Article
Chemistry, Applied
Zhiyun Peng, Guangcheng Wang, Qiao-Hui Zeng, Yufeng Li, Yi Wu, Haiquan Liu, Jing Jing Wang, Yong Zhao
Summary: A series of 1,2,4-triazole hydrazones were synthesized and evaluated for their inhibitory activities on tyrosinase. Compound 9 showed superior inhibitory activity, competitive-noncompetitive mixed inhibition mechanism, potent DPPH scavenging activity, and effective antibrowning effect on fresh-cut potatoes. It also displayed low cytotoxicity against human normal cell line, suggesting its potential as lead molecules for novel antibrowning agents in the food industry.
Article
Chemistry, Medicinal
Sin -Min Li, Jia-Yu Chou, Shuo-En Tsai, Ching-Chun Tseng, Cheng-Yen Chung, Wei-Zheng Zeng, Yu-Pei Hu, Naoto Uramaru, Guan-Jhong Huang, Fung-Fuh Wong
Summary: An efficient synthesis method was developed for furoxan/1,2,4-triazole hybrids 5a-k from methyl 5-(halomethyl)-1-aryl-1H-1,2,4-triazole-3-carboxylates 1 through two-steps reaction including hydrolyzation and esterification. The newly synthesized compounds were evaluated for their exogenous NO release ability, in vitro and in vivo anti-inflammatory activity, and in silico predictions. Compound 5f showed extraordinary COX-2 inhibition and selectivity, as well as better inhibition of cytokine and gastric safety compared to Indomethacin. Molecular modeling and in silico predictions identified compound 5f as a potential anti-inflammatory agent with comparable effects to Celecoxib.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Renata Paprocka, Przemyslaw Kolodziej, Malgorzata Wiese-Szadkowska, Anna Helmin-Basa, Anna Bogucka-Kocka
Summary: Parasitic diseases caused by intestinal helminths are a serious problem, but the study found that certain triazole derivatives may have anti-inflammatory and anthelmintic activity, making them promising drug candidates.
Article
Biochemistry & Molecular Biology
Mohamed T-E Maghraby, Tahani Mazyad Almutairi, Stefan Brase, Ola I. A. Salem, Bahaa G. M. Youssif, Mahmoud M. Sheha
Summary: A novel series of 1,2,3-triazole/1,2,4-triazole hybrids were designed and synthesized as antiproliferative agents targeting aromatase enzymes. Compounds 6a and 6b demonstrated the highest antiproliferative activity and aromatase inhibitory action, indicating their potential as anticancer candidates. Molecular docking investigations further supported these findings.
Article
Biochemistry & Molecular Biology
Ping Yang, Jia-Bao Luo, Zi-Zhou Wang, Li-Lei Zhang, Jin Feng, Xiao-Bao Xie, Qing-Shan Shi, Xin-Guo Zhang
Summary: A series of 1,2,4-triazole-norfloxacin hybrids were designed, synthesized, and evaluated for their in vitro antibacterial activity against common pathogens. The newly synthesized compounds showed superior antibacterial activity to norfloxacin, with high toxicity towards bacterial cells but good biocompatibility. Molecular docking analysis suggested strong affinity of the compounds for bacterial topoisomerase IV.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Suembuel Yildirim, Aslihan Ayvaz, Arif Mermer, Fatih Kocabas
Summary: Novel 1,2,4-triazole-containing compounds with anticancer and potent anti-CB1 activity were synthesized using green chemistry methods, microwave irradiation, and ultrasonication. These compounds showed anticancer activity against pancreatic, prostate, and breast cancer cells, with cytotoxicity to fibroblast cells. Compounds 5e and 5f exhibited similar structure, binding affinity, and poses to CB1 antagonists. Cell cycle analysis revealed that compounds 5e-g inhibited cancer cell growth primarily by arresting the cell cycle at S-phase. Overall, this study demonstrates the development of novel compounds with anticancer and potent anti-CB1 activity.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Biochemistry & Molecular Biology
Reem I. Al-Wabli, Mona A. Alsulami, Sarah I. Bukhari, Nadine M. S. Moubayed, Maha S. Al-Mutairi, Mohamed I. Attia
Summary: A series of new indole-triazole conjugates were designed and synthesized for evaluation as new antimicrobial candidates, showing good to moderate activity against most tested Gram-negative strains and potent activity against Candida tropicalis, with one compound exhibiting the strongest activity against Candida albicans.
Review
Biochemistry & Molecular Biology
Shima Nasri, Mohammad Bayat, Khudaidad Kochia
Summary: Compounds containing 1,2,4-triazole scaffolds play a crucial role in drug discovery, this review article summarizes their pharmacological significance and synthesis strategies, encouraging further research to discover new drug candidates.
MOLECULAR DIVERSITY
(2022)
Article
Chemistry, Physical
Kainat Ahmed, Maryam Bashir, Rehana Bano, Muhammad Sarfraz, Hidayat Ullah Khan, Shahnaz Khan, Ahsan Sharif, Amir Waseem, Mazhar Amjad Gilani, Komal Batool, Rabia Idrees, Abdul Rauf, Rahman Shah Zaib Saleem, Muhammad Arshad
Summary: In this study, a series of 1,2,4-triazine-based hydrazone scaffolds with impressive biological activities were synthesized using heteroaromatic aldehydes. The target compounds were characterized using spectroscopic techniques and showed excellent antioxidant capacities and cholinesterase inhibitory potentials. Density functional theory simulations complemented the experimental data and confirmed the stability and reactivity of the compounds. Molecular docking study indicated that the synthesized compounds have strong binding energy and affinity towards the active pocket of the target protein. These findings suggest that the synthesized compounds can potentially be developed as potent drugs for the treatment of Alzheimer's disease.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Agriculture, Multidisciplinary
Yan-En Wang, Dongchen Yang, Jingqian Huo, Lai Chen, Zhanhai Kang, Jianyou Mao, Jinlin Zhang
Summary: Compounds 5av and 5aw showed excellent herbicidal activity in vitro, with over 90% inhibition against tested weeds at concentrations as low as 100 mg/L. Furthermore, they exhibited higher postemergence herbicidal activity than positive controls in a greenhouse setting, while being safe for crops of maize and wheat. Fluorescent binding experiments and molecular docking analyses indicated strong TK inhibitory activity of 5av and 5aw, making them promising herbicide candidates for weed control in wheat and maize fields.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Yang Wang, Ruiqi Su, Jianwen Chen, Xuan Liu, Jingning Luo, Yaoqiang Lao, Ping Huang, Jinguo Shi, Caibao Jiang, Liping Liao, Jingxia Zhang
Summary: This study designed and synthesized a series of 1,3,5-triphenyl-1,2,4-triazole derivatives, and the optimal compound 9 was obtained by evaluating their antioxidant and anti-inflammatory effects. The neuroprotective effect of compound 9 was evaluated in a rat middle cerebral artery occlusion (MCAO) model, and the mechanisms were explored through Western blot. The results suggest that compound 9 may exert anti-AIS neuroprotection by inhibiting oxidative stress and neuroinflammation.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Fenghai Zhao, Xianjun Tang, Min Liu, Zhaohai Qin, Jia-Qi Li, Yumei Xiao
Summary: A series of compounds containing trifluoroacetyl groups were synthesized and evaluated for their insecticidal activity against Nilaparvata lugens and Aphis craccivora. The study found that compound 4-1, 4-2, and 4-19 showed the best activity against Nilaparvata lugens at 100 mg/L concentration. Structure-activity relationship of different substituents of R-1 or R-2 was investigated, and molecular docking of compounds 4-1 and 4-2 was discussed.
MOLECULAR DIVERSITY
(2022)
Article
Chemistry, Medicinal
Xin-Hui Zhang, Hui-Qin Kang, Yuan-Yuan Tao, Yi-Han Li, Jun-Ru Zhao, Ya-Gao, Li-Ying Ma, Hong-Min Liu
Summary: In this study, a series of 1,3-diaryl-1,2,4-triazole-capped HDAC6 inhibitors were designed, synthesized and verified, with compound 9r showing the best inhibitory activity with potential for gastric cancer therapy. The high selectivity and affinity of 9r to HDAC6, along with its ability to upregulate acetylated alpha-tubulin levels and exhibit antiproliferative and anti-metastatic effects without significant toxicity, suggest that 9r could serve as a lead compound for the development of novel therapeutic agents for gastric cancer.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Li Zhu, Si-Yu Tang, Dan-Ping Chen, Cheng-Peng Li, Li-Hui Shao, Gui-Ping Ouyang, Zhen-Chao Wang, Zhu-Rui Li
Summary: In this study, a series of novel indole 3-substituted-[1,2,4]triazole derivatives were designed and synthesized. The antibacterial activities of these compounds were evaluated and showed excellent bioactivity against Xanthomonas oryzae pv. oryzae (Xoo).
Article
Biochemistry & Molecular Biology
Bushra Khan, Abdullah Naiyer, Fareeda Athar, Shakir Ali, Sonu Chand Thakur
Summary: Through synthesis and evaluation, we found that the compound B6 among the 16 derivatives exhibited the highest radical scavenging and anti-inflammatory activities, showing important potential for pharmaceutical applications.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Chemistry, Organic
Nhlanhla Gracious Shabalala, Nontuthuko Pamela Hadebe, Nagaraju Kerru, Suresh Maddila, Werner E. van Zyl, Sreekantha B. Jonnalagadda
Summary: In this study, a highly efficient and catalyst-free green synthetic protocol was developed for the synthesis of two series of poly-functionalized pyran derivatives. The protocol showed excellent yields, simple workup, short reaction times, and high atom economy and carbon efficiency. The circumvention of chromatographic separations was also an advantage of this procedure.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Review
Chemistry, Organic
Hari Babu Bollikolla, S. N. Murthy Boddapati, Swetha Thangamani, Baby Ramana Mutchu, Mohammed Mujahid Alam, Mohamed Hussien, Sreekantha Babu Jonnalagadda
Summary: This review article presents various synthetic strategies for the preparation of benzotriazole and its derivatives, and provides a brief overview of their bio applications and pharmacological activity.
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Buri Apparao, Alice R. Robert, Muthyala Murali Krishna Kumar, Rama Krishna Madaka, Pamerla Muralidhar, Suresh Maddila, Sreekantha B. Jonnalagadda
Summary: This study describes a facile, eco-friendly, and efficient approach for the multicomponent synthesis of 2-amino-pyran analogues using rutheia-doped alumina as a heterogeneous catalyst. The key benefits of this protocol include operational simplicity, economy, green reaction conditions, and high product yields. Additionally, the catalyst material can be recycled and reused up to eight runs without any significant loss of catalytic activity.
RESEARCH ON CHEMICAL INTERMEDIATES
(2023)
Article
Chemistry, Multidisciplinary
Neha Kumari, Sudhakar Chintakula, Immandhi Sai Sonali Anantha, Suresh Maddila
Summary: In this study, a poly3-thenoic acid assisted P3TA/Fe doped TiO2 nano-hybrid was prepared via sol-gel approach for photocatalytic degradation of brilliant green (BG) dye. The results showed that 0.20 g of P3TA/Fe-TiO2 at pH 10 efficiently degraded 10 mg/L BG dye solution under visible light irradiation, and also exhibited antibacterial activity against E.coli and S.aureus.
RESULTS IN CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Komati Satish Kumar, Alice Rinky Robert, Nagaraju Kerru, Suresh Maddila
Summary: We have developed a facile and efficient method for synthesizing morpholino-linked 1,4-dihydropyridine derivatives. By combining morpholin-4-amine, diethyl acetylene dicarboxylate, malononitrile, and chosen substituted benzaldehydes under mild conditions in the presence of potassium carbonate as a catalyst, we achieved excellent yields (92-98%) with easy handling, simple workup, and shorter reaction time (<= 10 min), while avoiding the need for column chromatography for purification.
RESULTS IN CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Chittala Subrahmanyam, Battula Sreenivasa Rao, Badampudi Santosh Kumar, Suresh Maddila
Summary: An efficient and eco-friendly copper loaded hetero-poly-acid [Cu5(PW10V2O40)2] nano-catalystic complex was developed for the synthesis of poly substituted 1,4-dihydropyridines. The successful synthesis of the nanocomposite was confirmed through various techniques. This approach offers easy handling, commercial availability of starting materials, cost-effectiveness, short reaction times, high to excellent efficiencies, simple catalyst separation, recyclability, no purification of products, and safe and green solvent use.
INORGANIC CHEMISTRY COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Leela Prasad Kowtharapu, Naresh Kumar Katari, Christian A. Sandoval, Naresh Konduru, Siva Krishna Muchakayala, Surya Prakash Rao Pydimarry, Sreekantha Babu Jonnalagadda
Summary: This study evaluates the qualitative and quantitative formulas for nasal spray and ophthalmic solution formulations of olopatadine HCl using classical and instrumental techniques. The study accurately quantifies the reverse engineering of olopatadine HCl nasal spray and ophthalmic solution formulations using HPLC, osmometry, and titration techniques. The results show that the methods used are linear, accurate, precise, and specific, with good recovery rates and low relative standard deviations.
Review
Chemistry, Multidisciplinary
Neha Agarwal, Vijendra Singh Solanki, Brijesh Pare, Neetu Singh, Sreekantha B. Jonnalagadda
Summary: Present times face various environmental, atmosphere, and energy-related issues. Efficient catalysts and eco-friendly materials are capable of solving these problems effectively. The development of nano-based advanced catalysis has created new opportunities, as nanocatalysts with their small size and larger surface area offer superior interfaces and expanded functionality, attracting global attention. Extensive research on nanomaterials' size and properties has shifted the paradigm towards using materials with superior activity and selectivity as catalysts. Affordable and eco-friendly nanocatalysis is becoming increasingly popular, hence the need to understand their remarkable properties and applications. This review focuses on explicit properties of nanocatalysts due to their size, structure, and their applications in reducing environmental issues.
CURRENT OPINION IN GREEN AND SUSTAINABLE CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Challa Madhavi, Suresh Maddila, Palakondu Lavanya, Sreekantha B. Jonnalagadda
Summary: A mesoporous CeO2 doped HAp nanocomposite was synthesized and its catalytic potential in the facile synthesis of 1,4-dioxo-1,4-dihydronaphthalen-2-yl-1,4-dihydropyridine analogues was investigated. Characterization of the nanocomposite was carried out using various techniques. The synthetic route offered a broad substrate scope, mild reaction conditions, excellent yields, use of non-toxic solvents, and no need for column chromatography. The nanocomposite showed good recyclability with no significant loss in its catalytic activity after seven runs.
INORGANIC CHEMISTRY COMMUNICATIONS
(2023)
Article
Chemistry, Multidisciplinary
Kotyada Suryanarayana, Kranthi Kumar Gangu, Nagaraju Kerru, Kavita Khatana, Botcha Satyanarayana, Suresh Maddila
Summary: A series of quinoline-linked rhodanine-bearing 1,2,3-triazole analogs were designed and synthesized. The novel hybrids were characterized by spectroscopic analysis. Compound 10c showed higher anticancer activity than Combretastatin-A4, with IC50 values of 3.67, 3.93, 4.92, and 6.83 μM against MCF7, Caco-2, HeLa, HT-29, and Caco-2 cancer cells, respectively. This study reveals the potential of quinoline-linked rhodanine-bearing 1,2,3-triazole scaffolds as antitumor agents.
JOURNAL OF THE IRANIAN CHEMICAL SOCIETY
(2023)
Review
Chemistry, Physical
Thirupathi Damera, Ramakanth Pagadala, Surjyakanta Rana, Sreekantha Babu Jonnalagadda
Summary: Microwave energy has been fascinated as an alternative technique for the construction of heterocycles, with heterogeneous catalysts providing advantages in terms of recycling, catalyst preparation, and product yields. The usage of microwave energy has rapidly increased in various fields such as organic synthesis, peptide synthesis, polymer chemistry, material sciences, nanotechnology, and biological processes. This article covers the applications of microwave-assisted heterogeneous catalytic reactions in the construction of chromenes, pyridines, pyrroles, triazoles, pyrazoles, tetrazoles, trans and cis julolidines.
Article
Chemistry, Multidisciplinary
Panasa Mahesh, Parameswari Akshinthala, Naresh Kumar Katari, Lavleen Kumar Gupta, Dikshita Panwar, Manoj Kumar Sharma, Sreekantha Babu Jonnalagadda, Rambabu Gundla
Summary: In this study, two new series of 3,5-dimethyl-1H-pyrazole-4-sulfonamide and 1,3,5-trimethyl-1H-pyrazole-4-sulfonamide derivatives were designed and synthesized. These derivatives were characterized by various analytical techniques and their biological evaluation data were presented, paving the way for the development of new pyrazole-4-sulfonamide derivatives.
Article
Chemistry, Multidisciplinary
Neha Kumari, Sudhakar Chintakula, Immandhi Sai Sonali Anantha, Suresh Maddila
Summary: Indigo carmine is used in medical diagnostics, as a textile colouring agent, and as a component in pharmaceutical tablets and capsules. Photo catalysis using poly-3-thenoicacid/Ni-TiO2 nanohybrids shows effective degradation of dye pollutants and antibacterial activity against Staphylococcus aureus and Escherichia coli.
RESULTS IN CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Ganeshbabu Bathula, Surjyakanta Rana, Siddaramagoud Bandalla, Vijaykumar Dosarapu, Satyanarayana Mavurapu, V. V. Aswathi Rajeevan, Bhaskar Sharma, Sreekantha B. Jonnalagadda, Mallesham Baithy, Chandra Shekar Vasam
Summary: This study demonstrates the high efficacy of WOx-promoted CeO2-SiO2 and CeO2-ZrO2 mixed oxide catalysts in the selective oxidation of benzyl alcohol to benzaldehyde. The WOx/CeO2-SiO2 catalyst, characterized by improved physicochemical properties and a higher number of oxygen vacancies, exhibited superior conversion and selectivity compared to other catalysts. Additionally, this catalyst showed excellent recyclability without significant activity loss.
