Article
Pharmacology & Pharmacy
Saad M. Alshahrani, El-Sayed Khafagy, Yassine Riadi, Ahmed Al Saqr, Munerah M. Alfadhel, Wael A. H. Hegazy
Summary: A new ZnO-PEGylated AMB nanoparticles with strong antifungal effects on Candida spp. were synthesized. Compared to other nanoparticles and free AMB, ZnO-AMB-PEG significantly reduced the minimum inhibitory concentration and minimum fungicidal concentration. Additionally, the nanoparticles had little nephrotoxicity.
Article
Microbiology
Lajos Forgacs, Andrew M. Borman, Renato Kovacs, David Balazsi, Zoltan Toth, Bence Balazs, Chiu Chun-Ju, Gabor Kardos, Ilona Kovacs, Laszlo Majoros
Summary: The efficacy of AMB against Candida auris is weak, leading to therapeutic failures. It is necessary to maximize killing at the start of treatment to avoid complications in the heart and central nervous system.
Article
Chemistry, Medicinal
Liping Li, Hao Wu, Shuo Zhu, Zhe Ji, Xiaochen Chi, Fei Xie, Yumeng Hao, Hui Lu, Feng Yang, Lan Yan, Dazhi Zhang, Yuanying Jiang, Tingjunhong Ni
Summary: This study identified a compound, P163-0892, that showed potent antifungal activity against Cryptococcus spp. both in vitro and in vivo. It also demonstrated that P163-0892 was not cytotoxic and showed synergism with fluconazole. The findings highlight the potential of P163-0892 as a novel anti-Cryptococcus agent.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Polymer Science
Elsa R. Arias, Vivian Angarita-Villamizar, Yolima Baena, Claudia Parra-Giraldo, Leon D. Perez
Summary: The research studied the effect of modifying polymer micelles with DSPE as carriers for AmB, finding that the modified copolymers self-assembled into particles with sizes below 100 nm and a lower critical micelle concentration. Furthermore, the presence of DSPE increased the loading capacity of AmB, reduced its aggregation, and decreased its toxicity towards red blood cells.
Article
Pharmacology & Pharmacy
Ahmad Khosravi, Iraj Sharifi, Hadi Tavakkoli, Elaheh Molaakbari, Sina Bahraminegad, Ehsan Salarkia, Fatemeh Seyedi, Alireza Keyhani, Zohreh Salari, Fatemeh Sharifi, Mehdi Bamorovat, Ali Afgar, Shahriar Dabiri
Summary: The study investigated the effects of different types of amphotericin B (Amp B) on fetal organs and found that AmBisome has superior pharmacological effects compared to Amp B. The in vivo analyses supported these findings.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Qifan Zhou, Yinzhu Luo, Yujun Zhu, Qishu Chen, Jingfei Qiu, Feng Cong, Yingjun Li, Xumu Zhang
Summary: GS-441524 is a broad-spectrum antiviral nucleoside with poor oral bioavailability. Researchers designed and synthesized conjugates by combining nonsteroidal anti-inflammatory drugs (NSAIDs) with GS-441524. The ibuprofen conjugate, ATV041, showed strong in vitro anti-coronaviral activity against four zoonotic coronaviruses and had favorable oral bioavailability. In mouse experiments, ATV041 dose-dependently reduced viral replication and alleviated inflammation in the liver and lungs caused by the infection. This study provides a novel drug conjugate strategy to improve oral pharmacokinetics and offers a potent lead compound for further anti-coronavirus studies.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Qiyu Li, Wenjing Li, Keyuan Xu, Yutong Xing, Haobo Shi, Zhe Jing, Shuang Li, Zhangyong Hong
Summary: This study proposed a novel design strategy for miniaturized ADCs by site-specific coupling drug molecules and small ligand proteins via a bifunctional poly(ethylene glycol) (PEG) chain, significantly prolonging the circulation half-life while reducing the cytotoxicity of the conjugates. The results indicated that prolonging the half-life is very helpful in improving the therapeutic capacity of miniaturized ADCs.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Aviran Amir, Michal Levin-Khalifa, Tamar Dvash
Summary: Fungal infections are becoming more of a problem for immunocompromised individuals, and there is evidence of new medicine-resistant strains. Researchers have discovered an ethanol amide derivative of Nystatin that shows promise as a potential drug with higher solubility and lower toxicity.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Medicine, Research & Experimental
Xiaotian Ji, Changying Shi, Dandan Guo, Xiguang Yang, Liye Suo, Juntao Luo
Summary: Systemic fungal infections are a growing health problem and the drug of choice for severe cases is Amphotericin B. However, it has dose-limiting side effects. In this study, researchers prepared nanocarriers called telodendrimers to encapsulate AmB and adjust its aggregation status. The optimized nanocarrier showed improved antifungal activity, reduced toxicity, and increased therapeutic index compared to common clinical formulations.
MOLECULAR PHARMACEUTICS
(2023)
Article
Chemistry, Multidisciplinary
Guldjan Yakub, Nevena E. Manolova, Iliya B. Rashkov, Nadya Markova, Reneta Toshkova, Ani Georgieva, Rosica Mincheva, Antoniya Toncheva, Jean -Marie Raquez, Philippe Dubois
Summary: The synthesis of polymer prodrug structures based on natural compounds has shown promise in cancer prevention and detection. In this study, pegylated curcumin derivatives were successfully prepared and showed cytotoxic and antibacterial activity.
Article
Medicine, Legal
Francesca Pretto, Rex E. FitzGerald
Summary: ADCs are complex biotherapeutics that combine tumor-targeting antibodies with potent cytotoxicants for cancer treatment, with a growing number of drugs in development. Safety evaluation of ADCs requires novel integrated strategies to address off-target toxicity and narrow therapeutic index, with a focus on developing and validating analytical assays.
REGULATORY TOXICOLOGY AND PHARMACOLOGY
(2021)
Review
Pharmacology & Pharmacy
Tahereh Zadeh Mehrizi, Seyed Mahdi Rezayat, Mehdi Shafiee Ardestani, Hasan Ebrahimi Shahmabadi, Amitis Ramezani
Summary: The review study evaluated the effectiveness of chitosan nanocarrier on the treatment of leishmaniasis, showing that by increasing drug loading efficiency and reducing toxicity, chitosan nanoparticles can enhance the inhibition and killing of the parasite. The study also highlighted that chitosan nanoparticles with higher drug loading were the most effective in inhibiting and killing the parasite, suggesting chitosan nanocarrier as a potential candidate for future treatment without causing side effects.
CURRENT DRUG DELIVERY
(2021)
Article
Pharmacology & Pharmacy
Alessia Felici, Michele Schlich, Daniele Di Mascolo, Luca Goldoni, Anna Lisa Palange, Paolo Decuzzi
Summary: Rationally designing drug conjugates-particle complexes can maximize drug loading and release from nanoparticles, leading to improved therapeutic efficacy.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2022)
Article
Chemistry, Applied
Sophie Bou, Feifei Ng, Elise Guegain, Charlotte Peloso, Adolfo Lopez-Noriega, Mayeul Collot
Summary: Biodegradable and biocompatible polymer materials are important for controlled drug delivery. This study developed a FRET system for monitoring the stability of short copolymers. Results showed that these materials rapidly hydrolyze into approved products in the subcutaneous space of mice.
REACTIVE & FUNCTIONAL POLYMERS
(2023)
Article
Infectious Diseases
Katharine E. Stott, Ajisa Ahmadu, Cheusisime Kajanga, Melanie Moyo, Ebbie Gondwe, Wezzie Chimang'anga, Madalitso Chasweka, Jennifer Unsworth, Ana Jimenez-Valverde, Bhavana Jagota, Reya Shah, David S. Lawrence, David G. Lalloo, Tom Harrison, Joseph N. Jarvis, William Hope, Henry C. Mwandumba
Summary: This study described the pharmacokinetics (PK) of flucytosine in patients with HIV-associated cryptococcal meningoencephalitis and found significant interindividual variability in flucytosine PK in plasma and cerebrospinal fluid (CSF). A four-compartment PK model was developed, and Monte Carlo simulations were performed to study the dosage of flucytosine in different schedules.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2023)
Article
Chemistry, Organic
Keshaba N. Parida, Gulab K. Pathe, Shimon Maksymenko, Alex M. Szpilman
BEILSTEIN JOURNAL OF ORGANIC CHEMISTRY
(2018)
Article
Chemistry, Organic
Atul A. More, Gulab K. Pathe, Keshaba N. Parida, Shimon Maksymenko, Yuriy B. Lipisa, Alex M. Szpilman
JOURNAL OF ORGANIC CHEMISTRY
(2018)
Article
Engineering, Biomedical
David Svetlizky, Ofer Levi, Itai Benhar, Noam Eliaz
JOURNAL OF THE MECHANICAL BEHAVIOR OF BIOMEDICAL MATERIALS
(2019)
Article
Chemistry, Organic
Atul A. More, Sourav K. Santra, Alex M. Szpilman
Article
Chemistry, Multidisciplinary
Shlomy Arava, Sourav K. Santra, Gulab K. Pathe, Raja Kapanaiah, Alex M. Szpilman
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2020)
Article
Chemistry, Organic
Atul A. More, Alex M. Szpilman
Article
Chemistry, Organic
Sourav K. Santra, Alex M. Szpilman
Summary: In this study, a visible-light-mediated benzylic C-H oxygenation reaction has been reported, which can take place at ambient temperature and air pressure with higher yield than current industrial conditions.
JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Abhaya K. Mishra, Galit Parvari, Sourav K. Santra, Andrii Bazylevich, Ortal Dorfman, Jonatan Rahamim, Yoav Eichen, Alex M. Szpilman
Summary: This study presents a peptide coupling reaction design that relies on sun-light activation to generate a novel coupling reagent in situ. The method is rapid, does not require dry solvents or inert atmosphere, and is compatible with all common amino acids and protecting groups. The proposed mechanism is supported by experimental and computational studies.
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2021)
Review
Chemistry, Organic
Ishita Neogi, Alex M. Szpilman
SYNTHESIS-STUTTGART
(2022)
Article
Chemistry, Multidisciplinary
Sagi Sevilia, Galit Parvari, Jonathan Bernstein, Natalia Fridman, Dan Grinstein, Levi Gottlieb, Yoav Eichen, Alex M. Szpilman
Summary: We have shown that salts of 1-(2-hydroxyethyl)-1H-imidazol-3-ium and 1-(2-hydroxyethyl)-3-methyl-1H-imidazol-3-ium, as well as their nitrite ester salts, possess high decomposition enthalpies, high decomposition temperatures, and high densities. Particularly, the perchlorate salts exhibit potential as energetic materials. Many of these salts are ionic liquids, which could be useful as energetic plasticizers or gel fillers.
Article
Chemistry, Organic
Lenin Kumar Verdhi, Natalia Fridman, Alex M. Szpilman
Summary: A chiral nitroxide catalyst, generated in situ by a readily prepared chiral hydroxylamine precatalyst, in combination with a copper co-catalyst, serves as an environmentally friendly terminal oxidant for the enantioselective oxidative kinetic resolution of racemic axially chiral N-arylpyrrole alcohols, providing high enantioselectivity and reaction efficiency.
Article
Chemistry, Organic
Asit Ghosh, Yuriy B. Lipisa, Natalia Fridman, Alex M. Szpilman
Summary: 2-Nitrocyclopropanes with various functional groups can be obtained as single diastereoisomers in one step by introducing ketones, amides, esters, and carboxylic acids at the 1 position of corresponding unsaturated carbonyl compounds using nitromethane as the nitromethylene component. The reaction proceeds at room temperature under mild conditions and the products can be further transformed into cyclopropyl-amino acids, among others. Nitrocyclopropanes and aminocyclopropanes are important structural motifs found in biologically active compounds and natural products.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Lenin Kumar Verdhi, Asit Ghosh, Natalia Fridman, Alex M. Szpilman
Summary: A copper and chiral nitroxide co-catalyzed aerobic enantioselectiveoxidation process has been developed for the synthesis of axially chiral molecules. Two complementary atroposelective approaches, oxidative kinetic resolution (OKR) and desymmetrization, were studied using ambient air as the terminal oxidant. OKR results in optically pure compounds with er up to 3.5:96.5 and 5.5:94.5 for rac-N-arylpyrrole alcohols and rac-biaryl alcohols, respectively. Desymmetrization of prochiral diols produces axially chiral biaryl compounds with er up to 99:1.
JOURNAL OF ORGANIC CHEMISTRY
(2023)
Article
Chemistry, Organic
Subrata Maity, Alex M. Szpilman
Summary: In this paper, a new method for the formation of 2-fluoroenones from ubiquitous enones in a single step is reported. The reaction shows high yields (63-90%) and is applicable to a wide range of aromatic and alkenyl enones. Mechanistic investigations reveal a rare umpolung Morita-Baylis-Hillman-type mechanism.
Article
Chemistry, Organic
Hila Toledo, Boris Tumanskii, Denis Sh. Sabirov, Alexander Kaushansky, Natalia Fridman, Alex M. Szpilman
ORGANIC & BIOMOLECULAR CHEMISTRY
(2019)
