Open Journal of Medicinal Chemistry

Journal Information
ISSN / EISSN : 21643121 / 2164313X
Current Publisher: Scientific Research Publishing, Inc, (10.4236)
Total articles ≅ 62
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Latest articles in this journal

Samiyah Alhamed, Jawzah Alnakhli, William Boadi, Ryan Beni
Open Journal of Medicinal Chemistry, Volume 9, pp 49-62; doi:10.4236/ojmc.2019.93003

Abstract:Antioxidants are substances that can prevent or slow damage to cells caused by free radicals, unstable molecules that the body produces as a reaction to environmental and other pressures. Free radicals may play a role in heart disease, cancer and other diseases. If the body cannot process and remove free radicals efficiently, oxidative stress can result. This can harm cells and body function. Free radicals are also known as reactive oxygen species (ROS). In this research, Triptorelin® (TRP) conjugates of triphenylmethanol derivatives (TPMs) were synthesized to evaluate their in vitro lipid peroxidation potency. Comparative lipid peroxidation assays between TRP-TPMs conjugates and the corresponding TPMs derivatives were measured using thiobarbituric reactive substance (TBARS) in a dose- and time-dependent manner following the Fenton’s pathway. Overall, TBARS decreased between 20% - 30% for the treated samples of synthesized conjugates compared to their respective control physical mixtures. These data suggest that TRP-TPMs derivatives can be used to improve the biological activity of TRP.
Sameena E. Tanwir, Ajay Kumar
Open Journal of Medicinal Chemistry, Volume 9, pp 1-35; doi:10.4236/ojmc.2019.91001

Abstract:Alzheimer’s disease (AD) is a neurodegenerative disease distinguished by progressive cognitive deterioration along with declining activities of daily living and behavioral changes. It is the commonest type of pre-senile and senile dementia. Many new therapeutic strategies have been developed in the last few years. We aimed at reviewing the evidence supporting these new therapeutic targets, including anti-amyloid and anti-Tau strategies. This review is focused on important future direction in investigation of potential therapeutic targets for AD drug discovery. Medical advances have improved treatment of many diseases but still there is a need to establish new tools for early diagnosis of AD. A thorough comprehensive understanding of the unexplored mechanism can ameliorate the diagnostic and therapeutic management of AD. There have been several disease-modifying therapeutic strategies for AD in the last few years and are presently at various phases of investigation. Few of them have shown promising results, but their safety and efficacy need to be further explored.
Ryan Beni, William Boadi, Kaleh Karim, Jawzah Alnakhli, Samiyah Alhamed, Beni Ryan, Boadi William, Karim Kaleh, Alnakhli Jawzah, Alhamed Samiyah
Open Journal of Medicinal Chemistry, Volume 9, pp 37-47; doi:10.4236/ojmc.2019.92002

Abstract:Leuprorelin® (LEP) is an FDA drug for breast cancer and prostate cancer treatment. There are several reported adverse effects such as transient hypertension, excessive salivation, and increased dysuria during treatment with LEP. In this study, the efficacy and toxicity of LEP were modified by using a drug delivery system to adjust the physicochemical properties. In this regard, Leuprorelin® conjugates of triphenylmethanol derivatives (TPMs) were synthesized as prodrugs. Comparative antiproliferative assays showed that LEP-TPMs conjugates had significantly higher antiproliferative activities than the corresponding non-covalent physical mixtures of the TPMs and LEP against human invasive ductal carcinoma (BT-549), human prostate carcinoma (PC3), human lung cancer (A549) and mouse pre-adipocytes (3T3-L1) cells.
B. Ramachandra, N. Venkatasubba Naidu
Open Journal of Medicinal Chemistry, Volume 8, pp 15-21; doi:10.4236/ojmc.2018.82002

Abstract:Simple, selective and sensitive spectrophotometric method has been developed for the determination of Azacitidine in pharmaceutical formulations and blood with MBTH (3-methyl-2-benzothiazolone hydrazone hydrochloride) reagent, at PH_4.0 which is extractable at 620 nm. Beer’s law is obeying in the concentration ranges 10 - 35 µg∙ml−1 for formulations and 4 - 24 µg∙ml−1 for blood sample. %R.S.D was found to be 0.0240%, 0.0610 and Recovery 99.82% 99.24% respectively. The method was completely validated and proven to be rugged. The interferences of the other ingredients and excipients were not observed. The repeatability and the performance of the proven method were conventional by point and interior proposition and through recovery studies.
Edward C. Lisic, Victoria G. Rand, Lana Ngo, Patrick Kent, Jeffrey Rice, Deidra Gerlach, Elizabeth T. Papish, Xiaohua Jiang
Open Journal of Medicinal Chemistry, Volume 8, pp 30-46; doi:10.4236/ojmc.2018.82004

Matthew Onyema Agu, Barminas Jeff Tsware, A. Osemeahon Sunday, Jude Chinedu Onwuka, Hotton Joseph Anthony
Open Journal of Medicinal Chemistry, Volume 8, pp 1-14; doi:10.4236/ojmc.2018.81001

V. Esther Rani, P. Raveendra Reddy
Open Journal of Medicinal Chemistry, Volume 8, pp 22-29; doi:10.4236/ojmc.2018.82003

Abstract:The most important nitrogen containing heterocycles of pyridine containing substituted phenyl azetidine-2-ones have found pharmacological application such as antibiotics and these compounds also have practical importance. The structure of the new derivatives was confirmed by the spectral data and elemental analyses. Out of five new derivatives, three were revealed mild to moderate activity compared with Streptomycin & Fluconazole as a reference standard. Among this new series, 3-chloro-1-(4-fluoro phenyl)/(4-chloro phenyl)-4-(pyridine-3-yl) azetidine-2-one (4a & b) were found most activity.
Ahmed M. El-Morsy, Mohamed S. El-Sayed, Hamada S. Abulkhair
Open Journal of Medicinal Chemistry, Volume 7, pp 1-17; doi:10.4236/ojmc.2017.71001

Abstract:A new series of 3-(methylthio)-1-phenyl-1H-pyrazolo[3,4-d]pyrimidine derivatives was synthesized. The structures of the new derivatives were confirmed by the spectral data and elemental analyses. The antitumor activity of this series against human breast adenocarcinoma cell line MCF7 was evaluated. Out of twenty new derivatives, ten were revealed mild to moderate activity compared with doxorubicin as a reference antitumor. Among this new series N-(2-chlorophenyl)-2-(3-(methylthio)-4-oxo-1-phenyl-1H-pyrazolo[3,4-d]pyrimidin-5(4H)-yl)acetamide (13a) was found the most active one with IC50 equal to 23 μM.
Shinya Nakamura, Kazuko Shimada, Genzoh Tanabe, Osamu Muraoka, Isao Nakanishi
Open Journal of Medicinal Chemistry, Volume 7, pp 19-28; doi:10.4236/ojmc.2017.72002

Ajay Kumar, Venkatesh Chelvam, Mahalingam Sakkarapalayam, Guo Li, Pedro Sanchez-Cruz, Natasha S. Piñero, Philip S. Low, Antonio E. Alegria
Open Journal of Medicinal Chemistry, Volume 6, pp 1-17; doi:10.4236/ojmc.2016.61001

Abstract:Almost all cells are easily killed by exposure to potent oxidants. Indeed, major pathogen defense mechanisms in both animal and plant kingdoms involve production of an oxidative burst, where host defense cells show an invading pathogen with reactive oxygen species (ROS). Although cancer cells can be similarly killed by ROS, development of oxidant-producing chemotherapies has been limited by their inherent nonspecificity and potential toxicity to healthy cells. In this paper, we describe the targeting of an ROS-generating molecule selectively to tumor cells using folate as the tumor-targeting ligand. For this purpose, we exploit the ability of 9,10-phenanthraquinone (PHQ) to enhance the continuous generation of H2O2 in the presence of ascorbic acid to establish a constitutive source of ROS within the tumor mass. We report here that incubation of folate receptor-expressing KB cells in culture with folate-PHQ plus ascorbate results in the death of the cancer cells with an IC50 of ~10 nM (folate-PHQ). We also demonstrate that a cleavable spacer linking folate to PHQ is significantly inferior to a noncleavable spacer, in contrast to most other folate-targeted therapeutic agents. Unfortunately, no evidence for folate-PHQ mediated tumor regression in murine tumor models is obtained, suggesting that unanticipated impediments to generation of cytotoxic quantities of ROS in vivo are encountered. Possible mechanisms and potential solutions to these unanticipated results are offered.