Medicinal Chemistry

Design, Synthesis and Biological Evaluation of Anti-tuberculosis Agents based on Bedaquiline Structure

Volume: 16   Issue: 5
Pp: 703-714
Chengjun Wu, Jinghan Luo, Mengtong Wu, Fanzhen Meng, Zhiqiang Cai, Yu Chen* and Tiemin Sun*
DOI: 10.2174/1573406415666190613094433

Highly Potent and Selective Ectonucleoside Triphosphate Diphosphohydrolase (ENTPDase1, 2, 3 and 8) Inhibitors Having 2-substituted-7- trifluoromethyl-thiadiazolopyrimidones Scaffold

Volume: 16   Issue: 5
Pp: 689-702
Saira Afzal, Sumera Zaib, Behzad Jafari, Peter Langer, Joanna Lecka, Jean Sévigny and Jamshed Iqbal*
DOI: 10.2174/1573406415666190614095821

iATP: A Sequence Based Method for Identifying Anti-tubercular Peptides

Volume: 16   Issue: 5
Pp: 620-625
Wei Chen*, Pengmian Feng and Fulei Nie
DOI: 10.2174/1573406415666191002152441

Prediction and Analysis of Hub Genes in Renal Cell Carcinoma based on CFS Gene Selection Method Combined with Adaboost Algorithm

Volume: 16   Issue: 5
Pp: 654-663
Yina Wang, Benrong Zheng, Manbin Xu, Shaoping Cai, Jeong Younseo, Chi Zhang* and Boxiong Jiang*
DOI: 10.2174/1573406415666191004100744

Recent Advancement in Predicting Subcellular Localization of Mycobacterial Protein with Machine Learning Methods

Volume: 16   Issue: 5
Pp: 605-619
Shi-Hao Li, Zheng-Xing Guan, Dan Zhang, Zi-Mei Zhang, Jian Huang, Wuritu Yang* and Hao Lin*
DOI: 10.2174/1573406415666191004101913

The Assessment of Interleukin-18 on the Risk of Coronary Heart Disease

Volume: 16   Issue: 5
Pp: 626-634
Weiju Sun, Ying Han, Shuo Yang, He Zhuang, Jingwen Zhang, Liang Cheng* and Lu Fu*
DOI: 10.2174/1573406415666191004115128

Application of Machine Learning Methods in Predicting Nuclear Receptors and their Families

Volume: 16   Issue: 5
Pp: 594-604
Zi-Mei Zhang, Zheng-Xing Guan, Fang Wang, Dan Zhang and Hui Ding*
DOI: 10.2174/1573406415666191004125551

Computational Analysis and Synthesis of Syringic Acid Derivatives as Xanthine Oxidase Inhibitors

Volume: 16   Issue: 5
Pp: 643-653
Neelam Malik, Anurag Khatkar* and Priyanka Dhiman
DOI: 10.2174/1573406415666191004134346

Integrative Analysis of Whole-genome Expression Profiling and Regulatory Network Identifies Novel Biomarkers for Insulin Resistance in Leptin Receptor-deficient Mice

Volume: 16   Issue: 5
Pp: 635-642
Yuchi Zhang, Xinyu Wu, Cong Zhao, Kai Li, Yi Zheng, Jing Zhao and Pengling Ge*
DOI: 10.2174/1573406415666191004135450

Dairy Safety Prediction Based on Machine Learning Combined with Chemicals

Volume: 16   Issue: 5
Pp: 664-676
Jiahui Chen, Guangya Zhou, Jiayang Xie, Minjia Wang, Yanting Ding, Shuxian Chen, Sijing Xia, Xiaojun Deng*, Qin Chen* and Bing Niu*
DOI: 10.2174/1573406415666191004142810

Preliminary Anti-Coxsackie Activity of Novel 1-[4-(5,6-dimethyl(H)- 1H(2H)-benzotriazol-1(2)-yl)phenyl]-3-alkyl(aryl)ureas

Volume: 16   Issue: 5
Pp: 677-688
Sandra Piras, Paola Corona, Roberta Ibba, Federico Riu, Gabriele Murineddu, Giuseppina Sanna, Silvia Madeddu, Ilenia Delogu, Roberta Loddo* and Antonio Carta*
DOI: 10.2174/1573406416666191226142744

Computational Analysis in Medicinal Chemistry. The Case of Pharmacogenomics and Pharmacoproteomics promotion: free to download

Volume: 16   Issue: 5
Pp: 593-593
Hao Lin
DOI: 10.2174/157340641605200608102355

Antiglycation Activity of Triazole Schiff’s Bases Against Fructosemediated Glycation: In Vitro and In Silico Study

Volume: 16   Issue: 4
Pp: 575-591
Muniza Shaikh, Salman Siddiqui, Humaira Zafar, Uzma Naqeeb, Fakiha Subzwari, Rehan Imad, Khalid M. Khan and Muhammad I. Choudhary*
DOI: 10.2174/1573406415666190212105718

Novel Coupled Molecules from Active Structural Motifs of Synthetic and Natural Origin as Immunosuppressants

Volume: 16   Issue: 4
Pp: 544-554
Richa Minhas, Gulshan Bansal and Yogita Bansal*
DOI: 10.2174/1573406415666190409111459

Recent Advances in Therapeutic Applications of Bisbenzimidazoles

Volume: 16   Issue: 4
Pp: 454-486
Smita Verma , Vishnuvardh Ravichandiran, Nihar Ranjan and Swaran J.S. Flora*
DOI: 10.2174/1573406415666190416120801

Design and Biological Evaluation of Novel Imidazolyl Flavonoids as Potent and Selective Protein Tyrosine Phosphatase Inhibitors

Volume: 16   Issue: 4
Pp: 563-574
Rong Y. Han, Yu Ge, Ling Zhang* and Qing M. Wang
DOI: 10.2174/1573406415666190430125547

Matrine-Family Alkaloids: Versatile Precursors for Bioactive Modifications

Volume: 16   Issue: 4
Pp: 431-453
Xiao-hua Cai*, Hong-yan Zhang and Bing Xie*
DOI: 10.2174/1573406415666190507121744

New Serotoninergic Ligands Containing Indolic and Methyl Indolic Nuclei: Synthesis and In Vitro Pharmacological Evaluation

Volume: 16   Issue: 4
Pp: 517-530
Elisa Magli, Beatrice Severino*, Angela Corvino, Elisa Perissutti, Francesco Frecentese, Irene Saccone, Flavia Giordano, Marián Castro, José Brea, María I. Loza, Vincenzo Santagada, Giuseppe Caliendo and Ferdinando Fiorino
DOI: 10.2174/1573406415666190613153220

Synthesis of Novel 8-Hydroxyquinoline Derivatives through Mannich Reaction and their Biological Evaluation as Potential Immunomodulatory Agents

Volume: 16   Issue: 4
Pp: 531-543
Shaheen Faizi*, Tahira Sarfaraz, Saima Sumbul, Almas Jabeen, Sobia A. Halim, Mohammad A. Mesaik and Zaheer Ul-Haq*
DOI: 10.2174/1573406415666190626121650

Synthesis and Antitrypanosomal Profile of Novel Hydrazonoyl Derivatives

Volume: 16   Issue: 4
Pp: 487-494
Natália N. Santiago, Giulianna P. de Alcântara, Juliana S. da Costa, Samir A. Carvalho, Juliana M.C. Barbosa, Kelly Salomão, Solange L. de Castro, Henrique M.G. Pereira and Edson F. da Silva*
DOI: 10.2174/1573406415666190712115237

Synthesis of N-Substituted Benzamide Derivatives and their Evaluation as Antitumor Agents

Volume: 16   Issue: 4
Pp: 555-562
Taiping Chen, Hongwu Jiang, Jianjun Zhou, Zicheng Li*, Wencai Huang, Youfu Luo and Yinglan Zhao
DOI: 10.2174/1573406415666190712120611

Novel Furan Coupled Quinoline Diamide Hybrid Scaffolds as Potent Antitubercular Agents: Design, Synthesis and Molecular Modelling

Volume: 16   Issue: 4
Pp: 507-516
Anantacharya Rajpurohit, Nayak D. Satyanarayan*, Lokesh Pathak, Siva Ayyanar, Chidambaram R. Rishinaradamangalam and Praveen Shoorapani
DOI: 10.2174/1573406415666190904124630

Synthesis of Silver Nanoparticles using Euphorbia wallichii Extract and Assessment of their Bio-functionalities

Volume: 16   Issue: 4
Pp: 495-506
Abdul-Rehman Phull*, Attarad Ali, Akhtar Ali, Sanaullah Abbasi, Muhammad Zia, Muhammad H. Khaskheli, Ihsan ul Haq and Mohammad A. Kamal*
DOI: 10.2174/1573406415666191111143213

Design, Synthesis, and Anti-bacterial Activity of Novel Deoxycholic Acid- Amino Alcohol Conjugates

Volume: 16   Issue: 3
Pp: 385-391
Satyendra Mishra* and Sejal Patel
DOI: 10.2174/1573406415666190206231002

Design, Synthesis, and Biological Evaluation of Novel C5-Modified Pyrimidine Ribofuranonucleosides as Potential Antitumor or/and Antiviral Agents

Volume: 16   Issue: 3
Pp: 368-384
Nikolaos Kollatos, Christos Mitsos, Stella Manta, Niki Tzioumaki, Christos Giannakas, Tania Alexouli, Aggeliki Panagiotopoulou, Dominique Schols, Graciela Andrei and Dimitri Komiotis*
DOI: 10.2174/1573406415666190225112950

First Example of Antiparasitic Activity Influenced by Thermochromism: Leishmanicidal Evaluation of 5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine Metal Complexes

Volume: 16   Issue: 3
Pp: 422-430
José M. Méndez-Arriaga*, Itziar Oyarzabal, Álvaro Martín-Montes, Judith García-Rodríguez, Miguel Quirós and Manuel Sánchez-Moreno
DOI: 10.2174/1573406415666190401120607

Design and Synthesis of New Sulfonamides-Based Flt3 Inhibitors

Volume: 16   Issue: 3
Pp: 403-412
Reem F. Abutayeh, Jehad Almaliti and Mutasem O. Taha*
DOI: 10.2174/1573406415666190401144053

Hybrids of Coumarin Derivatives as Potent and Multifunctional Bioactive Agents: A Review

Volume: 16   Issue: 3
Pp: 272-306
Ioannis Fotopoulos and Dimitra Hadjipavlou-Litina*
DOI: 10.2174/1573406415666190416121448

Molecular Docking and Dynamics Simulation Analysis of Thymoquinone and Thymol Compounds from Nigella sativa L. that Inhibits P38 Protein: Probable Remedies for Hepatocellular Carcinoma

Volume: 16   Issue: 3
Pp: 350-357
Heena Tabassum and Iffat Z. Ahmad*
DOI: 10.2174/1573406415666190416165732

Design, Synthesis and In Vitro Anti-Cancer Evaluation of Novel Derivatives of 2-(2-Methyl-1,5-diaryl-1H-pyrrol-3-yl)-2-oxo-N-(pyridin-3- yl)acetamide

Volume: 16   Issue: 3
Pp: 340-349
Ebrahim S. Moghadam, Farhad Saravani, Ernest Hamel, Zahra Shahsavari, Mohsen Alipour, Saman Hosseinkhani, Seyednasser Ostad and Mohsen Amini*
DOI: 10.2174/1573406415666190425153717

Anti-Mycobacterial Peroxides: A New Class of Agents for Development Against Tuberculosis

Volume: 16   Issue: 3
Pp: 392-402
Christiaan W. van der Westhuyzen, Richard K. Haynes, Jenny-Lee Panayides, Ian Wiid and Christopher J. Parkinson*
DOI: 10.2174/1573406415666190430143535

Design, Synthesis and Evaluation of 8-Thiosubstituted 1,3,7- Trimethylxanthine Hydrazones with In-vitro Neuroprotective and MAO-B Inhibitory Activities

Volume: 16   Issue: 3
Pp: 326-339
Javor Mitkov, Alexandra Kasabova-Angelova, Magdalena Kondeva-Burdina, Virginia Tzankova, Diana Tzankova, Maya Georgieva and Alexander Zlatkov*
DOI: 10.2174/1573406415666190531121927

Cyclic Tripeptide-based Potent and Selective Human SIRT5 Inhibitors

Volume: 16   Issue: 3
Pp: 358-367
Yanhong Jiang and Weiping Zheng*
DOI: 10.2174/1573406415666190603101937

Inhibitors of Cyclin-Dependent Kinase 1/2 for Anticancer Treatment

Volume: 16   Issue: 3
Pp: 307-325
Jiajia Mou*, Danghui Chen and Yanru Deng
DOI: 10.2174/1573406415666190626113900

Synthesis and Assessment of 3-Substituted Phenazines as Novel Antichlamydial Agents

Volume: 16   Issue: 3
Pp: 413-421
Xiaofeng Bao, Ziyi Liu, Min Ni, Chao Xia, Shunxin Xu, Shengju Yang* and Yu Zhao*
DOI: 10.2174/1573406415666190708145639

The Coronavirus Epidemic promotion: free to download

Volume: 16   Issue: 3
Pp: 271-271
A. Hilgeroth
DOI: 10.2174/157340641603200226092100

Target Based Virtual Screening of New Leads Inhibitor against Bacterial Cell Division Protein FtsZ for the Discovery of Antibacterial Agents

Volume: 16   Issue: 2
Pp: 169-175
Ratish C. Mishra, Rosy Kumari, Shivani Yadav and Jaya P. Yadav*
DOI: 10.2174/1573406415666190206233448

Design and Synthesis of New Substituted Pyrazolopyridines with Potent Antiproliferative Activity

Volume: 16   Issue: 2
Pp: 176-191
Vassiliki Giannouli, Nikolaos Lougiakis, Ioannis K. Kostakis, Nicole Pouli*, Panagiotis Marakos, Alexios-Leandros Skaltsounis, David A. Horne, Sangkil Nam, Katerina Gioti and Roxane Tenta
DOI: 10.2174/1573406415666190222130225

Bicycloheptylamine-Doxorubicin Conjugate: Synthesis and Anticancer Activities in σ2 Receptor-Expressing Cell Lines

Volume: 16   Issue: 2
Pp: 192-201
Mohammed A. Alamri, Zeynep Ates-Alagoz and Adeboye Adejare*
DOI: 10.2174/1573406415666190301145203

Synthesis, Biological Evaluation and Molecular Dynamics Simulation Studies of Novel Diphenyl Ethers

Volume: 16   Issue: 2
Pp: 256-270
Amol B. Khade, Sidhartha S. Kar, Cinu T. Alummoottil, Ashutosh Tiwari, Mradul Tiwari, Vandana K. Eshwara, Pritesh Bhat, Varadaraj B. Giliyar and Gurupur G. Shenoy*
DOI: 10.2174/1573406415666190306152907

Synthesis of β-Ketosulfone Derivatives As New Non-Cytotoxic Urease Inhibitors In Vitro

Volume: 16   Issue: 2
Pp: 244-255
Sarosh Iqbal*, Ajmal Khan, Rashid Nazir, Shumaila Kiran, Shahnaz Perveen, Khalid M. Khan* and Muhammad I. Choudhary*
DOI: 10.2174/1573406415666190415163309

Three Dimensional Quantitative Structure Activity Relationship and Pharmacophore Modeling of Tacrine Derivatives as Acetylcholinesterase Inhibitors in Alzheimer's Treatment

Volume: 16   Issue: 2
Pp: 155-168
Fatemeh Ansari, Jahan B. Ghasemi* and Ali Niazi
DOI: 10.2174/1573406415666190513100646

Novel p-Functionalized Chromen-4-on-3-yl Chalcones Bearing Astonishing Boronic Acid Moiety as MDM2 Inhibitor: Synthesis, Cytotoxic Evaluation and Simulation Studies

Volume: 16   Issue: 2
Pp: 212-228
Richa K. Bhatia*, Lakhwinder Singh, Ruchika Garg, Maninder Kaur, Manmohan Yadav, Jitender Madan, Satyavathi Kancherla, Raghuvir R.S. Pissurlenkar and Evans C. Coutinho
DOI: 10.2174/1573406415666190531123751

Styrylquinoline – A Versatile Scaffold in Medicinal Chemistry

Volume: 16   Issue: 2
Pp: 141-154
Robert Musiol*
DOI: 10.2174/1573406415666190603103012

Design, Synthesis, and Evaluation of Isoquinoline Ureas as TRPV1 Antagonists

Volume: 16   Issue: 2
Pp: 202-211
Nehaben A. Gujarati, Bradley J. Undem and Vijaya L. Korlipara*
DOI: 10.2174/1573406415666190626130453

4-Aminocoumarin based Aroylthioureas as Potential Jack Bean Urease Inhibitors; Synthesis, Enzyme Inhibitory Kinetics and Docking Studies

Volume: 16   Issue: 2
Pp: 229-243
Tanzeela A. Fattah, Aamer Saeed*, Zaman Ashraf*, Qamar Abbas, Pervaiz A. Channar, Fayaz A. Larik and Mubashir Hassan
DOI: 10.2174/1573406415666190715164834

Design and Synthesis of Novel Sulfonamide-Derived Triazoles and Bioactivity Exploration

Volume: 16   Issue: 1
Pp: 104-118
Shi-Chao He, Hui-Zhen Zhang*, Hai-Juan Zhang, Qing Sun and Cheng-He Zhou*
DOI: 10.2174/1573406414666181106124852

The Substantial Improvement of Amphotericin B Selective Toxicity Upon Modification of Mycosamine with Bulky Substituents

Volume: 16   Issue: 1
Pp: 128-139
Edward Borowski, Natalia Salewska, Joanna Boros-Majewska, Marcin Serocki, Izabela Chabowska, Maria J. Milewska, Dominik Ziętkowski and Sławomir Milewski*
DOI: 10.2174/1573406415666181203114629

Evaluation of Cytotoxic Potentials of Some Isoindole-1, 3-Dione Derivatives on HeLa, C6 and A549 Cancer Cell Lines

Volume: 16   Issue: 1
Pp: 69-77
Ayse Tan, Ayse Sahin Yaglioglu, Nurhan Horasan Kishali*, Ertan Sahin and Yunus Kara*
DOI: 10.2174/1573406415666181206115638

Benzoylthioureas: Design, Synthesis and Antimycobacterial Evaluation

Volume: 16   Issue: 1
Pp: 93-103
Tiago O. Brito, Lethícia O. Abreu, Karen M. Gomes, Maria C.S. Lourenço, Patricia M.L. Pereira, Sueli F. Yamada-Ogatta, Ângelo de Fátima, Cesar A. Tisher, Fernando Macedo Jr and Marcelle L.F. Bispo*
DOI: 10.2174/1573406415666181208110753

Synthesis, Anticancer Evaluation and Synergistic Effects with cisplatin of Novel Palladium Complexes: DNA, BSA Interactions and Molecular Docking Study

Volume: 16   Issue: 1
Pp: 78-92
Nenad Joksimović, Nenad Janković, Jelena Petronijević, Dejan Baskić, Suzana Popovic, Danijela Todorović, Milan Zarić, Olivera Klisurić, Milan Vraneš, Aleksandar Tot and Zorica Bugarčić*
DOI: 10.2174/1573406415666190128095732

Structure-activity Relationship Study on Therapeutically Relevant EGFR Double Mutant Inhibitors

Volume: 16   Issue: 1
Pp: 52-62
Shehnaz Fatima and Subhash M. Agarwal*
DOI: 10.2174/1573406415666190206204853

The Effects of Trifluoromethylated Derivatives on Prostaglandin E₂ and Thromboxane A₂ Production in Human Leukemic U937 Macrophages

Volume: 16   Issue: 1
Pp: 63-68
Ivana Beara*, Tatjana Majkić, Stefania Fioravanti, Laura Trulli, Neda Mimica-Dukić, Lucio Pellacani and Luciano Saso
DOI: 10.2174/1573406415666190208150253

Synthesis and Biological Evaluation of 5-benzyl-3-pyridyl-1H-1,2,4-triazole Derivatives as Xanthine Oxidase Inhibitors

Volume: 16   Issue: 1
Pp: 119-127
Song-Ye Li , Ting-Jian Zhang , Qing-Xia Wu, Kamara M. Olounfeh, Yi Zhang and Fan-Hao Meng*
DOI: 10.2174/1573406415666190409112209

Synthesis of New Cyclic Imides Derived From Safrole, Structure- and Ligand-based Approaches to Evaluate Potential New Multitarget Agents Against Species of Leishmania

Volume: 16   Issue: 1
Pp: 39-51
José A. de Sousa Luis*, Normando A. da Silva Costa, Cristiane C.S. Luis, Bruno F. Lira, Petrônio F. Athayde-Filho, Tatjana K. de Souza Lima, Juliana da Câmara Rocha, Luciana Scotti and Marcus T. Scotti*
DOI: 10.2174/1573406415666190430144950

Thiazole Compounds as Antiviral Agents: An Update

Volume: 16   Issue: 1
Pp: 4-23
Inder P. Singh*, Shiv Gupta and Sanjay Kumar
DOI: 10.2174/1573406415666190614101253