Bioorganic and Medicinal Chemistry Letters This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

An ascidian Polycarpa aurata-derived pan-inhibitor against coronaviruses targeting M < sup > pro < /sup >
Bioorg Med Chem Lett. 2024 Mar 18:129706. doi: 10.1016/j.bmcl.2024.129706. Online ahead of print.ABSTRACTCoronaviruses (CoVs) are responsible for a wide range of illnesses in both animals and human. The main protease (Mpro) of CoVs is an attractive drug target, owing its critical and highly conserved role in viral replication. Here, we developed and refined an enzymatic technique to identify putative Mpro inhibitors from 189 marine chemicals and 46 terrestrial natural products. The IC50 values of Polycarpine (1a), a marine natural substance we studied and synthesized, are 30.0 ± 2.5 nM for SARS-CoV-2 Mpro and 0.12 ± 0.05...
Source: Bioorganic and Medicinal Chemistry Letters - March 20, 2024 Category: Chemistry Authors: Jing Zhang Lili Zhao Yuxin Bai Shanshan Li Meifang Zhang Bo Wei Xianyang Wang Yan Xue Li Li Guiliang Ma Yu Tang Xin Wang Source Type: research

Hydrazyl hydroxycoumarins as new potential conquerors towards Pseudomonas aeruginosa
Bioorg Med Chem Lett. 2024 Mar 15;103:129709. doi: 10.1016/j.bmcl.2024.129709. Online ahead of print.ABSTRACTA class of unique hydrazyl hydroxycoumarins (HHs) as novel structural scaffold was developed to combat dreadful bacterial infections. Some HHs could effectively suppress bacterial growth at low concentrations, especially, pyridyl HH 7 exhibited a good inhibition against Pseudomonas aeruginosa 27853 with a low MIC value of 0.5 μg/mL, which was 8-fold more active than norfloxacin. Furthermore, pyridyl HH 7 with low hemolytic activity and low cytotoxicity towards NCM460 cells showed much lower trend to induce the drug...
Source: Bioorganic and Medicinal Chemistry Letters - March 17, 2024 Category: Chemistry Authors: Jiang-Sheng Zhao Nisar Ahmad Shuo Li Cheng-He Zhou Source Type: research

Hydrazyl hydroxycoumarins as new potential conquerors towards Pseudomonas aeruginosa
Bioorg Med Chem Lett. 2024 Mar 15:129709. doi: 10.1016/j.bmcl.2024.129709. Online ahead of print.ABSTRACTA class of unique hydrazyl hydroxycoumarins (HHs) as novel structural scaffold was developed to combat dreadful bacterial infections. Some HHs could effectively suppress bacterial growth at low concentrations, especially, pyridyl HH 7 exhibited a good inhibition against Pseudomonas aeruginosa 27,853 with a low MIC value of 0.5 μg/mL, which was 8-fold more active than norfloxacin. Furthermore, pyridyl HH 7 with low hemolytic activity and low cytotoxicity towards NCM460 cells showed much lower trend to induce the drug-re...
Source: Bioorganic and Medicinal Chemistry Letters - March 17, 2024 Category: Chemistry Authors: Jiang-Sheng Zhao Nisar Ahmad Shuo Li Cheng-He Zhou Source Type: research

Synthesis, biological evaluation and molecular docking study of pyrimidine linked thiazolidinedione derivatives as potential antimicrobial and antitubercular agents
Bioorg Med Chem Lett. 2024 Mar 15;103:129707. doi: 10.1016/j.bmcl.2024.129707. Online ahead of print.ABSTRACTThe design and development of novel antimicrobial agents are highly desired to combat the emergence of medication resistance against microorganisms that cause infections. A series of new pyrimidine-linked thiazolidinedione derivatives (5a-j) were synthesized, characterized, and their antimicrobial properties assessed in the current investigation. Here, novel pyrimidine-linked thiazolidinedione compounds were designed using the molecular hybridization approach. Elemental and spectral techniques were used to determine...
Source: Bioorganic and Medicinal Chemistry Letters - March 16, 2024 Category: Chemistry Authors: M S Raghu C B Pradeep Kumar K Yogesh Kumar M K Prashanth Fahd Alharethy Byong-Hun Jeon Source Type: research

Synthesis, biological evaluation and molecular docking study of pyrimidine linked thiazolidinedione derivatives as potential antimicrobial and antitubercular agents
Bioorg Med Chem Lett. 2024 Mar 14:129707. doi: 10.1016/j.bmcl.2024.129707. Online ahead of print.ABSTRACTThe design and development of novel antimicrobial agents are highly desired to combat the emergence of medication resistance against microorganisms that cause infections. A series of new pyrimidine-linked thiazolidinedione derivatives (5a-j) were synthesized, characterized, and their antimicrobial properties assessed in the current investigation. Here, novel pyrimidine-linked thiazolidinedione compounds were designed using the molecular hybridization approach. Elemental and spectral techniques were used to determine the...
Source: Bioorganic and Medicinal Chemistry Letters - March 16, 2024 Category: Chemistry Authors: M S Raghu K C B Pradeep Kumar Yogesh Kumar M K Prashanth Fahd Alharethy Byong-Hun Jeon Source Type: research

C3-Symmetric ligands in drug design: An overview of the challenges and opportunities ahead
Bioorg Med Chem Lett. 2024 Mar 13:129702. doi: 10.1016/j.bmcl.2024.129702. Online ahead of print.ABSTRACTC3-symmetry is a type of star-shaped molecule consisting of a central core and three symmetrically attached chains. These molecules are used in drug discovery due to their unique three-fold rotational symmetry, which allows for specific binding interactions and improved molecular recognition. In this text, we provide an overview of synthetic approaches with C3-symmetry as a pharmaceutical tool: progress, challenges, and opportunities. C3-symmetric ligands offer both challenges and opportunities in drug design. Their uni...
Source: Bioorganic and Medicinal Chemistry Letters - March 15, 2024 Category: Chemistry Authors: Maha A Alshubramy Faez S Alotaibi Hamad M Alkahtani Khalid A Alamry Mahmoud A Hussein Source Type: research

Synthesis and biological evaluation of hydantoin derivatives as potent antiplasmodial agents
Bioorg Med Chem Lett. 2024 Mar 12:129701. doi: 10.1016/j.bmcl.2024.129701. Online ahead of print.ABSTRACTMalaria, a devastating disease, has claimed numerous lives and caused considerable suffering, with young children and pregnant women being the most severely affected group. However, the emergence of multidrug-resistant strains of Plasmodium and the adverse side effects associated with existing antimalarial drugs underscore the urgent need for the development of novel, well-tolerated, and more efficient drugs to combat this global health threat. To address these challenges, six new hydantoins derivatives were synthesized...
Source: Bioorganic and Medicinal Chemistry Letters - March 14, 2024 Category: Chemistry Authors: Ee-Zhen Chin Wei-Jin Chang Hui-Yin Tan Sook Yee Liew Yee-Ling Lau Yee-Ling Ng Mohd Azlan Nafiah Thomas Kurz Siow-Ping Tan Source Type: research

Novel ether derivatives of 11-azaartemisinins with high order antimalarial activity against multidrug-resistant Plasmodium yoelii in Swiss mice
This study investigates cutting-edge synthetic chemistry approaches for designing and producing innovative antimalarial drugs with improved efficacy and fewer adverse effects. Novel amino (-NH2) and hydroxy (-OH) functionalized 11-azaartemisinins 9, 12, and 14 were synthesized along with their derivatives 11a, 13a-e, and 15a-b through ART and were tested for their AMA (antimalarial activity) against Plasmodium yoelii via intramuscular (i.m.) and oral routes in Swiss mice. Ether derivative 13c was the most active compound by i.m. route, it has shown 100 % protection at the dose of 12 mg/kg × 4 days and showed 100 % clearan...
Source: Bioorganic and Medicinal Chemistry Letters - March 13, 2024 Category: Chemistry Authors: Komal Rathi Mohammad Hassam Chandan Singh Sunil K Puri Jawahar L Jat Ved Prakash Verma Source Type: research

Design, synthesis, α-amylase and glucose diffusion inhibition, and molecular docking studies of new indenopyrazolones bearing benzothiazole derivatives
Bioorg Med Chem Lett. 2024 Mar 5;103:129692. doi: 10.1016/j.bmcl.2024.129692. Online ahead of print.ABSTRACTAn eco-friendly facile synthesis of a series of twenty 1-(4/6-substitutedbenzo[d]thiazol-2-yl)-3-(phenyl/substitutedphenyl)indeno[1,2-c]pyrazol-4(1H)-ones 7a-t was achieved by the reaction of 2-(benzoyl/substitutedbenzoyl)-(1H)-indene-1,3(2H)-dione 3a-t and 2-hydrazinyl-4/6-substitutedbenzo[d]thiazole 6a-t in presence of freshly dried ethanol and glacial acetic acid under reflux conditions in good yields. The newly synthesized derivatives were well characterized using different physical and spectral techniques (FTIR,...
Source: Bioorganic and Medicinal Chemistry Letters - March 7, 2024 Category: Chemistry Authors: Ravinder Punia Satbir Mor Suchita Sindhu Deepak Kumar Priyanku Pradip Das Deepak Kumar Jindal Ashwani Kumar Rajni Mohil Komal Jakhar Source Type: research

Synthesis and biological evaluation of radioiodinated benzoxazole and benzothiazole derivatives for imaging myelin in multiple sclerosis
In conclusion, [123I]BO-2 demonstrated the fundamental characteristics of a myelin imaging probe for SPECT.PMID:38452827 | DOI:10.1016/j.bmcl.2024.129691 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - March 7, 2024 Category: Chemistry Authors: Hiroyuki Watanabe Miho Ikawa Masashi Kakae Hisashi Shirakawa Shuji Kaneko Masahiro Ono Source Type: research