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"Letters in Drug Design & Discovery should be available in every library in the pharmaceutical industry and in universities."

R. F. Borne, Associate Director
Laboratory for Applied Drug Design and Synthesis, The University of Mississippi, USA

Forthcoming Special Issues

Antimalarial drug discovery - Exploration of novel structural scaffolds towards development of potent antimalarial agents

Guest Editor(s): Mithun Rudrapal, Dipak Chetia
Tentative Publication Date: July, 2019
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Special Issues - In-Press

Opportunities and challenges in anticandidal drug discovery and development

Guest Editor(s): Mohammad Abid
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Published Special Issues


Letters in Drug Design & Discovery, Volume 15, Number 03
Guest Editor(s): Gokhan Zengin, Marcello Locatelli

Authors' Comments
I would like to thank Bentham Science Publishers for their peerless effort to keep up scientists and students updated with the latest science and research work. Actually, Bentham assists researchers to achieve their goals to spread their reputation worldwide. I have experienced sincere, efficient and effective communication while dealing with Bentham team members. I intend to submit my work to Bentham and try to pick up journals that match my research profile. I have submitted a recent work to Medicinal Chemistry and nowadays I am drafting a manuscript targeting Current Pharmaceutical Design. Honestly, no words neither sentences would express my gratefulness and admiration. Bentham has offered my institution three months trial to access their journal lists and surf on its Board. This free access trial fulfills my literature review and broadens my horizon to absorb the recent research in pharmaceutical sciences and medicinal chemistry. Finally, I wish Bentham more success and achievement!

Dima Sabbah
(Department of Pharmacy, Faculty of Pharmacy, Al-Zaytoonah University of Jordan, Amman, Jordan)

Letters in Drug Design & Discovery


Volume 16


Number 2

Biography   Open Access

Research Article   Open Access

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

, 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

Research Article

Synthesis and Anticancer Activity of Some 1H-inden-1-one Substituted (Heteroaryl)Acetamide Derivatives

, 16(2): 111 - 118

Ahmet Cagri Karaburun, Nalan Gundogdu-Karaburun*, Leyla Yurttas, Ismail Kayagil and Seref Demirayak

DOI: 10.2174/1570180815666180606081042

Research Article

Research Article

The Impact of Antioxidants from the Diet on Breast Cancer Cells Monitored by Raman Microspectroscopy

, 16(2): 127 - 137

Paula Sofia Coutinho Medeiros, Ana Lúcia Marques Batista de Carvalho*, Cristina Ruano, Juan Carlos Otero and Maria Paula Matos Marques

DOI: 10.2174/1570180815666180502120804

Research Article

Indolin-2-one Derivatives: Theoretical Studies Aimed at Finding More Potent Aurora B Kinase Inhibitors

, 16(2): 138 - 152

Ítalo Antônio Fernandes, Tamiris Maria de Assis, Isael Aparecido Rosa and Elaine Fontes Ferreira da Cunha*

DOI: 10.2174/1570180815666180528090945

Research Article

Research Article

Synthesis, Antimicrobial Evaluation and In silico Studies of Novel 2,4- disubstituted-1,3-thiazole Derivatives

, 16(2): 160 - 173

Mir Mohammad Masood, Mohammad Irfan, Shadab Alam , Phool Hasan, Aarfa Queen, Shifa Shahid, Muhammad Zahid, Amir Azam and Mohammad Abid*

DOI: 10.2174/1570180815666180502120042

Articles Ahead of Print

Design, Synthesis and Antitumor Activity of Quinazoline Derivatives Bearing 2,3-Dihydro-indole or 1,2,3,4-Tetrahydroquinoline

Yiqiang Ou Yang, Bingbing Zhao, Xiuying Chen, Caolin Wang, Hong Zhang, Shuang Jia, Wufu Zhu* and Pengwu Zheng

View Abstract

Synthesis and Anticancer Activity of New Hydrazide-hydrazones and Their Pd(II) Complexes

Bedia Kocyigit-Kaymakcioglu*, Senem Sinem Yazici, Fatih Tok, Miris Dikmen, Selin Engur , Emine Elcin Oruc-Emre and Aysegul Iyidogan

View Abstract

Synthesis and Anti-Tumor Activity Evaluation of Novel 7-Fluoro-4-(1- Piperazinyl) Quinolines

Dan Liu*, Aiqi Xue, Zhixin Liu, Yi Zhang, Penghui Peng and Haifeng Wang

View Abstract

Paclitaxel-Tyroserleutide Conjugates Self-assembly into Nanocarrier for Drug Delivery

Yongjia Liu, Leilei Shi, Bangshang Zhu*, Yue Su, Hui Li and Xinyuan Zhu

View Abstract

Synthesis and Biological Activity of N-(arylsulfonyl) Valine Hydrazones and Assistance of NMR Spectroscopy for Definitive 3D Structure

Sevil Senkardes, Esra Tatar, Ridvan Nepravishta, Dorisa Cela, Maurizio Paci, Ozlem Bingol Ozakpinar, Turgut Sekerler, Erik De Clercq, Christophe Pannecouque, S. Guniz Kucukguzel* and Ilkay Kucukguzel

View Abstract

Structure Based Identification of Potential Inhibitors of NS3 Protein of Zika virus

Md Imam Faizan, Abu Turab Naqvi , Md. Imtaiyaz Hassan, Mohd Abdullah, Ayesha Tazeen, Zoya Shafat, Malik Hisamuddin, Aftab Alam, Shahnawaz Ali, Sher Ali, Anam Farooqui, Abu Hamza, Nazish Parveen, Farah Deeba, Anwar Ahmed and Shama Parveen*

View Abstract

(Substituted)-benzo[b]thiophene-4-carboxamide Synthesis and Antiproliferative Activity Study

Chandrakant D. Pawar, Dattatraya N. Pansare and Devanand B. Shinde*

View Abstract

QSAR and Molecular Modeling Studies on a Series of Pyrrolidine Analogs Acting as BACE-1 Inhibitors

Richa Arya, Satya P. Gupta*, S. Paliwal, Seema Kesar, Achal Mishra and Y.S. Prabhakar

View Abstract

Abstracts Ahead of Print

Targeting inflammation with conjugate cinnamic amides, ethers and esters

Ioannis Fotopoulos, Eleni Pontiki and Dimitra Hadjipavlou-Litina*

View Abstract

The structure of MT189-tubulin complex provides insights into drug design

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

View Abstract

Synthesis and Analgesic Activity of Monoterpenoid Aldehyde-Derived Hydro-2H-chromeneols

Irina V. Il`ina*, Ekaterina A. Morozova*, Dina V. Korсhagina, Konstantin P. Volcho, Tat`yana G. Tolstikova and Nariman F. Salakhutdinov

View Abstract

Synthesis, antiproliferative, and antioxidant activities of substituted N-[(1,3,4-oxadiazol-2-yl)methyl]benzamines

Mohamed Jawed Ahsan, Lakshya Bhandari, Shally Makkar, Rajan Singh, Mohd. Zaheen Hassan, Mohammed H. Geesi, Mohammed Afroz Bakht, Surender Singh Jadav, Tuniki Balaraju, Yassine Riadi , Sandhya Rani, Habibullah Khalilullah, Vasubabu Gorantla and Afzal Hussain

View Abstract

Synthesis of Limonin Derivatives with Improved Anti-inflammatory and Analgesic Properties

Chengshu Jia, Bin Hub, Yingying Ji, Yourui Su, Guoqing Gong*, Qihua Zhu and Yungen Xu*

View Abstract

The natural products as hydroxymethylglutaryl-CoA reductase inhibitors

Hayrettin Ozan Gulcan*, Serkan Yigitkan and Ilkay Erdogan Orhan

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

Antimicrobial, Gastroprotective and Healing Effect of the Hydroalcoholic Extract of Astronium fraxinifolium

, 2018; 15(3): 325 - 334

Anita Oliveira Brito Pereira Bezerra Martins, Ana Luiza Albuquerque Siebra, Cicera Datiane de Morais Oliveira, Gerlania Oliveira Leite, Henrique Douglas Melo Coutinho, Margareth Linde Athayde, Aline Augusti Bolignon, Jacqueline Cosmo Andrade, Larissa Rolim Oliveira, Marta Regina Kerntopf, Roseli Barbosa, Francisco Rafael Alves Santana Cesario, Thales Silva Coutinho, Lucindo Jose Quintans-Junior and Irwin Rose Alencar de Menezes*

DOI: 10.2174/1570180814666170213160114

Open Access Articles

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*

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

, 2018; 15: 1 - 7 (E-Pub Ahead of Print)

David Illes Nagy, Alajos Grun, Julia Sinkovicz, Sandor Garadnay, Istvan Greiner and Gyorgy Keglevich*

A Facile Synthesis and Drug Design of Some New Heterocyclic Compounds Incorporating Pyridine Moiety and Their Antimicrobial Evaluation

, 2017; 14(7): 752 - 762

Fathy M. Abdelrazek, Sobhi M. Gomha*, Aly H. Abdelrahman, Peter Metz and Mohsen A. Sayed

Alzheimer’s Disease Drugs- In Vitro Comparison of Cholinesterase Inhibition and beta-amyloid Modulation

, 2017; 14(6): 743 - 750

Ondrej Holas, Jan Korabecny, Zuzana Gazova, Katarina Siposova, Kamil Musilek, Veronika Opletalova, Lukas Gorecki, Eugenie Nepovimova, Katarina Spilovska, Eva Mezeiova and Kamil Kuca*

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

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

Synthesis of New Thiazolyl-Pyrazoline Derivatives and Evaluation of Their Antimicrobial, Cytotoxic and Genotoxic Effects

, 2018; 15(7): 744-756.

Belgin Sever, Mehlika Dilek Altıntop, Hulya Karaca Gencer, Handan Acelya Kapkac, Ozlem Atli, Merve Baysal and Ahmet Ozdemir*

DOI: 10.2174/1570180814666170925152902

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

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

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 In Vitro Evaluation of Novel 1, 2, 4-Triazole Derivatives as Antifungal Agents

, 2010; 7(1): 46-49.

Ganesh R. Kokil, Prarthana V. Rewatkar, Sandeep Gosain, Saurabh Aggarwal, Arunima Verma, Atin Kalra and Suresh Thareja

DOI: 10.2174/157018010789869415

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