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Letters in Drug Design & Discovery

Volume 16, 12 Issues, 2019
ISSN: 1875-628X (Online)
ISSN: 1570-1808 (Print)
This journal supports open access

Aims & Scope

Letters in Drug Design & Discovery publishes letters, mini-reviews, highlights and guest edited thematic issues in all areas of rational drug design and discovery including medicinal chemistry, in-silico drug design, combinatorial chemistry, high-throughput screening, drug targets, and structure-activity relationships. The emphasis is on publishing quality papers very rapidly by taking full advantage of latest Internet technology for both submission and review of manuscripts. The online journal is an essential reading to all pharmaceutical scientists involved in research in drug design and discovery.

Letters in Drug Design & Discovery

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Volume 16

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Number 3



Biography   Open Access



Research Article   Open Access

A Study on the Synthesis of Risedronic Acid: The Role of an Ionic Liquid Additive

, 16(3): 238 - 244

Dávid Illés Nagy, Alajos Grün, Júlia Sinkovicz, Sándor Garadnay, István Greiner and György Keglevich*


DOI: 10.2174/1570180815666180626122630


Research Article



Research Article

Green Synthesis, Characterization, DPPH and Ferrous Ion-chelating (FIC) Activity of Tetrakis-Schiff’s Bases of Terephthalaldehyde

, 16(3): 249 - 255

Momin Khan*, Umar Ali, Anis Ur Rahman, Muhammad Ibrahim, Abdul Hameed, Muhammad Asif, Zahid Hussain, Kanwal, Khalid Mohammed Khan, Shahnaz Perveen and Munir ur Rehman


DOI: 10.2174/1570180815666180531101404


Research Article

Coumarinyl Aryl/Alkyl Sulfonates with Dual Potential: Alkaline Phosphatase and ROS Inhibitory Activities: In-Silico Molecular Modeling and ADME Evaluation

, 16(3): 256 - 272

Uzma Salar, Khalid Mohammed Khan*, Syeda Abida Ejaz, Abdul Hameed, Mariya al-Rashida, Shahnaz Perveen, Muhammad Nawaz Tahir, Jamshed Iqbal* and Muhammad Taha


DOI: 10.2174/1570180815666180327125738


Research Article



Research Article



Research Article

Assessing the Antimalarial Potentials of Phytochemicals: Virtual Screening, Molecular Dynamics and In-Vitro Investigations

, 16(3): 291 - 300

Saumya K. Patel, Mohd Athar, Prakash C. Jha*, Vijay M. Khedkar, Yogesh Jasrai, Himanshu A. Pandya, Linz-buoy George, Hyacinth Highland and Supriya Sharma


DOI: 10.2174/1570180815666180604085626


Letters in Drug Design & Discovery, Volume 16 (2019) - Number 4


This issue is in progress but contains articles that are final and fully citable.

Articles Ahead of Print


Benzo[d]imidazol-5-yl)-5-(substituted)-1, 3, 4-Oxadiazoles: Synthesis, Anticancer, Antimicrobial and In-silico Studies


Naveen Kumar, Swamy Sreenivasa*, Bhuvanesh Sukhlal Kulal, Vasantha Kumar, Bantwal Shivarama Holla, Vinitha Ramanath Pai, Nadigar Revansiddappa Mohand and Shivaraj Govindaiah


View Abstract


Synthesis and SAR Study of Simple Aryl Oximes and Nitrofuranyl Derivatives with Potent Activity Against Mycobacterium Tuberculosis


Cristiane França da Costa, Marcus Vinicius Nora de Souza*, Maria Cristina da Silva Lourenço, Elaine Soares Coimbra, Guilherme da Silva Lourenço Carvalho, James Wardell, Stephane Lima Calixto and Juliana da Trindade Granato


View Abstract



Synthesis and Antimicrobial Activity of Thiohydantoins Obtained from L-Amino Acids


Priscila Goes Camargo de Carvalho, Jhonatan Macedo Ribeiro, Renata Perugini Biasi Garbin, Gerson Nakazato, Sueli F. Yamada- Ogatta, Ângelo de Fátima, Marcelle L. F. Bispo and Fernando Macedo Jr*


View Abstract



The Structure of MT189-Tubulin Complex Provides Insights into Drug Design


Zhongping Li, Lingling Ma, Chengyong Wu, Tao Meng, Lanping Ma, Wenyue Zheng, Yamei Yu*, Qiang Chen*, Jinliang Yang and Jingkang Shen


View Abstract


The Development of Tyrosyl-DNA Phosphodyesterase 1 (TDP1) Inhibitors Based on the Amines Combining Aromatic/Heteroaromatic and Monoterpenoid Moieties


Evgenii Mozhaitsev, Evgenii Suslov*, Yuliya Demidova, Dina Korchagina, Konstantin Volcho, Alexandra Zakharenko, Inna Vasil`eva, Maksim Kupryushkin, Arina Chepanova, Daniel Moscoh Ayine-Tora, Jóhannes Reynisson, Nariman Salakhutdinov and Olga Lavrik


View Abstract


Synthesis, Formulation and Analytical Method Validation of Rutin Derivative


Murad Abualhasan*, Mohyeddin Assali, Nidal Jaradat and Tala Sarhan


View Abstract


Synthesis and In vitro Biological Activity Evaluation of Novel Imidazo [2,1-B][1,3,4] Thiadiazole as Anti-alzheimer Agents


Sara Azimi, Omidreza Firuzi, Aida Iraji, Afsaneh Zonouzi , Mahsima Khoshneviszadeh, Mohammad Mahdavi* and Najmeh Edraki*


View Abstract


Abstracts Ahead of Print




Biology-Oriented Drug Synthesis (BIODS), Structural Characterization and Bioactivities of Novel Albendazole Derivatives


Momin Khan*, Shahid Khan, Uzma Salar, Khalid Mohammed Khan, Gauhar Rehman, Naeem Gul and Iltaf Khan


View Abstract


Effects of acute and chronic treatment of novel psychotropic drug, 8-(trifluoromethyl)-1,2,3,4,5-benzopentathiepin-6-amine hydrochloride (TC-2153), on behavior of zebrafish (Danio rerio): a comparison with fluoxetine


Alexander V. Kulikov, Nadezhda A. Sinyakova, Elizabeth A. Kulikova, Tatyana M. Khomenko, Nariman F. Salakhutdinov, Victor A. Kulikov and Konstantin P. Volcho*


View Abstract



Design, Synthesis and Biological Evaluation of Camptothecin Conjugated with NSAIDs as Novel Dual-action Antitumor Agents


Xingchen Cai, Weiwei Huang, Yi Huang, Lihua Xia, Miao Liu, Mengke Wang, Wenchao Wang and Qingyong Li*


View Abstract





Editor's Choice



Synthesis and Antichlamydial Activity of Novel Phenazines

, 2019; 16(2): 174 - 181

Xiaofeng Bao, Xiaowei Yu, Chao Xia, Ningjing Yang, Shengju Yang* and Yu Zhao*


DOI: 10.2174/1570180815666180518112952



A New Class of Pure Estrogen Alpha Receptor Antagonists; Design, Synthesis and in-vitro Screening

, 2019; 16(1): 66 - 81

Akbar John Jameera Begam, Katike Ahamed Basheer, Selvaraj Jubie*, Srikanth Jupudi, Mohammed Afzal Azam and Palanisamy Dhanabal


DOI: 10.2174/1570180815666180327124634



Preparation and Characterization of GLUT1-mediated Novel Brain Targeting Magnetic Nanoparticles

, 2018; 15(12): 1308 - 1313

Li Zhang, Yi Zhao, Qiming Yue, Qiuyi Fu, Li Hai, Li Guo, Qiantao Wang* and Yong Wu*


DOI: 10.2174/1570180815666180322113934



Synthesis and Mosquiticidal Activity of Novel Hydrazone Containing Pyrimidine Derivatives against Aedes aegypti

, 2018; 15(9): 951 - 956

Zhong-Hua Shen, Zhao-Hui Sun, James J. Becnel, Alden Estep, David E. Wedge*, Cheng-Xia Tan, Jian-Quan Weng, Liang Han and Xing-Hai Liu*


DOI: 10.2174/1570180815666180102141640



Inhibitory Effects of 1,4-disubstituted Thiosemicarbazide Derivatives on Streptococcus mutans and Streptococcus sanguinis Mono-species Biofilms

, 2018; 15(8): 843 - 850

Malgorzata Miazga-Karska, Maciej Wos, Agnieszka A. Kaczor, Anna Pachuta-Stec, Grazyna Ginalska and Monika Pitucha*


DOI: 10.2174/1570180814666171012164241



Enhancement Antimicrobial Activity of Clarithromycin by Amine Functionalized Mesoporous Silica Nanoparticles as Drug Delivery System

, 2018; 15(7): 787 - 795

Pegah Khosravian, Mehdi Khoobi, Mehdi Shafiee Ardestani, Mohammad Porgham Daryasari, Malihe Hassanzadeh, Payam Ghasemi-Dehkordi, Massoud Amanlou and Hamid Akbari Javar*


DOI: 10.2174/1570180815666180117155818



Synthesis and Mosquitocidal Activity of a Series of Hydrazone Derivatives against Aedes aegypti

, 2018; 15(6): 671 - 677

Mehlika Dilek Altintop*, Nurhayat Tabanca, James J. Becnel, Jeffrey R. Bloomquist, Zafer Asim Kaplancikli and Ahmet Ozdemir


DOI: 10.2174/1570180814666171002155548




Open Access Articles

A Study on the Synthesis of Risedronic Acid: The Role of an Ionic Liquid Additive

, 2019; 16(3): 238 - 244

Dávid Illés Nagy, Alajos Grün, Júlia Sinkovicz, Sándor Garadnay, István Greiner and György Keglevich*




Synthesis and Biological Evaluation of Some Novel Thiophene-bearing Quinazoline Derivatives as EGFR Inhibitors

, 2019; 16(2): 102 - 110

Min Zou, Bo Jin, Yanrong Liu, Huiping Chen, Zhuangli Zhang, Changzheng Zhang, Zhihong Zhao and Liyun Zheng*




Efficient Synthesis of Ibandronate in the Presence of an Ionic Liquid

, 2018; 15(7): 713 - 720

David Illes Nagy, Alajos Grun, Oliver Pavela, Sandor Garadnay, Istvan Greiner and Gyorgy Keglevich*




L-carnitine Supplementation Improves Self-rating Depression Scale Scores in Uremic Male Patients Undergoing Hemodialysis

, 2017; 14(6): 737 - 742

Kyoko Tashiro, Yusuke Kaida, Sho-ichi Yamagishi, Hideharu Tanaka, Miyuki Yokoro, Junko Yano, Kazuko Sakai, Yuka Kurokawa, Kensei Taguchi, Yosuke Nakayama, Takahiro Inokuchi and Kei Fukami*




The Synthesis of (Iodobenzyl)oxybenzaldehydes, Useful Intermediates for Biologically Active Targets

, 2017; 14(2): 233 - 239

Hedvig Bölcskei, Andrea Német-Hanzelik, István Greiner, Zsófia Dubrovay, Viktor Háda and György Keglevich




In Vitro and In Vivo Investigations into the Carbene Gold Chloride and Thioglucoside Anticancer Drug Candidates NHC-AuCl and NHC-AuSR

, 2017; 14(2): 125 - 134

Wolfgang Walther, Oyinlola Dada, Cillian O’Beirne, Ingo Ott, Goar Sánchez-Sanz, Claudia Schmidt, Carsta Werner, Xiangming Zhu and Matthias Tacke




Efficient Synthesis of Pamidronic Acid Using an Ionic Liquid Additive

, 2016; 13(6): 475 - 478

Alajos Grun, Dávid Illés Nagy, Sándor Garadnay, István Greiner and Gyorgy Keglevich






4-Substituted-2-Methoxyphenol: Suitable Building Block to Prepare New Bioactive Natural-like Hydroxylated Biphenyls

, 2015; 12(2): 131 - 139

Maria Antonietta Dettori, Davide Fabbri, Marina Pisano, Carla Rozzo, Giuseppe Palmieri, Alessandro Dessi, Roberto Dallocchio and Giovanna Delogu




Design and Synthesis of New Dual Binding Site Cholinesterase Inhibitors: in vitro Inhibition Studies with in silico Docking

, 2014; 11(3): 331 - 338

Muhammad Yar, Marek Bajda, Rana Atif Mehmood, Lala Rukh Sidra, Nisar Ullah, Lubna Shahzadi, Muhammad Ashraf, Tayaba Ismail, Sohail Anjum Shahzad, Zulfiqar Ali Khan, Syed Ali Raza Naqvi and Nasir Mahmood




Optimized Synthesis of Etidronate

, 2013; 10(8): 733 - 737

Rita Kovacs, David Illes Nagy, Alajos Grün, Gyorgy Tibor Balogh, Sandor Garadnay, Istvan Greiner and Gyorgy Keglevich






Selective Androgen Receptor Modulators Antagonize Apolipoprotein E4-Induced Cognitive Impairments

, 2008; 5(4): 271 - 276

Summer Acevedo, Luis Gardell, Stefania Risso Bradley, Fabrice Piu and Jacob Raber





Most Cited Articles

Microwave Assisted Synthesis and Antifungal Activity of Some Novel Thioethers Containing 1,2,4-triazolo[4,3-a] pyridine Moiety

, 2016; 13(6): 521-525.

Zhi-Wen Zhai, Yan-Xia Shi, Ming-Yan Yang, Wen Zhao, Zhao-Hui Sun, Jian-Quan Weng, Cheng-Xia Tan, Xing-Hai Liu, Bao-Ju Li and Yong-Gang Zhang


DOI: 10.2174/157018081306160618181757








Synthesis of Novel C3-Linked β-Carboline-Pyridine Derivatives Employing Khronke Reaction: DNA-binding Ability and Molecular Modeling Studies

, 2016; 13(4): 335-342.

Nagula Shankaraiah, Pankaj Sharma, Srinivas Pedapati, Shalini Nekkanti, Vunnam Srinivasulu, Niggula Praveen Kumar and Ahmed Kamal


DOI: 10.2174/157018081304160303180050



Prediction of Caco-2 Cell Permeability Using Bilinear Indices and Multiple Linear Regression

, 2016; 13(2): 161-169.

Huong Le-Thi-Thu, Yudith Canizares-Carmenate, Yovani Marrero-Ponce, Francisco Torrens and Juan A. Castillo-Garit


DOI: 10.2174/1570180812666150630183511


Synthesis and Antimicrobial Evaluation of Amphipathic Peptide Models

, 2016; 13(7): 715-724.

Marianna Sakka, Alexandra Balliou, Asimina Marianou, Dimitris Krikorian, Margarita Tsirogianni, Artemis Tsiligianni, Katerina Vartzeli, Anna-Irini Koukkou, Maria Sakarellos-Daitsiotis and Eugenia Panou- Pomonis


DOI: 10.2174/1570180813666160616122410


Efficient Synthesis of Pamidronic Acid Using an Ionic Liquid Additive

, 2016; 13(6): 475-478.

Alajos Grun, Dávid Illés Nagy, Sándor Garadnay, István Greiner and Gyorgy Keglevich


DOI: 10.2174/1570180812666151022221805


Design, Synthesis and Mode of Action of Some New 2-(4'-aminophenyl) benzothiazole Derivatives as Potent Antimicrobial Agents

, 2016; 13(5): 429-437.

Meenakshi Singh, Sudhir Kumar Singh, Mayank Gangwar, Satheeshkumar Sellamuthu, Gopal Nath and Sushil K. Singh


DOI: 10.2174/1570180812666150821003220



Design and Synthesis of Novel Spiro-Piperidinyl Pyrazolone Derivatives and Their Potential Antiviral Activity

, 2016; 13(2): 149-160.

Rajagopalan Srinivasan, Badiadka Narayana, Balladka Kunhanna Sarojini, Veerakyathappa Bhanuprakash, Chenna Govindaraju Darshan Raj and Prakash S. Nayak


DOI: 10.2174/1570180812666150630182740



Most Accessed Articles

Synthesis and Cytotoxicity Evaluation of Novel Tricyclic Dihydropyrazolo [4,3-f][1,2,3]triazolo Diazepines

, 2018; 15(10): 1020-1025.

Chiranjeevi Bingi, Ashok Kale, Yedla Poornachandra, Chityal Ganesh Kumar and Krishnaiah Atmakur*


DOI: 10.2174/1570180815666180222143229


Antimicrobial Activities of Synthetic Arylidine Nicotinic and Isonicotinic Hydrazones

, 2018; 15(10): 1057-1067.

Muhammad Hayat, Khalid Mohammed Khan*, Sumayya Saeed, Uzma Salar, Momin Khan, Taimoor Baig, Aqeel Ahmad, Shahnaz Parveen and Muhammad Taha


DOI: 10.2174/1570180814666170914120337




Design, Synthesis and Characterization of Novel Urolithin Derivatives as Cholinesterase Inhibitor Agents

, 2018; 15(11): 1131-1140.

Maryam Norouzbahari, Emine V. Burgaz, Tugba Ercetin, Amirhossein Fallah, Alireza Foroumadi, Loghman Firoozpour, Mustafa F. Sahin, Mustafa Gazi and Hayrettin O. Gulcan*


DOI: 10.2174/1570180815666180115144608


Synthesis and Antibacterial/Antitubercular/Antioxidant Activities of Compounds Containing Fluoroquinolone Ring Linked to a 4-thiazolidinone Moiety

, 2018; 15(10): 1087-1094.

Tejeswara Rao Allaka, Naresh Kumar Katari, Venkanna Banothu, Srinubabu Maddela, Manojit Pal* and Jaya Shree Anireddy*


DOI: 10.2174/1570180815666171229150032


Synthesis and Biological Evaluation of Some Novel Thiophene-bearing Quinazoline Derivatives as EGFR Inhibitors

, 2019; 16(2): 102-110.

Min Zou, Bo Jin, Yanrong Liu, Huiping Chen, Zhuangli Zhang, Changzheng Zhang, Zhihong Zhao and Liyun Zheng*


DOI: 10.2174/1570180815666180803125935



Synthesis and Biological Evaluation of Novel Bioisosteric Analogues of Dimebon™

, 2010; 7(6): 446-451.

Alexandre Vasilevich Ivachtchenko, Eugene Borisovich Frolov, Oleg Dmitrievich Mitkin, Sergey Evgenevich Tkachenko and Alexandre Khvat


DOI: 10.2174/157018010791306579



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