18 Works

Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents

Mohammad M. Al-Sanea, Abdelrahman Hamdi, Simone Brogi, Samar S. Tawfik, Dina I. A. Othman, Mahmoud Elshal, Hidayat Ur Rahman, Della G. T. Parambi, Rehab M. Elbargisy, Samy Selim, Ehab M. Mostafa & Ahmed A. B. Mohamed
A novel series of 12 antipyrine derivatives containing 1,3,4-oxadiazoles (4a-d), 1,3,4-thiadiazoles (6a-d), and pyrimidines (8a-d), was preparedand assessed for its potential in vitro COX-2 inhibitors. Compared to Celecoxib, compounds 4b-d and 8d were the most potent derivatives c with a half-maximal inhibitory concentration range of 53–69 nM. Considering COX-2 selectivity index, compounds 4 b and 4c were chosen among these most potent derivatives for further investigation. The in vivo ability of compounds 4 b and...

Design, synthesis and cytotoxic evaluation of novel bis-thiazole derivatives as preferential Pim1 kinase inhibitors with in vivo and in silico study

Mohammad M. Al-Sanea, Tamer M. Nasr, Samir Bondock, Aya Y. Gawish & Nada M. Mohamed
Bis-thiazole derivatives were synthesised conforming to the Pim1 pharmacophore model following Hantzsch condensation. Pim1 has a major role in regulating the G1/S phase which upon inhibition the cell cycle stops at its early stages. Derivatives 3b and 8b showed the best Pim1 IC50 0.32 and 0.24 µM, respectively relative to staurosporine IC50 0.36 µM. Further confirmation of 3b and 8b Pim1 inhibition was implemented by hindering the T47D cell cycle at G0/G1 and S phases...

Antibiotic resistance in Gram-negative Bacteria Causing Blood stream infections

Altaf Bandy & Abdulrahman Hamdan Almaeen
Background: The pathogenic spectrum of blood stream infections (BSIs) varies across regions. Monitoring the pathogenic profile and antimicrobial resistance is a prerequisite for effective therapy and infection control. The study analyzed the pathogenic spectrum of blood cultures with special focus on the resistance pattern of A.baumannii, E.coli and K. pneumoniae from a referral hospital of Saudi Arabia.

New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and in silico study

Mohammad M. Al-Sanea, Abdelrahman Hamdi, Ahmed A. B. Mohamed, Hamed W. El-Shafey, Mahmoud Moustafa, Abdullah A. Elgazar, Wagdy M. Eldehna, Hidayat Ur Rahman, Della G. T. Parambi, Rehab M. Elbargisy, Samy Selim, Syed Nasir Abbas Bukhari, Omnia Magdy Hendawy & Samar S. Tawfik
A new series of 2-aminobenzothiazole hybrids linked to thiazolidine-2,4-dione 4a–e, 1,3,4-thiadiazole aryl urea 6a–d, and cyanothiouracil moieties 8a–d was synthesised. The in vitro antitumor effect of the new hybrids was assessed against three cancer cell lines, namely, HCT-116, HEPG-2, and MCF-7 using Sorafenib (SOR) as a standard drug. Among the tested compounds, 4a was the most potent showing IC50 of 5.61, 7.92, and 3.84 µM, respectively. Furthermore, compounds 4e and 8a proved to have strong...

Design, synthesis and cytotoxic evaluation of novel bis-thiazole derivatives as preferential Pim1 kinase inhibitors with in vivo and in silico study

Mohammad M. Al-Sanea, Tamer M. Nasr, Samir Bondock, Aya Y. Gawish & Nada M. Mohamed
Bis-thiazole derivatives were synthesised conforming to the Pim1 pharmacophore model following Hantzsch condensation. Pim1 has a major role in regulating the G1/S phase which upon inhibition the cell cycle stops at its early stages. Derivatives 3b and 8b showed the best Pim1 IC50 0.32 and 0.24 µM, respectively relative to staurosporine IC50 0.36 µM. Further confirmation of 3b and 8b Pim1 inhibition was implemented by hindering the T47D cell cycle at G0/G1 and S phases...

Additional file 1 of Experimental validation and molecular docking to explore the active components of cannabis in testicular function and sperm quality modulations in rats

Charles O. Nwonuma, Victoria C. Nwatu, Gomaa Mostafa-Hedeab, Oluyomi S. Adeyemi, Omokolade O. Alejolowo, Oluwafemi Adeleke Ojo, Sylvanus A. Adah, Oluwakemi J. Awakan, Charles E. Okolie, Nnaemeka Tobechukwu Asogwa, Udofia A. Inemesit, Godshelp O. Egharevba, Nada H. Aljarba, Saad Alkahtani & Gaber El-Saber Batiha
Additional file 1. HPLC chromatogram of ethanolic leaf extract of cannabis.

Experimental validation and molecular docking to explore the active components of cannabis in testicular function and sperm quality modulations in rats

Charles O. Nwonuma, Victoria C. Nwatu, Gomaa Mostafa-Hedeab, Oluyomi S. Adeyemi, Omokolade O. Alejolowo, Oluwafemi Adeleke Ojo, Sylvanus A. Adah, Oluwakemi J. Awakan, Charles E. Okolie, Nnaemeka Tobechukwu Asogwa, Inemesit A. Udofia, Godshelp O. Egharevba, Nada H. Aljarba, Saad Alkahtani & Gaber El-Saber Batiha
Abstract Background Data available support that ninety percent of male infertility cases are due to low sperm counts. There is a scarcity of data on the medicinal effects of cannabis on fertility. This study evaluated testicular function and sperm quality modulation with cannabis in rats. Methodology Twenty-five male Wistar rats were randomly grouped into five: A, B, C, and D, each group have 5 rats. A (control): 0.2 ml 2% DMSO, B (vitamin C): 90...

Experimental validation and molecular docking to explore the active components of cannabis in testicular function and sperm quality modulations in rats

Charles O. Nwonuma, Victoria C. Nwatu, Gomaa Mostafa-Hedeab, Oluyomi S. Adeyemi, Omokolade O. Alejolowo, Oluwafemi Adeleke Ojo, Sylvanus A. Adah, Oluwakemi J. Awakan, Charles E. Okolie, Nnaemeka Tobechukwu Asogwa, Inemesit A. Udofia, Godshelp O. Egharevba, Nada H. Aljarba, Saad Alkahtani & Gaber El-Saber Batiha
Abstract Background Data available support that ninety percent of male infertility cases are due to low sperm counts. There is a scarcity of data on the medicinal effects of cannabis on fertility. This study evaluated testicular function and sperm quality modulation with cannabis in rats. Methodology Twenty-five male Wistar rats were randomly grouped into five: A, B, C, and D, each group have 5 rats. A (control): 0.2 ml 2% DMSO, B (vitamin C): 90...

New benzothiazole hybrids as potential VEGFR-2 inhibitors: design, synthesis, anticancer evaluation, and in silico study

Mohammad M. Al-Sanea, Abdelrahman Hamdi, Ahmed A. B. Mohamed, Hamed W. El-Shafey, Mahmoud Moustafa, Abdullah A. Elgazar, Wagdy M. Eldehna, Hidayat Ur Rahman, Della G. T. Parambi, Rehab M. Elbargisy, Samy Selim, Syed Nasir Abbas Bukhari, Omnia Magdy Hendawy & Samar S. Tawfik
A new series of 2-aminobenzothiazole hybrids linked to thiazolidine-2,4-dione 4a–e, 1,3,4-thiadiazole aryl urea 6a–d, and cyanothiouracil moieties 8a–d was synthesised. The in vitro antitumor effect of the new hybrids was assessed against three cancer cell lines, namely, HCT-116, HEPG-2, and MCF-7 using Sorafenib (SOR) as a standard drug. Among the tested compounds, 4a was the most potent showing IC50 of 5.61, 7.92, and 3.84 µM, respectively. Furthermore, compounds 4e and 8a proved to have strong...

Additional file 1 of Experimental validation and molecular docking to explore the active components of cannabis in testicular function and sperm quality modulations in rats

Charles O. Nwonuma, Victoria C. Nwatu, Gomaa Mostafa-Hedeab, Oluyomi S. Adeyemi, Omokolade O. Alejolowo, Oluwafemi Adeleke Ojo, Sylvanus A. Adah, Oluwakemi J. Awakan, Charles E. Okolie, Nnaemeka Tobechukwu Asogwa, Inemesit A. Udofia, Godshelp O. Egharevba, Nada H. Aljarba, Saad Alkahtani & Gaber El-Saber Batiha
Additional file 1. HPLC chromatogram of ethanolic leaf extract of cannabis.

Additional file 1 of Experimental validation and molecular docking to explore the active components of cannabis in testicular function and sperm quality modulations in rats

Charles O. Nwonuma, Victoria C. Nwatu, Gomaa Mostafa-Hedeab, Oluyomi S. Adeyemi, Omokolade O. Alejolowo, Oluwafemi Adeleke Ojo, Sylvanus A. Adah, Oluwakemi J. Awakan, Charles E. Okolie, Nnaemeka Tobechukwu Asogwa, Inemesit A. Udofia, Godshelp O. Egharevba, Nada H. Aljarba, Saad Alkahtani & Gaber El-Saber Batiha
Additional file 1. HPLC chromatogram of ethanolic leaf extract of cannabis.

Evaluation of knowledge and practices about administration and regulations of high alert medications among hospital pharmacists in Pakistan: findings and implications

Muhammad Salman, Zia Ul Mustafa, Naureen Shehzadi, Tauqeer Hussain Mallhi, Noman Asif, Yusra Habib Khan, Tahir Mehmood Khan & Khalid Hussain
A death of a nine months old child in Pakistan following the rapid administration of potassium chloride raised serious concerns on the awareness of appropriate use of high alert medications (HAMs) among healthcare professionals (HCPs). This study aimed to ascertain HAMs-related knowledge among hospital pharmacists in Pakistan. A cross-sectional study using exponential non-discriminative snowball sampling was conducted among hospital pharmacists in healthcare settings in Punjab, Pakistan. A validated study tool was used to determine knowledge...

Evaluation of knowledge and practices about administration and regulations of high alert medications among hospital pharmacists in Pakistan: findings and implications

Muhammad Salman, Zia Ul Mustafa, Naureen Shehzadi, Tauqeer Hussain Mallhi, Noman Asif, Yusra Habib Khan, Tahir Mehmood Khan & Khalid Hussain
A death of a nine months old child in Pakistan following the rapid administration of potassium chloride raised serious concerns on the awareness of appropriate use of high alert medications (HAMs) among healthcare professionals (HCPs). This study aimed to ascertain HAMs-related knowledge among hospital pharmacists in Pakistan. A cross-sectional study using exponential non-discriminative snowball sampling was conducted among hospital pharmacists in healthcare settings in Punjab, Pakistan. A validated study tool was used to determine knowledge...

An experimental study on the separation of lanthanides from phosphate ore by organic and inorganic acids

A. Nayl, Ahmed Abd-Elhamid, Wael Arafa & Reda Elkhashab
In this study, the separation of Lanthanides from phosphate ore using C2H2O4, C4H6O6, C3H6O3, H2SO4, and HCl was investigated. The ore was characterized before and after leaching processes by XRF, SEM, XRD, and IR. The different parameters affect the leaching rate such as leaching time, acid concentration, liquid/solid ratios, temperature, and leaching kinetics were studied. The optimal leaching conditions were determined as 0.4M H2C2O4, 2.5M C4H6O6, 1.8M C3H6O3, 2.0M H2SO4, and 3.0M HCl, with a...

Experimental validation and molecular docking to explore the active components of cannabis in testicular function and sperm quality modulations in rats

Charles O. Nwonuma, Victoria C. Nwatu, Gomaa Mostafa-Hedeab, Oluyomi S. Adeyemi, Omokolade O. Alejolowo, Oluwafemi Adeleke Ojo, Sylvanus A. Adah, Oluwakemi J. Awakan, Charles E. Okolie, Nnaemeka Tobechukwu Asogwa, Udofia A. Inemesit, Godshelp O. Egharevba, Nada H. Aljarba, Saad Alkahtani & Gaber El-Saber Batiha
Abstract Background Data available support that ninety percent of male infertility cases are due to low sperm counts. There is a scarcity of data on the medicinal effects of cannabis on fertility. This study evaluated testicular function and sperm quality modulation with cannabis in rats. Methodology Twenty-five male Wistar rats were randomly grouped into five: A, B, C, and D, each group have 5 rats. A (control): 0.2 ml 2% DMSO, B (vitamin C): 90...

Design, synthesis, and biological investigation of oxadiazolyl, thiadiazolyl, and pyrimidinyl linked antipyrine derivatives as potential non-acidic anti-inflammatory agents

Mohammad M. Al-Sanea, Abdelrahman Hamdi, Simone Brogi, Samar S. Tawfik, Dina I. A. Othman, Mahmoud Elshal, Hidayat Ur Rahman, Della G. T. Parambi, Rehab M. Elbargisy, Samy Selim, Ehab M. Mostafa & Ahmed A. B. Mohamed
A novel series of 12 antipyrine derivatives containing 1,3,4-oxadiazoles (4a-d), 1,3,4-thiadiazoles (6a-d), and pyrimidines (8a-d), was preparedand assessed for its potential in vitro COX-2 inhibitors. Compared to Celecoxib, compounds 4b-d and 8d were the most potent derivatives c with a half-maximal inhibitory concentration range of 53–69 nM. Considering COX-2 selectivity index, compounds 4 b and 4c were chosen among these most potent derivatives for further investigation. The in vivo ability of compounds 4 b and...

The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico mechanistic investigations

Arafa Musa, Saleh K. Ihmaid, David L. Hughes, Musa A. Said, Hamada S. Abulkhair, Ahmed H. El-Ghorab, Mohamed A. Abdelgawad, Khaled Shalaby, Mohamed E. Shaker, Khalid Saad Alharbi, Nasser Hadal Alotaibi, Deborah L. Kays, Laurence J. Taylor, Della Grace Thomas Parambi, Sami I. Alzarea, Ahmed A. Al-Karmalawy, Hany E. A. Ahmed & Ahmed M. El-Agrody
Treatment options for the management of breast cancer are still inadequate. This inadequacy is attributed to the lack of effective targeted medications, often resulting in the recurrence of metastatic disorders. Cumulative evidence suggests that epidermal growth factor receptor (EGFR-TK) and cyclin-dependent kinases-9 (CDK-9) overexpression correlates with worse overall survival in breast cancer patients. Pyranopyrazole and pyrazolone are privileged options for the development of anticancer agents. Inspired by this proven scientific fact, we report here the...

The anticancer and EGFR-TK/CDK-9 dual inhibitory potentials of new synthetic pyranopyrazole and pyrazolone derivatives: X-ray crystallography, in vitro, and in silico mechanistic investigations

Arafa Musa, Saleh K. Ihmaid, David L. Hughes, Musa A. Said, Hamada S. Abulkhair, Ahmed H. El-Ghorab, Mohamed A. Abdelgawad, Khaled Shalaby, Mohamed E. Shaker, Khalid Saad Alharbi, Nasser Hadal Alotaibi, Deborah L. Kays, Laurence J. Taylor, Della Grace Thomas Parambi, Sami I. Alzarea, Ahmed A. Al-Karmalawy, Hany E. A. Ahmed & Ahmed M. El-Agrody
Treatment options for the management of breast cancer are still inadequate. This inadequacy is attributed to the lack of effective targeted medications, often resulting in the recurrence of metastatic disorders. Cumulative evidence suggests that epidermal growth factor receptor (EGFR-TK) and cyclin-dependent kinases-9 (CDK-9) overexpression correlates with worse overall survival in breast cancer patients. Pyranopyrazole and pyrazolone are privileged options for the development of anticancer agents. Inspired by this proven scientific fact, we report here the...

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