39 nM against hCA II, respectiv...
Abdelrahman, Mohamed A Eldehna, Wagdy M Nocentini, Alessio Ibrahim, Hany S Almahli, Hadia Abdel-Aziz, Hatem A Abou-Seri, Sahar M Supuran, Claudiu T
Published in
Journal of enzyme inhibition and medicinal chemistry
Pursuing on our efforts toward searching for efficient hCA IX and hCA XII inhibitors, herein we report the design and synthesis of new sets of benzofuran-based sulphonamides (4a,b, 5a,b, 9a-c, and 10a-d), featuring the zinc anchoring benzenesulfonamide moiety linked to a benzofuran tail via a hydrazine or hydrazide linker. All the target benzofuran...
