Article
Biochemistry & Molecular Biology
Mohamed H. Hekal, Paula S. Farag, Magdy M. Hemdan, Wael M. El-Sayed
Summary: This study synthesized a series of N-(1,3,4-thiadiazol-2yl)furan-2-carboxamide derivatives and found higher yields and rates under microwave conditions compared to traditional methods. The antiproliferative activities of these compounds were assessed, showing promising results against three cancer cell lines and VEGFR-2 as a potential molecular target. Some compounds exhibited significant antiproliferative activity, with Compound 7 identified as the best inhibitor of VEGFR-2.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Asiya Ramzan, Sajad Ahmad Padder, Khalid Z. Masoodi, Syed Shafi, Inayatullah Tahir, Reiaz Ul Rehman, Rajendra Prasad, Abdul Haseeb Shah
Summary: This study examined the antifungal potential of chemically synthesized beta-Nitrostyrene derivatives and found that they have strong inhibitory effects on pathogenic fungi and are effective against drug-resistant strains. Furthermore, the derivatives were found to impact cell wall morphology, enhance ROS generation, and modulate drug efflux.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
M. Shaheer Malik, Reem I. Alsantali, Qazi Mohammad Sajid Jamal, Zaki S. Seddigi, Moataz Morad, Meshari A. Alsharif, Essam M. Hussein, Rabab S. Jassas, Munirah M. Al-Rooqi, Zainularifeen Abduljaleel, Ahmed O. Babalgith, Hatem M. Altass, Ziad Moussa, Saleh A. Ahmed
Summary: An efficient atom-economical protocol for the synthesis of new imidazole-based N-phenylbenzamide derivatives was described, providing a series of compounds with high yields in a short reaction time. Cytotoxic evaluation showed that derivatives 4e and 4f exhibited good anticancer activity, with computational studies revealing their higher affinity towards target receptor proteins and stable complex formations. The ADME and drug-likeness of the derivatives reinforced their potential for further development as anticancer agents.
FRONTIERS IN CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Siddappa A. Patil, Shivaputra A. Patil, Ever A. Ble-Gonzalez, Stephen R. Isbel, Sydney M. Hampton, Alejandro Bugarin
Summary: This review discusses various carbazole derivatives and their antimicrobial activity, providing valuable references for medicinal chemists in their search for new approaches to combat microbial infections, which are a leading cause of death worldwide.
Article
Chemistry, Medicinal
Lige Liu, Hu Wu, Yan Long, Xinlong Yang, Chuanbiao Du, Yajie Xu, Qinggang Ji
Summary: A series of spiro[pyrrolidine-2,3'-quinoline]-2'-one derivatives were designed and synthesized for the discovery of novel antifungal drugs. These compounds showed inhibitory effects against chitin synthase, excellent antifungal activity, and potency against drug-resistant fungal variants.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Deblina Roy, Mohammad Anas, Ashan Manhas, Satyen Saha, Niti Kumar, Gautam Panda
Summary: In this study, a series of quinoline-imidazole hybrid compounds were synthesized and evaluated for their blood-stage antimalarial activity against Plasmodium falciparum. The results showed that one of the compounds exhibited significant antimalarial efficacy with low cytotoxicity and high selectivity. Furthermore, the study revealed the influence of substituents on the quinoline ring and the role of stereochemistry in the inhibitory activity.
BIOORGANIC CHEMISTRY
(2022)
Article
Microbiology
Benas Balandis, Povilas Kavaliauskas, Birute Grybaite, Vidmantas Petraitis, Ruta Petraitiene, Ethan Naing, Andrew Garcia, Ramune Grigaleviciute, Vytautas Mickevicius
Summary: Researchers have designed and synthesized benzenesulfonamide-bearing functionalized imidazole or S-alkylated derivatives and evaluated their antimicrobial activity against drug-resistant Mycobacterium abscessus strains. The compounds showed strong antimicrobial activity and could be potential candidates for further research.
Article
Agriculture, Multidisciplinary
Dongguo Xia, Xiang Cheng, Xiaohang Liu, Chengqi Zhang, Yunxiao Wang, Qiaoyun Liu, Qi Zeng, Niqian Huang, Yao Cheng, Xianhai Lv
Summary: Novel pyrazole carboxylate derivatives containing a flexible thiazole backbone were successfully synthesized and evaluated for their antifungal bioactivities. Compound 24 showed excellent bioactivities against Botrytis cinerea and Sclerotinia sclerotiorum, while compound 15 exhibited remarkable antifungal activity against Valsa mali. Compounds 3, 15, and 24 are promising antifungal candidates worthy of further fungicide development.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Deweshri Nandurkar, Sunil Menghani, Kishor Danao, Vijayshri Rokde, Nilesh Rarokar, Pramod Khedekar, Supriya Mana
Summary: A series of compounds were synthesized and characterized, showing significant antimicrobial properties against various pathogenic bacteria and fungi. Some compounds exhibited remarkable activity against Gram-negative and Gram-positive bacteria. Moderate to outstanding antibacterial activity was observed against E. coli, P. aeruginosa, S. aureus, and B. subtilis. Moderate to excellent antifungal activity was observed against Candida tropicalis and Candida glabrata. Compounds 25 and 34 showed the highest activity against both Gram-positive and Gram-negative bacteria. Compound 35 exhibited comparable antifungal activity to the standard drug. Molecular docking and QSAR analysis suggested that these compounds could be further explored as potential antimicrobial drugs.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Chemistry, Medicinal
Yun-Peng Xie, Nagarajan Sangaraiah, Jiang-Ping Meng, Cheng-He Zhou
Summary: Novel carbazole-oxadiazoles were developed as potential antibacterial agents and showed predominant inhibitory effects on both Gram-positive and -negative bacteria, especially in impeding the growth of MRSA and Pseudomonas aeruginosa ATCC 27853. The compounds exhibited low cytotoxicity and low tendency to develop resistance, and could disintegrate bacterial cell membranes to exert excellent antibacterial effects.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Physical
Mohamed H. A. Soliman, Sahar S. El-Sakka, Asmaa S. Fathy, Rasha M. Kamel
Summary: A new class of 5-aryl-3-((E)-3-phenylallylidene)-2(3H)-furanones (3a-f) derivatives was synthesized and characterized. The absorption and emission spectra of the compounds were studied in ten solvents with different polarities. The emission spectra showed a consistent shape with a significant red shift as solvent polarity increased. The quantum yield decreased over 20-fold from toluene to water due to the formation of hydrogen bonds with protic solvents.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Agriculture, Multidisciplinary
Dai-Chuan Huang, Zhuo He, Dale Guo, Fang Deng, Qiang Bian, Haifeng Zhang, Abdallah S. Ali, Ming-Zhi Zhang, Wei-Hua Zhang, Yu-Cheng Gu
Summary: Streptochlorin, an indole alkaloid derived from marine microorganisms, showed potent bioactivity against phytopathogenic fungi. A series of benzoxaborole-containing streptochlorin derivatives were synthesized and exhibited significant antifungal activities, especially compounds 4i and 5f, which showed impressive effects against Gibberella zeae and Rhizoctorzia solani.
JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Fang Yan Guo, Chang Ji Zheng, Meiyuan Wang, Jiangping Ai, Lan Ying Han, Liu Yang, Ye Fang Lu, Yu Xuan Yang, Ming Guan Piao, Hu-Ri Piao, Chun-Mei Jin, Cheng Hua Jin
Summary: Three series of new imidazole-fused imidazo[2,1-b][1,3,4]thiadiazole analogues have been synthesized and evaluated for their antibacterial and antifungal activities. One of the compounds showed strong antifungal activity with high selectivity for Candida albicans. This compound exhibited significantly higher activity against C. albicans compared to the positive control compounds.
Article
Chemistry, Medicinal
Jing-Rui Liu, Jia-Mu Liu, Ya Gao, Zhan Shi, Ke-Rui Nie, Dale Guo, Fang Deng, Hai-Feng Zhang, Abdallah S. Ali, Ming-Zhi Zhang, Wei-Hua Zhang, Yu-Cheng Gu
Summary: In this study, a series of compounds were designed and synthesized based on the combination strategy of pimprinine and streptochlorin. The evaluation of their antifungal activity showed that compounds 4a and 5a displayed excellent effects against two common phytopathogenic fungi. SAR analysis revealed the relationship between the 5-(3'-indolyl)oxazole scaffold and antifungal activity. Molecular docking models provided insight into the mode of action for compound 4a. These results highlight the potential of compounds 4a and 5a as novel antifungal agents.
Article
Chemistry, Physical
Ghazaleh Zarrinzadeh, Mahmood Tajbakhsh, Rahman Hosseinzadeh, Zahra Ghanbarimasir, Maryam Roudbary, Mojtaba Mohseni, Hamid Nadri
Summary: Euparin and 2-hydroxy acetophenone hydrazone derivatives (2-7) were synthesized and characterized. Their inhibitory potential on AchE enzyme was determined using a modified spectrophotometric approach. Compounds 3, 5, and 7 showed strong and specific inhibition of AchE. Docking tests confirmed the interactions between these compounds and AchE. Compound 7 exhibited the highest AchE inhibitory activity and docking score compared to the reference drug, Donepezil.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Multidisciplinary
Thibault Viennet, Aldino Viegas, Arne Kuepper, Sabine Arens, Vladimir Gelev, Ognyan Petrov, Tom N. Grossmann, Henrike Heise, Manuel Etzkorn
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
(2016)
Article
Chemistry, Medicinal
Mariana S. Gerova, Silviya R. Stateva, Elena M. Radonova, Rositsa B. Kalenderska, Rusi I. Rusew, Rositsa P. Nikolova, Christo D. Chanev, Boris L. Shivachev, Margarita D. Apostolova, Ognyan I. Petrov
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Organic
Desislava V. Stanisheva, Mariana S. Gerova, Ognyan I. Petrov
HETEROCYCLIC COMMUNICATIONS
(2017)
Article
Chemistry, Inorganic & Nuclear
Mariana S. Gerova, Filip E. Svetoslavov, Boris L. Shivachev, Rositsa P. Nikolova, Ognyan I. Petrov
PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
(2017)
Article
Biochemistry & Molecular Biology
D. Cheshmedzhieva, N. Toshev, M. Gerova, O. Petrov, T. Dudev
JOURNAL OF MOLECULAR MODELING
(2018)
Article
Biochemical Research Methods
Andras Boeszoermenyi, Sandeep Chhabra, Abhinav Dubey, Denitsa L. Radeva, Nikola T. Burdzhiev, Christo D. Chanev, Ognyan I. Petrov, Vladimir M. Gelev, Meng Zhang, Clemens Anklin, Helena Kovacs, Gerhard Wagner, Ilya Kuprov, Koh Takeuchi, Haribabu Arthanari
Article
Chemistry, Medicinal
Ognyan Ivanov Petrov, Yordanka Borisova Ivanova, Mariana Stefanova Gerova, Georgi Tsvetanov Momekov
LETTERS IN DRUG DESIGN & DISCOVERY
(2020)
Article
Chemistry, Medicinal
Gjorgji Atanasov, Rusi I. Rusew, Vladimir M. Gelev, Christo D. Chanev, Rosica Nikolova, Boris L. Shivachev, Ognyan I. Petrov, Margarita D. Apostolova
Summary: In this study, a series of 26 new styryl-2(3H)-benzothiazolone analogs of combretastatin-A4 (CA-4) were synthesized, characterized, and tested for their biological activities. Compound 26Z showed the most potent cytotoxic activity against EA.hy926 cells and demonstrated anti-vasculogenic effects. Furthermore, 26Z exhibited anti-proliferative activity in CA-4 resistant cells and induced G2/M arrest and mitotic spindle multipolarity, suggesting its potential as a new chemotherapeutic agent with further investigation needed.
Article
Chemistry, Organic
Yordanka Ivanova, Antonya Todorova, Christo Chanev, Ognyan Petrov
Meeting Abstract
Oncology
G. Atanasov, S. Stateva, M. Gerova, O. Petrov, M. Apostolova
EUROPEAN JOURNAL OF CANCER
(2018)
Article
Chemistry, Multidisciplinary
M. S. Gerova, E. A. Aleksandrova, Y. B. Ivanova, D. V. Stanisheva, G. Ts. Momekov, O. I. Petrov
BULGARIAN CHEMICAL COMMUNICATIONS
(2017)
Article
Chemistry, Organic
Yordanka Ivanova, Mariana Gerova, Christo Chanev, Ognyan Petrov
Article
Chemistry, Organic
Mariana S. Gerova, Yordanka B. Ivanova, Christo D. Chanev, Ognyan I. Petrov
