Exploring structure-activity relationship of S-substituted 2-mercaptoquinazolin-4(3H)-one including 4-ethylbenzenesulfonamides as human carbonic anhydrase inhibitors

by Adel S. El-Azab, Alaa A.-M. Abdel-Aziz, Hany E. A. Ahmed, Sivia Bua, Alessio Nocentini, Nawaf A. AlSaif, Ahmad J. Obaidullah, Mohamed M. Hefnawy, Claudiu T. Supuran
Published 2020-01-01

Synthesis and evaluation of a large library of nitroxoline derivatives as pancreatic cancer antiproliferative agents

by Serena Veschi, Simone Carradori, Laura De Lellis, Rosalba Florio, Davide Brocco, Daniela Secci, Paolo Guglielmi, Mattia Spano, Anatoly P. Sobolev, Alessandro Cama
Published 2020-01-01

Hydroxypropyl-β-cyclodextrin as an effective carrier of curcumin – piperine nutraceutical system with improved enzyme inhibition properties

by Anna Stasiłowicz, Ewa Tykarska, Kornelia Lewandowska, Maciej Kozak, Andrzej Miklaszewski, Joanna Kobus-Cisowska, Daria Szymanowska, Tomasz Plech, Jacek Jenczyk, Judyta Cielecka-Piontek
Published 2020-01-01

Mechanistic and biological characterisation of novel N5-substituted paullones targeting the biosynthesis of trypanothione in Leishmania

by Andrea Medeiros, Diego Benítez, Ricarda S. Korn, Vinicius C. Ferreira, Exequiel Barrera, Federico Carrión, Otto Pritsch, Sergio Pantano, Conrad Kunick, Camila I. de Oliveira, Oliver C. F. Orban, Marcelo A. Comini
Published 2020-01-01

Aspartic peptidase of Phialophora verrucosa as target of HIV peptidase inhibitors: blockage of its enzymatic activity and interference with fungal growth and macrophage interaction

by Marcela Q. Granato, Ingrid S. Sousa, Thabatta L. S. A. Rosa, Diego S. Gonçalves, Sergio H. Seabra, Daniela S. Alviano, Maria C. V. Pessolani, André L. S. Santos, Lucimar F. Kneipp
Published 2020-01-01

Discovery of 3,6-disubstituted pyridazines as a novel class of anticancer agents targeting cyclin-dependent kinase 2: synthesis, biological evaluation and in silico insights

by Ahmed Sabt, Wagdy M. Eldehna, Tarfah Al-Warhi, Ohoud J. Alotaibi, Mahmoud M. Elaasser, Howayda Suliman, Hatem A. Abdel-Aziz
Published 2020-01-01

Flavonoids with inhibitory activity against SARS-CoV-2 3CLpro

by Seri Jo, Suwon Kim, Dae Yong Kim, Mi-Sun Kim, Dong Hae Shin
Published 2020-01-01

Intra-site differential inhibition of multi-specific enzymes

by Mario Cappiello, Francesco Balestri, Roberta Moschini, Umberto Mura, Antonella Del-Corso
Published 2020-01-01

New horizons in drug discovery of lymphocyte-specific protein tyrosine kinase (Lck) inhibitors: a decade review (2011–2021) focussing on structure–activity relationship (SAR) and d...

by Ahmed Elkamhawy, Eslam M. H. Ali, Kyeong Lee
Published 2021-01-01

Aryl derivatives of 3H-1,2-benzoxathiepine 2,2-dioxide as carbonic anhydrase inhibitors

by Aleksandrs Pustenko, Alessio Nocentini, Anastasija Balašova, Ahmed Alafeefy, Mikhail Krasavin, Raivis Žalubovskis, Claudiu T. Supuran
Published 2020-01-01

Synthesis and structure-activity relationships of novel 5-(hydroxamic acid)methyl oxazolidinone derivatives as 5-lipoxygenase inhibitors

by Oludotun A. Phillips, Mira A. Bosso, Charles I. Ezeamuzie
Published 2020-01-01

Discovery of N-(1-(3-fluorobenzoyl)-1H-indol-5-yl)pyrazine-2-carboxamide: a novel, selective, and competitive indole-based lead inhibitor for human monoamine oxidase B

by Ahmed Elkamhawy, Sora Paik, Hyeon Jeong Kim, Jong-Hyun Park, Ashwini M. Londhe, Kyeong Lee, Ae Nim Pae, Ki Duk Park, Eun Joo Roh
Published 2020-01-01

Development of potent reversible selective inhibitors of butyrylcholinesterase as fluorescent probes

by Stane Pajk, Damijan Knez, Urban Košak, Maja Zorović, Xavier Brazzolotto, Nicolas Coquelle, Florian Nachon, Jacques-Philippe Colletier, Marko Živin, Jure Stojan, Stanislav Gobec
Published 2020-01-01

A class of carbonic anhydrase IX/XII – selective carboxylate inhibitors

by Rakia Abd Alhameed, Emanuela Berrino, Zainab Almarhoon, Ayman El-Faham, Claudiu T. Supuran
Published 2020-01-01

Design, synthesis, and anticonvulsant effects evaluation of nonimidazole histamine H3 receptor antagonists/inverse agonists containing triazole moiety

by Mingxia Song, Rui Yan, Yanhui Zhang, Dongfu Guo, Naiming Zhou, XianQing Deng
Published 2020-01-01

Design, synthesis and in vitro antiproliferative activity of new thiazolidinedione-1,3,4-oxadiazole hybrids as thymidylate synthase inhibitors

by Zohor Mohammad Mahdi Alzhrani, Mohammad Mahboob Alam, Thikryat Neamatallah, Syed Nazreen
Published 2020-01-01

A structure-based approach towards the identification of novel antichagasic compounds: Trypanosoma cruzi carbonic anhydrase inhibitors

by Manuel A. Llanos, María L. Sbaraglini, María L. Villalba, María D. Ruiz, Carolina Carrillo, Catalina Alba Soto, Alan Talevi, Andrea Angeli, Seppo Parkkila, Claudiu T. Supuran, Luciana Gavernet
Published 2020-01-01

Further validation of strecker-type α-aminonitriles as a new class of potent human carbonic anhydrase II inhibitors: hit expansion within the public domain using differential scann...

by Mikhail Krasavin, Stanislav Kalinin, Sergey Zozulya, Anastasia Griniukova, Petro Borysko, Andrea Angeli, Claudiu T. Supuran
Published 2020-01-01

Bioorganometallic derivatives of 4-hydrazino-benzenesulphonamide as carbonic anhydrase inhibitors: synthesis, characterisation and biological evaluation

by Jeremie Brichet, Rodrigo Arancibia, Emanuela Berrino, Claudiu T. Supuran
Published 2020-01-01

7-Acylamino-3H-1,2-benzoxathiepine 2,2-dioxides as new isoform-selective carbonic anhydrase IX and XII inhibitors

by Aleksandrs Pustenko, Alessio Nocentini, Anastasija Balašova, Mikhail Krasavin, Raivis Žalubovskis, Claudiu T. Supuran
Published 2020-01-01