Zala, Ajayrajsinh R Tiwari, Ramgopal Naik, Hem N Ahmad, Iqrar Patel, Harun Jauhari, Smita Kumari, Premlata
Published in
Molecular diversity
Novel pyrrolo[2,3-d]pyrimidine-based analogues were designed, synthesized, and evaluated for their ability to inhibit the α-amylase enzyme in order to treat diabetes. In vitro antidiabetic analysis demonstrated excellent antidiabetic action for compounds 5b, 6c, 7a, and 7b, with IC50 values in the 0.252-0.281 mM range. At a 200 μg/mL concentration,...
Rao, Priyashi Ninama, Jinal Dudhat, Mansi Goswami, Dweipayan Rawal, Rakesh M
Published in
Molecular diversity
Throughout history, vector-borne diseases have consistently posed significant challenges to human health. Among the strategies for vector control, chemical insecticides have seen widespread use since their inception. Nevertheless, their effectiveness is continually undermined by the steady growth of insecticide resistance within these vector popula...
Islam, Aminul Choudhury, Prasun Sarkar, Kaushik Das, Rajesh Kumar Bhattacharya, Malay Ghosh, Pranab
Published in
Molecular diversity
Here we demonstrated a solvent free, mechanochemical I2 catalyzed C(sp2)-H sulfenylation of enaminones under grinding condition. Only catalytic amount of I2 is required on silica surface without any external heating. The reaction time has reduced to a great extent in comparison to their solution based counterpart. The frictional energy created by b...
Dash, Rudra N Prabhudutta, Mamidi De, Saikat Swain, Ranjit P Moharana, Alok K Subudhi, Bharat B Chattopadhyay, Soma
Published in
Molecular diversity
Chikungunya virus infection has become a global health concern because of its high rates of morbidity and mortality in patients with preexisting conditions. Inflammation and arthritis are the major symptoms of CHIKV that persist even after clearance of CHIKV. To develop an antiviral that can reduce infection and manage inflammation independent of t...
Alananzeh, Waleed A Al-Qattan, Mohammed N Ayipo, Yusuf Oloruntoyin Mordi, Mohd N
Published in
Molecular diversity
Manipulating intracellular signals by interaction with transmembranal G-protein-coupled receptors (GPCRs) is the way of action of more than 30% of available medicines. Designing molecules against GPCRs is most challenging due to their flexible binding orthosteric and allosteric pockets, a property that lead to different mode and extent of activatio...
Venturi, Valentina Presini, Francesco Trapella, Claudio Bortolini, Olga Giovannini, Pier Paolo Lerin, Lindomar Alberto
Published in
Molecular diversity
Various geraniol esters act as insect pheromones and display pharmacological activities, especially as neuroprotective agents. Therefore, the search for synthetic strategies alternative to traditional chemical synthesis could help designing ecofriendly routes for the preparation of such bioactive compounds. Hence, this work aims at the microwave-as...
Olukunle, Oluwatoyin Folake Olowosoke, Christopher Busayo Khalid, Aqsa Oke, Grace Ayomide Omoboyede, Victor Umar, Haruna Isiyaku Ibrahim, Ochapa Adeboboye, Covenant Femi Iwaloye, Opeyemi Olawale, Femi
...
Published in
Molecular diversity
Various studies have established that molecules specific for MDMX inhibition or optimized for dual inhibition of p53-MDM2/MDMX interaction signaling are more suitable for activating the Tp53 gene in tumor cells. Nevertheless, there are sparse numbers of approved molecules to treat the health consequences brought by the lost p53 functions in tumor c...
Liu, Yu-Yang Yi, Yang-Jie Ye, Jiao Hu, Ai-Xi
Published in
Molecular diversity
A series of 4-methyl-5-(3-phenylacryloyl)thiazoles based on chalcones were designed, synthesized and evaluated for their influenza neuraminidase (NA) inhibitory activity in vitro. A preliminary structure-activity relationship (SAR) analysis showed that thiazoles bearing amide had greater potency. It also showed that mono-hydroxyl group at 4-positio...
Peytam, Fariba Norouzbahari, Maryam Saadattalab, Toktam Şanlıtürk, Gizem Firoozpour, Loghman Emamgholipour, Zahra Dogaheh, Mahtab Ghasemi Nikou, Mohammad Tehrani, Maliheh Barazandeh Bijanzadeh, Hamid Reza
...
Published in
Molecular diversity
Bacterial resistance to fluoroquinolone has been increasing at an alarming rate worldwide. In an attempt to find more potent anti-bacterial agents, an efficient, straightforward protocol was performed to obtain a large substrate scope of novel ciprofloxacin and sarafloxacin analogues conjugated with 4-(arylcarbamoyl)benzyl 7a-ab. All prepared compo...
Mili, Ajay Birangal, Sumit Nandakumar, Krishnadas Lobo, Richard
Published in
Molecular diversity
Drug-induced liver injury can be caused by any drugs, their metabolites, or natural products due to the inefficient functioning of drug-metabolizing enzymes, resulting in reactive oxygen species generation and leading to oxidative stress-induced cell death. For protection against oxidative stress, our cell has various defense mechanisms. One of the...
