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Current Drug Discovery Technologies

Atousa Khalatbari, Mehdi Mahdavi, Fahimeh Jafarnezhad, Sanaz Afraei, Farzaneh Tofighi Zavareh, Zahra Aghazadeh, Afshin Ghaderi, Abbas Mirshafiey
This investigation evaluates the pro-apoptotic and anti-inflammatory effects of β-D-mannuronic acid [M2000] compared to diclofenac, based on gene expression involved in apoptosis and inflammation process [including Bcl2, NFκB, IL-8 and Cd49d] in peripheral blood mononuclear cells [PBMCs] of healthy donors under exvivo conditions. The venous blood of twelve healthy volunteers with aged 25-60 years, were collected in heparinized tubes. The healthy volunteers were selected from no smoking group and without using illicit drugs and suffering from diabetes...
November 9, 2018: Current Drug Discovery Technologies
Ishan I Panchal, Roshani Rajput, Ashish D Patel
CONTEXT: objective: The series of 2-(4-Phenylamino)-N-(5-((4-nitrophenoxy)methyl) -1,3,4-oxadiazol-2-yl)acetamide (5a-5e) and substituted N-(5-(Phenoxymethyl)-1,3,4-oxadiazol-2-yl)-2-(phenylamino)acetamide (5f-5i) were designed, synthesized and investigated for Collapsin response mediator protein 1 (CRMP 1) inhibitors as small lung cancer. DESIGN: Design of compounds was done by literature review and molecular docking studies in iGEMDOCK 2.0. METHODS AND MATERIAL: Novel 1, 3, 4 Oxadiazole derivatives were synthesized and characterized by melting point, TLC, IR Spectroscopy, Mass spectroscopy and 1H NMR...
November 5, 2018: Current Drug Discovery Technologies
Fatemeh Forouzanfar, Mohammad Mahdi Vahedi, Azita Aghaei, Hassan Rakhshandeh
BACKGROUND: Insomnia is the most common sleep disorder. The present study was undertaken to evaluate the sedative-hypnotic potential of hydroalcoholic extract (HAE) of Cuscuta epithymum and its fractions. METHOD: HAE and its fractions including: water fraction (WF), ethyl acetate fraction (EAF) and n-hexan fraction (NHF) were i.p administered to male mice and 30 min later pentobarbital (30 mg/kg, i.p.) was injected to induce sleep. Then the latent period and continuous sleeping time were recorded...
November 4, 2018: Current Drug Discovery Technologies
Bhavana B Bhat, N Udupa, D Sreedhar
Herbal medicines have been used by mankind from time immemorial. Moreover, many modern medicines are originated from plant sources. In earlier days, patients were dependent on herbs for treatment and well-being. However, due to advent of industrial revolution and modern science, scenario of treating diseases has changed over a period of time. Majority of patients started preferring allopathy medicines due to their several advantages over herbal medicines. However, due to long term treatment by allopathic medicines for chronic diseases have led to side effects, hence, patients are now drifting back to the traditional medicines...
November 4, 2018: Current Drug Discovery Technologies
Ishan I Panchal, Sandip N Badeliya, Rakesh Patel
mTORC1/ PI3K control multiple anabolic pathways, including protein synthesis, ribosome production, lipogenesis, and nucleotide synthesis, all of which are important for cell and tissue growth.Sapanisertib and Dactolisib inhibit PI3K/AKT/mTOR pathway, an important signalling pathway for many cellular functions such as growth control, metabolism and translation initiation.Dactolisib contain quinolin-3-yl-2,3-dihydroimidazo[4,5-c]quinolin scaffold and Sapanisertib contain benzo[d]oxazol-5-yl-1-ethyl-1H-pyrazolo[3,4-d]pyrimidinnucleous...
November 2, 2018: Current Drug Discovery Technologies
Farnoush Falahat, Sedigheh Ayatiafin, Lida Jarahi, Roshanak Mokaberinejad, Hasan Rakhshandeh, Zohre Feyzabadi, Mandana Tavakkoli
BACKGROUND: The aim of this study was to evaluate the efficacy of the herbal tea based on Foeniculum vulgare, on inducing regular bleeding in women with oligomenorrhea and secondary amenorrhea(oligo/amenorrhea). METHODS: Forty women aged 18- 40 with oligo/amenorrhea were enrolled in this randomized controlled clinical trial and were allocated to two groups equally. The women in the first group were treated by Fomentex (Foeniculum vulgare / Mentha longifolia / Vitex agnus-castus) herbal tea 11...
October 29, 2018: Current Drug Discovery Technologies
Yau Xin Yi, Anand Gaurav
INTRODUCTION: The primary aim of this study is to understand the binding of curcumin and its analogues to different PDE4 subtypes and identification of the role of PDE4 subtype inhibition in the anti-inflammatory property of curcumin. Docking analysis has been used to acquire the above mentioned structural information and this has been further used for designing of curcumin derivatives with better anti-inflammatory activity. MATERIALS AND METHOD: Curcumin and its analogues were subjected to docking using PDE4A, PDE4B, PDE4C and PDE4D as the target...
October 16, 2018: Current Drug Discovery Technologies
Marjan Mahjour, Arash Khoushabi
BACKGROUND: Vitiligo is a pigmentary disorder characterizing by white macules due to loss of melanocytes. Vitiligo affects about 1 to 4% of people around the world. The treatment of vitiligo has a high cost and the long process of treatment in spite of no complete remedy. It has various psychological side-effects such as depression and anxiety affecting the quality of life seriously. Avicenna in his Canon treated these patients over a thousand years ago. This study aimed to introduce some herbal drugs in vitiligo based on the Canon of Avicenna besides the conventional medical treatments...
October 16, 2018: Current Drug Discovery Technologies
Rudrax N S Priolkar, Sunil Shingade, Mahesh Palkar, Shivalingrao Mamle Desai
BACKGROUND: According to WHO, in 2017, about 90.5 million of people suffer from cancer and about 8.8 million deaths occurred due to disease. Although the chemotherapeutic agents have decreased the mortality among the cancer patients but high toxicity and non-specific targets are still major drawbacks. Many researchers have identified linomide, a 4-hydroxy-2-quinolone derivative, as a lead molecule for the development of anticancer agents. With this background we thought of the following objective...
October 8, 2018: Current Drug Discovery Technologies
Arvind Kumar, Harpreet Singh, Amrita Mishra, Arun K Mishra
OBJECTIVE: Aripiprazole,a synthetic compound, obtained by chemical modification of the structure of quinolinone is considered as an atypical antipsychotic drug. The present review is an attempt to summarize the updated information related to reported chemistry and pharmacology of Aripiprazole. DEVELOPMENT: Aripiprazole, under development by Otsuka Pharmaceutical, was approved by the U.S. Food and Drug Administration (USFDA) in the end months of 2002 to with an aim to treat patients with schizophrenia...
October 8, 2018: Current Drug Discovery Technologies
Krishna A Gajjar, Anuradha K Gajjar
Pharmacophore mapping and molecular docking can be synergistically integrated to improve the drug design and discovery process. A rational strategy, combiphore approach, derived from the combined study of Structure and Ligand based pharmacophore has been described to identify novel GPR40 modulators. DISCOtech module from Discovery studio was used for the generation of the Structure and Ligand based pharmacophore models which gave hydrophobic aromatic, ring aromatic and negative ionizable as essential pharmacophoric features...
October 8, 2018: Current Drug Discovery Technologies
Raja Chakraborty, Pratap Kalita, Saikat Sen
Utilization of the native starch is increasing globally because of its wide distribution and occurring naturally. Starch is mainly abundant in tubers and food grains. Scientific research on starch is increasing in recent years due to their unique physiochemical and biomedical properties. Native starch is an emerging biopolymer and copolymer in front of biomedical and pharmaceutical areas due to their renewability, biocompatibility, biodegradability and their relative inexpensiveness. There is increasing interest in natural starches to design and produce diverse products due to their pertinent structural properties and non-toxicity...
October 3, 2018: Current Drug Discovery Technologies
Michael P Okoh, Lukman A Alli, Martti E E Tolvanen, Maxwell Nwegbu
Introduction Nigeria has the largest burden of Sickle Cell Disease (SCD) with estimated 100,000 new born affected annually. SCD is a hemoglobin (Hb) disorder with the major form resulting from the substitution of a polar glutamate (Glu) by non-polar Valine (Val) in an invariant region, of Hb chain-subunit. Species of Hb found in sickle cell trait are HbA and HbS at a 60:40 proportion, in SCD only HbS, in the HbC disease only HbC, and in the SC disease it's HbS and HbC in a 50:50 equal proportion. Objective This paper reviews herbal medicines usagein sub-Saharan Africa (sSA) to ameliorate the crisis associated with SCD...
October 1, 2018: Current Drug Discovery Technologies
Jagatkumar Upadhyay, Anuradha Gajjar, B N Suhagia
BACKGROUND: Dipeptidyl Peptidase 4 (DPP 4) enzyme cleaves an incretin based glucoregulatory hormone Glucagon Like Peptide -1 from N-terminal where penultimate amino acid is either alanine or proline. Several DPP 4 inhibitors, "gliptins", are approved for management of Type 2 Diabetes or under clinical trial. In present study, combined pharmacophore and docking based virtual screening protocol was used for identification of new hits from the Specs Database, which would inhibit DPP 4...
September 26, 2018: Current Drug Discovery Technologies
Abdel-Baset Halim
Cell-based assays are an important part of the drug discovery process and clinical research. One of the main hurdles is to design sufficiently robust assays with adequate signal to noise parameters while maintaining the inherent physiology of the cells and not interfering with the pharmacology of target being investigated. A plethora of assays that assess cell viability (or cell heath in general) are commercially available and can be classified under different categories according to their concepts and principle of reactions...
September 24, 2018: Current Drug Discovery Technologies
Mayura A Kale, Gajanan M Sonwane
The computational studies on 2-phenazinamines with their protein targets have been carried out to design compounds with potential anticancer activity. This strategy of designing compounds possessing selectivity over specific tyrosine kinase has been achieved through G-QSAR and molecular docking studies. The objective of this research has been to design newer 2-phenazinamine derivatives as Bcr-Abl tyrosine kinase inhibitors by G-QSAR, molecular docking studies followed by wet lab studies along with evaluation of their anticancer potential...
September 13, 2018: Current Drug Discovery Technologies
Payal Chatterjee, Mukesh Yadav, Namrata Chauhan, Ying Huang, Yun Luo
Although the major role of Nrf2 has long been established as a transcription factor for providing cellular protection against oxidative stress, multiple pieces of research and reviews now claim exactly the opposite. The dilemma - "to activate or inhibit" the protein requires an immediate answer, which evidently links cellular metabolism to the causes and purpose of cancer. Profusely growing cancerous cells have prolific energy requirements, which can only be fulfilled by modulating cellular metabolism...
September 10, 2018: Current Drug Discovery Technologies
Anuj Kumar, Yogesh Kumar, Jagdish K Sahu, Sushil Kumar
BACKGROUND: Due to the appearance of communicable microbial diseases and the toxicity related with presently used several antimicrobials such as β-lactam antibiotics, tetracyclines, quinolones, macrolides, glycopeptides (vancomycin) etc, demand for new antimicrobial agents has become great concern in new technologies to improve efficacy and safety. METHODS: In search of new antimicrobial agents with higher potency, some N-substituted benzimidazole derivatives (4, 5a-5h & 6) were obtained by chloroacetylation of benzimidazole followed by reaction with different amines which were characterized by spectroscopic methods...
August 31, 2018: Current Drug Discovery Technologies
Krishna A Gajjar, Anuradha K Gajjar
Human GPR40 receptor, also known as free fatty-acid receptor 1, is a G-protein-coupled receptor that binds long chain free fatty acids to enhance glucose-dependent insulin secretion. In order to improve the resistance and efficacy, computational tools were utilized. To build the 3D-QSAR models, CoMFA (Comparative Molecular Field Analysis), CoMSIA (Comparative Molecular Similarity Indices Analysis) and HQSAR (Hologram Quantitative Structure Activity Relationship) were performed on series of 3-aryl-3-ethoxypropanoic acid derivatives...
August 29, 2018: Current Drug Discovery Technologies
Salim Bouchentouf
BACKGROUND: In medicinal chemistry, the discovery of small organic molecules that can be optimized and lead to a future drug capable of effectively modulating the biological activity of a therapeutic target remains as major challenge. Because of harmful secondary effects of synthesized therapeutic molecules, the development of research has been oriented towards phytomedicines. Phenolic compounds from medicinal plants are constantly explored for new therapeutic use. METHODS: In this paper, we studied interactions between main enzymes responsible on type 2 diabetes mellitus (T2DM) and phenolic compounds from nettle (Urtica dioica L...
August 28, 2018: Current Drug Discovery Technologies
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