A Recent Review on Drug Modification Using 1,2,3-triazole

2020 ◽  
Vol 14 (2) ◽  
pp. 71-87
Author(s):  
Adarsh Sahu ◽  
Preeti Sahu ◽  
Ramkishore Agrawal
Keyword(s):  
Structural Features ◽  
Molecular Hybridization ◽  
Molecular Fragments ◽  
Reaction Conditions ◽  
Widespread Occurrence ◽  
Drug Discovery And Development ◽  
Bioisosteric Replacement ◽  
Anti Cancer ◽  
Medicinal Properties ◽  
Drug Modification

Motivated by evidence garnered from literature probing the use of triazoles in drug discovery and development, we reported the utilization of bioisosteric replacement and molecular hybridization in this review. Bio-isosteric replacement has played a significant role in modulating rapid and versatile strategy in synthesizing molecules with multifaceted medicinal properties. Molecular hybridization seeks to conjugate two molecular fragments with diverse applications under very mild reaction conditions. In this regard, 1,2,3-triazole is a well-known scaffold with widespread occurrence in medicinal compounds. It is characterized to have several bioactivities such as anti-microbial, anti-cancer, anti-viral, analgesic, anti- inflammatory effects. Furthermore, the structural features of 1,2,3-triazoles enable it to mimic different functional groups justifying its use as bio-isostere for the synthesis of new molecules of medicinal interest, which we have reported briefly.

Understanding factors controlling depolymerization and polymerization in catalytic degradation of β-ether linked model lignin compounds by versatile peroxidase

2017 ◽  
Vol 19 (9) ◽  
pp. 2145-2154 ◽  
Author(s):  
Jijiao Zeng ◽  
Matthew J. L. Mills ◽  
Blake A. Simmons ◽  
Michael S. Kent ◽  
Kenneth L. Sale
Keyword(s):  
Structural Features ◽  
Catalytic Degradation ◽  
Versatile Peroxidase ◽  
Reaction Conditions ◽  
Linked Model

Insights into reaction conditions and structural features of lignin that facilitate its versatile peroxidase catalyzed depolymerization.

scholarly journals Total Syntheses of Pladienolide-Derived Spliceosome Modulators

Molecules ◽  
2021 ◽  
Vol 26 (19) ◽  
pp. 5938
Author(s):  
Jaehoon Sim ◽  
Eunbin Jang ◽  
Hyun Jin Kim ◽  
Hongjun Jeon
Keyword(s):  
Total Synthesis ◽  
Natural Product ◽  
Structural Features ◽  
Synthetic Approach ◽  
Synthetic Analog ◽  
Phase I Clinical Trials ◽  
Total Syntheses ◽  
Naturally Occurring ◽  
Anti Cancer ◽  
Synthetic Approaches

Pladienolides, an emerging class of naturally occurring spliceosome modulators, exhibit interesting structural features, such as highly substituted 12-membered macrocycles and epoxide-containing diene side chains. The potential of pladienolides as anti-cancer agents is confirmed by H3B-8800, a synthetic analog of this natural product class, which is currently under Phase I clinical trials. Since its isolation in 2004 and the first total synthesis in 2007, a dozen total syntheses and synthetic approaches toward the pladienolide class have been reported to date. This review focuses on the eight completed total syntheses of naturally occurring pladienolides or their synthetic analogs, in addition to a synthetic approach to the main framework of the natural product.

scholarly journals Macrophage checkpoint blockade: results from initial clinical trials, binding analyses, and CD47-SIRPα structure–function

2020 ◽  
Vol 3 (2) ◽  
pp. 80-94 ◽  
Author(s):  
AbdelAziz R Jalil ◽  
Jason C Andrechak ◽  
Dennis E Discher
Keyword(s):  
Clinical Trials ◽  
Regulatory Protein ◽  
Clinical Results ◽  
Structural Features ◽  
Clinical Development ◽  
Combination Therapies ◽  
Syngeneic Mouse ◽  
Solid Malignancies ◽  
Anti Cancer ◽  
Tumor Types

Abstract The macrophage checkpoint is an anti-phagocytic interaction between signal regulatory protein alpha (SIRPα) on a macrophage and CD47 on all types of cells – ranging from blood cells to cancer cells. This interaction has emerged over the last decade as a potential co-target in cancer when combined with other anti-cancer agents, with antibodies against CD47 and SIRPα currently in preclinical and clinical development for a variety of hematological and solid malignancies. Monotherapy with CD47 blockade is ineffective in human clinical trials against many tumor types tested to date, except for rare cutaneous and peripheral lymphomas. In contrast, pre-clinical results show efficacy in multiple syngeneic mouse models of cancer, suggesting that many of these tumor models are more immunogenic and likely artificial compared to human tumors. However, combination therapies in humans of anti-CD47 with agents such as the anti-tumor antibody rituximab do show efficacy against liquid tumors (lymphoma) and are promising. Here, we review such trials as well as key interaction and structural features of CD47-SIRPα.

A close look at the structural features and reaction conditions that modulate the synthesis of low and high molecular weight fructans by levansucrases

2019 ◽  
Vol 219 ◽  
pp. 130-142 ◽  
Author(s):  
Maria Elena Ortiz-Soto ◽  
Jaime R. Porras-Domínguez ◽  
Jürgen Seibel ◽  
Agustín López-Munguía
Keyword(s):  
Molecular Weight ◽  
High Molecular Weight ◽  
Structural Features ◽  
Reaction Conditions

scholarly journals Medicinal properties of fungi occurring on Betula sp. trees. A review

2016 ◽  
Vol 62 (3) ◽  
pp. 63-76
Author(s):  
Joanna Smolibowska ◽  
Marcin Szymański ◽  
Arkadiusz Szymański
Keyword(s):  
Ganoderma Lucidum ◽  
Lentinula Edodes ◽  
Human Organism ◽  
Inonotus Obliquus ◽  
Fomes Fomentarius ◽  
Anti Cancer ◽  
Lenzites Betulina ◽  
Medicinal Properties

Summary The article presents the chemical costituents and pharmacological properties of polyporoid fungi found on birch, namely Piptoporus betulinus, Inonotus obliquus, Lenzites betulina, Fomes fomentarius, and Trametes versicolor. The in vitro and in vivo studies on the effect of different extracts from above-mentioned fungi on the human organism shown anti-cancer, anti-inflammatory, antiviral, antibacterial and immunostimulant activity, conditioned by the presence of such compounds as polysaccharides, polyphenols or terpenes. These fungi are commonly found in Poland and may superbly compete with Ganoderma lucidum (Reishi) or Lentinula edodes (Shitake) used in Asia for medicinal purposes.

scholarly journals Di-tungsten Bis-carbene Complexes Linked by Condensed Heteroaromatic Spacers

2007 ◽  
Vol 62 (3) ◽  
pp. 419-426 ◽  
Author(s):  
Marilé Landmana ◽  
Helmar Görls ◽  
Chantelle Crause ◽  
Hubert Nienaber ◽  
Andrew Olivier ◽  
...  
Keyword(s):  
Structural Features ◽  
Crystallographic Data ◽  
Reaction Conditions ◽  
Carbene Complexes

The 2,7-dilithiated substrates of 3,6-dimethylthieno[3,2-b]thiophene, N,N′-dimethylpyrrolo[3,2- b]pyrrole and N-methylthieno[3,2-b]pyrrole were reacted with W(CO)6 to give, after subsequent alkylation with Et3OBF4, the ditungsten biscarbene complexes [(CO)5W{C(OEt)XXC(OEt)} W(CO)5] (XX = condensed heteroaromatic spacers). Sites of attack during the dilithiation of the condensed rings were studied and compared, and the yields of the desired ditungsten biscarbene complexes optimized by changing the reaction conditions according to the role of the heteroatoms in the rings. The crystallographic data of the three ditungsten biscarbene complexes are reported and their structural features compared. The methyl substituents on the condensed heteroaromatic rings play an important role in determining the molecular configurations.

scholarly journals Medicinal properties of Abutilon indicum

2018 ◽  
Vol 1 (1) ◽  
pp. 1-4
Author(s):  
S Rajeshwari ◽  
SP Sevarkodiyone
Keyword(s):  
Medicinal Plant ◽  
Traditional Medicine ◽  
Phytochemical Analysis ◽  
Vaginal Infections ◽  
Anti Cancer ◽  
Anti Oxidant ◽  
Medicinal Properties ◽  
Anti Inflammatory ◽  
Larvicidal Activities ◽  
Abutilon Indicum

Abutilon indicum is a common Indian shrub, belonging to the family Malvaceae; Also known as Mallow in english, Abutilon indicum is used as a medicinal plant. It has been extensively used as a traditional medicine as a laxative, emollient, analgesic, anti-diabetic, anti-inflammatory and blood tonic agent and also in the treatment of leprosy, urinary disease, jaundice, piles, relieving thirst, cleaning wounds and ulcers, vaginal infections, diarrhea, rheumatism, mumps, pulmonary tuberculosis, bronchitis, allergy, blood dysentery, some nervous and some ear problems. Various studies on the plant extract have been performed to confirm the anti-oxidant, anti-bacterial, analgesic, anti-inflammatory, anti-cancer, hepato-protective, immuno-modulatory and larvicidal activities of the plant. This plant is often used as a medicinal plant and is considered invasive on certain tropical islands. In traditional medicine, A. indicum is used as a aphrodisiac, demulcent, diuretic, laxative, pulmonary and sedative (leaves). The bark is astringent and diuretic; laxative, expectorant and demulcent (seeds); laxative and tonic, anti-inflammatory and anthelmintic (plant); analgesic (fixed oil); diuretic and for leprosy (roots). The plant is very much used in Siddha medicines. In fact, the bark, root, leaves, flowers and seeds are all used for medicinal purposes by Tamils. The leaves are also used to treat for pile complaints. The flowers are traditionally used to increase semen in men. The phytochemical analysis showed the Presence of Alkaloid, Saponins, Amino acid, Flavonoids, Glycosides and steroids. This plant exhibits several potential pharmacological activities. A review on the various studies on the plant has been provided for the purpose of understanding its medicinal properties.

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