Eco-conscious synthesis of novel 1,2,4-triazolo[1,5-a]pyrimidine derivatives as potent Anti-microbial agent and comparative study of cell viability and cytotoxicity in HEK-293 cell line utilizing Indian gooseberry (Phyllanthus emblica) fruit extract

Article

Author: Bhatt, Vaibhav D. ; Dixit, Bharat C. ; Bhatt, Bhaktiben R ; Pandey, Kamalkishor ; Bhatt, Vaibhav D ; Bhatt, Bhaktiben R. ; Dixit, Bharat C ; Patel, Tarosh ; Halpani, Chandani ; Modi, Anupama

Antimicrobial resistance (AMR) is a pressing global health challenge that necessitates the search for novel antimicrobial agents and synthetic methodologies. This study investigates the synthesis and antimicrobial efficacy of 25 novel 1,2,4-triazolo[1,5-a]pyrimidine derivatives, catalyzed by Amla (Phyllanthus emblica) fruit juice, which is rich in organic acids and polyphenolic compounds, thus serving as an environmentally sustainable catalyst, in adherence to green chemistry principles. The synthesis is achieved through a one-pot, solvent-free process that yields high quantities of the desired compounds in significantly less time compared to traditional methods. Comprehensive antimicrobial evaluation was conducted against a range of clinically relevant microorganisms, including Chromobacterium violaceum, Klebsiella pneumoniae, Escherichia coli, Staphylococcus aureus, Bacillus subtilis, Candida albicans, Cryptococcus neoformans and Aspergillus niger. Concurrently, cytotoxic assays were performed on HEK-293 cells, to assess safety profiles, revealing that compounds B-1, B-6, B-7, B-14 and B-15 exhibited potent antimicrobial activity while maintaining low cytotoxicity and high cell viability. These findings underscore the therapeutic potential of the synthesized compounds in combatting infectious diseases and addressing the challenges posed by AMR, highlighting the critical importance of dose optimization in therapeutic applications. This study combats contagious diseases, mitigates AMR challenges and contributes significantly to the field of antimicrobial drug discovery, emphasizing the need for sustainable synthetic strategies that align with future pharmaceutical endeavors. Our research not only advances the understanding of these novel compounds but also supports ongoing efforts to develop safe and effective therapies against resistant pathogens.

01 Jul 2024·Bioorganic Chemistry

Total Synthesis, structure revision and antifungal activity of palmarumycin B8 and B7

Article

Author: An, Xinkun ; Wang, Mingan ; Zhang, Tingting ; Xu, Leichuan ; Lai, Daowan ; Zhou, Ligang ; Ma, Haoyun

Palmarymycins B₈ (1), its regioisomer (2) and B₇ (3) were synthesized via 10-, 9-, and 11-steps in 6.5 %, 2.3 % and 0.54 % overall yields from chroman-4-one (4), 4-hydroxyindanone (12), and 2,5-dimethoxybenzaldehyde (20) as the starting materials, using benzyl protection, enol trimethylsilyl ether by TMSOTf, Rubottom oxidation and deprotection with hydrogenation under Pd/C catalyst as the key steps, respectively. Their structures were characterized by ¹H, ¹³C NMR, COSY, HSQC, HMBC and HR-ESI-MS spectral data. The structure of palmarumycin B₈ was revised from 1 to 2 based on the total synthesis, 2D NMR analysis and DFT calculation. The antifungal assay results indicated that palmarumycin B₈ (1) showed moderate inhibitory activity against Phytophthora capsica. Compounds 15 and 16 exhibited excellent in vitro antifungal activities against P. capsica with EC₅₀ values of 2.17 and 8.50 μg/mL, respectively.

01 May 2024·World Journal of Microbiology and Biotechnology

Advances in biotin biosynthesis and biotechnological production in microorganisms

Review

Author: Xiao, Feng ; Cheng, Dong-Yuan ; Guo, Feng-Zhu ; Zhao, Jia-Run ; Chen, Lu-Yi ; Xu, Zhi-Nan ; Bi, Ke ; Zuo, Si-Qi

Biotin, also known as vitamin H or B₇, acts as a crucial cofactor in the central metabolism processes of fatty acids, amino acids, and carbohydrates. Biotin has important applications in food additives, biomedicine, and other fields. While the ability to synthesize biotin de novo is confined to microorganisms and plants, humans and animals require substantial daily intake, primarily through dietary sources and intestinal microflora. Currently, chemical synthesis stands as the primary method for commercial biotin production, although microbial biotin production offers an environmentally sustainable alternative with promising prospects. This review presents a comprehensive overview of the pathways involved in de novo biotin synthesis in various species of microbes and insights into its regulatory and transport systems. Furthermore, diverse strategies are discussed to improve the biotin production here, including mutation breeding, rational metabolic engineering design, artificial genetic modification, and process optimization. The review also presents the potential strategies for addressing current challenges for industrial-scale bioproduction of biotin in the future. This review is very helpful for exploring efficient and sustainable strategies for large-scale biotin production.

100 Deals associated with B-007 (Basilea Pharmaceutica)

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Preclinical	CH	Basilea Pharmaceutica International Ltd.	-

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