Browsing by Author "Haque, M. Akiful"

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A rapid and large volume synthesis of mono-, di-, tri-, and tetra-substituted imidazole derivatives via ultrasonic radiation-driven technique
(Scopus, 2024-01-12) Shaikh, Mohd Sayeed; Kale, Mayura A.; Zehravi, Mehrukh; Unnisa, Aziz; Haque, M. Akiful; Kumar, Kusuma Praveen; Khan, Sharuk L.; Siddiqui, Syed Sarfaraz Ali Falak A.; Khandaker, Mayeen Uddin
Sonochemistry under controlled conditions has proven effective in medicinal chemistry and drug development. It can substantially shorten reaction timelines from days or hours to minutes. A convenient one-pot synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives catalyzed by PTSA and benzenesulfonic acid in ethanol as solvent, under ultrasonic irradiation and without ultrasound irradiation at 50° C has been achieved successfully. These 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives synthesis were also accomplished using different solvents viz., Methanol, Ethanol, DCM, DMF, Acetonitrile and THF and PTSA as the catalyst. This method yielded the highest % synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with PTSA as the catalyst in solvent ethanol. These reactions were also optimized for % of PTSA catalyst required to obtain the maximum yield of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with and without ultrasound irradiation at 50° C. Synthesis of 2,4,5-trisubstituted Imidazole derivatives reaction follows first-order rate kinetics while that of 1,2,4,5-tetrasubstituted Imidazole derivatives reaction follows the second-order rate kinetics. Furthermore, sonochemistry has higher yields, lower cost, easier workups, and higher purity than conventional thermal organic synthesis, which has lower yields, tedious workups, longer reaction periods, lower purity, and numerous byproducts.
A Rapid and Large Volume Synthesis of Mono-, Di-, Tri-, and Tetra-Substituted Imidazole Derivatives via Ultrasonic Radiation-Driven Technique
(Taylor & Francis Group, 2024-01-12) Shaikh, Mohd Sayeed; Kale, Mayura A.; Zehravi, Mehrukh; Unnisa, Aziz; Haque, M. Akiful; Kumar, Kusuma Praveen; Khan, Sharuk L.; Ali, Syed Sarfaraz; Siddiqui, Falak A.; Emran, Talha Bin; Elrahim, Elrashed Abd; Khandaker, Mayeen Uddin
Sonochemistry under controlled conditions has proven effective in medicinal chemistry and drug development. It can substantially shorten reaction timelines from days or hours to minutes. A convenient one-pot synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives catalyzed by PTSA and benzenesulfonic acid in ethanol as solvent, under ultrasonic irradiation and without ultrasound irradiation at 50° C has been achieved successfully. These 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives synthesis were also accomplished using different solvents viz., Methanol, Ethanol, DCM, DMF, Acetonitrile and THF and PTSA as the catalyst. This method yielded the highest % synthesis of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with PTSA as the catalyst in solvent ethanol. These reactions were also optimized for % of PTSA catalyst required to obtain the maximum yield of 2,4,5-trisubstituted and 1,2,4,5-tetrasubstituted imidazole derivatives with and without ultrasound irradiation at 50° C. Synthesis of 2,4,5-trisubstituted Imidazole derivatives reaction follows first-order rate kinetics while that of 1,2,4,5-tetrasubstituted Imidazole derivatives reaction follows the second-order rate kinetics. Furthermore, sonochemistry has higher yields, lower cost, easier workups, and higher purity than conventional thermal organic synthesis, which has lower yields, tedious workups, longer reaction periods, lower purity, and numerous byproducts.
A Renewed Concept on Diabetic Retinopathy: Polyphenols as a Choice of Solution
(Biointerface research, 2021-04-07) Emran, Talha Bin; Haque, M. Akiful; Guntaka, Purnachandra Reddy; Singh, Laliteshwar Pratap; Khan, Mohd. Washid; Unnisa, Aziz; Nafady, Mohammed H.; Kazi, Aasim A.; Doukani, Koula; Nainu, Firzan
Diabetic retinopathy (DR) is the widespread microvascular consequence of diabetes mellitus and the most common effect of blindness in people with diabetes. Existing drugs are only effective in advanced stages of DR, and long-term efficacy and safety results for these treatments have yet to be clarified in multiple clinical trials. Furthermore, a more trustworthy and effective medication that may be deemed more advantageous in managing DR is unavoidable. Polyphenols, which are plant-derived chemical compounds, may be helpful in the initial stages of DR treatment. Compounds rich in polyphenols have been shown to slow the progression of long-term consequences of diabetes, for example, heart disease, nerve damage, kidney damage, and retinopathy. Polyphenols could be used instead of traditional treatments to halt the disease's progression. It has been proposed that in vitro investigations on the effects of polyphenols on ocular vision physiology and antioxidant protection have a substantial bearing on this assertion. Among the benefits of polyphenols are scavenging the free radicals, lowering the production of advanced glycation end products, inhibiting aldose reductase, anti- inflammatory activity, and affecting ocular blood flow. The present review discussed the significance of polyphenols in preclinical and clinical research of DR-affected cellular and molecular pathways.
Fighting Antibiotic Resistance: New Pyrimidine-Clubbed Benzimidazole Derivatives as Potential DHFR Inhibitors
(MDPI Publications, 2023-01-04) Haque, M. Akiful; Marathakam, Akash; Rana, Ritesh; Almehmadi, Samar J.; Tambe, Vishal B.; Charde, Manoj S.; Islam, Fahadul; Siddiqui, Falak A.; Culletta, Giulia; Almerico, Anna Maria; Tutone, Marco; Khan, Sharuk L.
The present work describes the design and development of seventeen pyrimidine-clubbed benzimidazole derivatives as potential dihydrofolate reductase (DHFR) inhibitors. These compounds were filtered by using ADMET, drug-likeness characteristics calculations, and molecular docking experiments. Compounds 27, 29, 30, 33, 37, 38, and 41 were chosen for the synthesis based on the results of the in silico screening. Each of the synthesized compounds was tested for its in vitro antibacterial and antifungal activities using a variety of strains. All the compounds showed antibacterial properties against Gram-positive bacteria (Staphylococcus aureus and Staphylococcus pyogenes) as well as Gram-negative bacteria (Escherichia coli and Pseudomonas aeruginosa). Most of the compounds either had a higher potency than chloramphenicol or an equivalent potency to ciprofloxacin. Compounds 29 and 33 were effective against all the bacterial and fungal strains. Finally, the 1,2,3,4-tetrahydropyrimidine-2-thiol derivatives with a 6-chloro-2-(chloromethyl)-1H-benzo[d]imidazole moiety are potent enough to be considered a promising lead for the discovery of an effective antibacterial agent.
Flavonoids as Potential Therapeutics Against Neurodegenerative Disorders
(Springer Nature, 2024-08-15) Faysal, Md.; Dehbia, Zerrouki; Zehravi, Mehrukh; Sweilam, Sherouk Hussein; Haque, M. Akiful; Kumar, Kusuma Praveen; Chakole, Rita D.; Shelke, Satish P.; Sirikonda, Swapna; Nafady, Mohamed H.; Khan, Sharuk L.; Nainu, Firzan; Ahmad, Irfan; Emran, Talha Bin
Neurodegeneration, the decline of nerve cells in the brain, is a common feature of neurodegenerative disorders (NDDs). Oxidative stress, a key factor in NDDs such as Alzheimer’s disease, Parkinson’s disease, amyotrophic lateral sclerosis, and Huntington’s disease can lead to neuronal cell death, mitochondria impairment, excitotoxicity, and Ca2+ stress. Environmental factors compromising stress response lead to cell damage, necessitating novel therapeutics for preventing or treating brain disorders in older individuals and an aging population. Synthetic medications offer symptomatic benefits but can have adverse effects. This research explores the potential of flavonoids derived from plants in treating NDDs. Flavonoids compounds, have been studied for their potential to enter the brain and treat NDDs. These compounds have diverse biological effects and are currently being explored for their potential in the treatment of central nervous system disorders. Flavonoids have various beneficial effects, including antiviral, anti-allergic, antiplatelet, anti-inflammatory, anti-tumor, anti-apoptotic, and antioxidant properties. Their potential to alleviate symptoms of NDDs is significant.
Synergistic Effects of Carotenoids: Therapeutic Benefits on Human Health
(Elsevier, 2024-01-20) Islam, Fahadul; Khan, Jishan; Zehravi, Mehrukh; Das, Rajib; Haque, M. Akiful; Banu, Ahmedi; Parwaiz, Shaikh; Nainu, Firzan; Nafady, Mohamed H.; Shahriar, S. M. Shatil; Hossain, Md. Jamal; Muzammil, Khursheed; Emran, Talha Bin
Carotenoids are naturally occurring compounds that are abundant and possess synergistic properties, contributing to their potential health benefits. This review provides an analysis of synergistic relationships among carotenoid compounds. The concept of synergy is of utmost importance due to the ongoing emphasis on consumer safety issues related to botanical natural products. To date, there is a lack of scientific reports specifically investigating the experimental evidence of synergistic effects associated with carotenoids. The carotenoid compounds purported to exhibit synergistic actions have demonstrated significant efficacy in combating oxidation, neurological diseases, peptic ulcers, tumors, and various other ailments. Furthermore, there have been reports of cancer prevention through apoptosis and the presence of antimicrobial, anti-inflammatory, and estrogenic properties. In addition to the observed combined benefits of carotenoids, this review elucidates the various health advantages associated with carotenoids. Among carotenoids, a substantial amount of data has been reported concerning lycopene. This review also examined the clinical status of the concurrent utilization of carotenoids with other bioactive molecules. As mentioned above, the findings offer valuable insights into the potential advantages of carotenoid compounds when combined, thereby presenting a promising avenue for further investigation in future research activities.
Synergistic effects of carotenoids: Therapeutic benefits on human health
(Scopus, 2024-01) Islam, Fahadul; Khan, Jishan; Zehravi, Mehrukh; Das, Rajib; Haque, M. Akiful; Banu, Ahmedi; Parwaiz, Shaikh; Nainu, Firzan; Nafady, Mohamed H.; Muzammil, Khursheed; Emran, Talha Bin
Carotenoids are naturally occurring compounds that are abundant and possess synergistic properties, contributing to their potential health benefits. This review provides an analysis of synergistic relationships among carotenoid compounds. The concept of synergy is of utmost importance due to the ongoing emphasis on consumer safety issues related to botanical natural products. To date, there is a lack of scientific reports specifically investigating the experimental evidence of synergistic effects associated with carotenoids. The carotenoid compounds purported to exhibit synergistic actions have demonstrated significant efficacy in combating oxidation, neurological diseases, peptic ulcers, tumors, and various other ailments. Furthermore, there have been reports of cancer prevention through apoptosis and the presence of antimicrobial, anti-inflammatory, and estrogenic properties. In addition to the observed combined benefits of carotenoids, this review elucidates the various health advantages associated with carotenoids. Among carotenoids, a substantial amount of data has been reported concerning lycopene. This review also examined the clinical status of the concurrent utilization of carotenoids with other bioactive molecules. As mentioned above, the findings offer valuable insights into the potential advantages of carotenoid compounds when combined, thereby presenting a promising avenue for further investigation in future research activities.