http://localhost:80/xmlui/handle/123456789/12721 2026-04-05T09:11:54Z 2026-04-05T09:11:54Z Walayat, Kamran Ahmad, Matloob Rasul, Azhar Aslam, Sana Anjum, Muhammad Naveed Sultan, Sadia Iqbal, Mazhar http://localhost:80/xmlui/handle/123456789/15863 2023-01-10T05:38:11Z 2020-03-15T00:00:00Z

Title: Synthesis, characterization and antimicrobial activity of norfloxacin based acetohydrazides Authors: Walayat, Kamran; Ahmad, Matloob; Rasul, Azhar; Aslam, Sana; Anjum, Muhammad Naveed; Sultan, Sadia; Iqbal, Mazhar Abstract: The drug resistance phenomenon in microbes is resulting in the ineffectiveness of available drugs to treat the infections. Thus, there is a continued need to discover new molecules to combat the drug resistance phenomenon. Norfloxacin is a fluoroquinolone antibiotic that is used for the treatment of urinary tract infections. In this research work, norfloxacin is structurally modified by hybridizing with a range of substituted acetohydrazidic moieties through a multistep reaction. The first step involves the coupling of norfloxacin 1 with methyl chloroacetate followed by the treatment with hydrazine hydrate to result in corresponding cetohydrazide 3. A range of substituted benzaldehydes were reacted with the acetohydrazide to form the targeted series of norfloxacin derivatives 4a-i. The final compounds were screened for antimicrobial activity. Among the tested compounds, 4c, 4d, 4e and 4f displayed better antifungal activity against F.avenaceum, while compound 4c and 4e were active against F. bubigeum.

2020-03-15T00:00:00Z Ibraheem, Farhat Ahmad, Matloob Ashfaq, Usman Ali Aslam, Sana Ali Khan, Zulfiqar Sultan, Sadia http://localhost:80/xmlui/handle/123456789/15862 2023-01-10T05:37:49Z 2020-03-15T00:00:00Z

Title: Synthesis, molecular docking and anti-diabetic studies of novel benzimidazole-pyrazoline hybrid molecules Authors: Ibraheem, Farhat; Ahmad, Matloob; Ashfaq, Usman Ali; Aslam, Sana; Ali Khan, Zulfiqar; Sultan, Sadia Abstract: : Pyrazoline and benzimidazoles derivatives have been widely studied due to their potential applications in the medicinal field. In this research project, we have hybridized these two heterocyclic systems in the same molecule. A new series of compounds, 2-((3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)methyl)-1H-benzo[d]imidazole (5a-i) were synthesized through a multistep reaction. In the first step, chalcones 3a-i were prepared by coupling of various acetophenones and benzaldehydes under alkaline conditions. These chalcones were cyclized with hydrazine hydrate to form a series of pyrazolines which were finally coupled with 2-chloromethyl-1H-benzimidazole to get a new series of titled hybrid molecules. The structures of these compounds were elucidated by spectral (1H NMR and 13C NMR) analysis. The anti diabetic potential of these compounds was studied by screening them for their α-glucosidase inhibition activity. The SAR was established through molecular docking analysis. Compound 5d appeared as effective inhibitor with IC50 = 50.06µM as compared to reference drug (acarbose) having IC50 = 58.8µM.

2020-03-15T00:00:00Z Kadir, Abdul Ibrahim, Sadaf Nawaid Shah, Syed Nudrat http://localhost:80/xmlui/handle/123456789/15861 2023-01-10T05:37:24Z 2020-03-20T00:00:00Z

Title: Attenuation of cisplatin-induced acute kidney injury by N-(2- Hydroxyphenyl) acetamide and its gold conjugated nano-formulations in mice Authors: Kadir, Abdul; Ibrahim, Sadaf; Nawaid Shah, Syed Nudrat Abstract: : The attenuation of cisplatin-induced acute kidney injury (AKI) in mice by N-(2-hydroxyphenyl) acetamide (NA-2) and NA-2-conjugated gold nanoparticles (NA2-AuNPs) was investigated. Male BALB/c mice (n = 54) were divided into nine groups having six animals in each group. Animals in groups 3-9 were pre-treated for 5 days with test compounds, whereas, animals in group 1 and 2 received normal saline. On day 4, animals in groups 2, 3, 4, 5, 6 and 9 were given single intra-peritoneal injection of CP at the dose of 5 mg/kg. After 72 hours of CP injection, all animals were sacrificed. Blood was collected for serum urea and creatinine estimation, and kidneys were harvested for histopathological examinations and qPCR studies for nuclear factor-κB p50, (NFκB) ; inducible nitric oxide synthase (iNOS); hemeoxygenase-1 (HO-1); and interleukin-6 (IL-6).NA-2 and NA2-AuNPs was observed to decrease the serum urea andcreatinine levels. Both the test compounds reduced kidney injury damage score and improved histological architecture in the treated animals in dose dependent manner. Furthermore, the mRNA expressions of NFkB p50, iNOS and IL-6 genes were down-regulated, and HO-1 gene was up-regulated in the animals treated with the test compounds. It is concluded that NA-2 and NA2-AuNPs attenuates CP-induced AKI in mice models through anti-inflammatory and anti-oxidant mechanisms.

2020-03-20T00:00:00Z Bektas, Nurcan Nemutlu, Dilara Cam, Mevcude Okcay, Yagmur Eken, Hazal Arslan, Rana http://localhost:80/xmlui/handle/123456789/14790 2022-12-07T03:50:21Z 2020-01-30T00:00:00Z

Title: The nicotinic modulation of pain Authors: Bektas, Nurcan; Nemutlu, Dilara; Cam, Mevcude; Okcay, Yagmur; Eken, Hazal; Arslan, Rana Abstract: Pain is a physiological unpleasant sensation that associated with actual or potential tissue damage and affects the major part of human population. Numerous modulatory system control pain through a complex process. The drugs that regulate the modulators involving in this process are currently available; however, the studies to understand the process and develop new agents are still going on. In this review, it is aimed to relay information about how nicotinic receptors contribute the pain modulation. It is obvious that a wide variety of nicotinic receptors is located in both peripheral and central areas. Among these receptors α7, α4β2 and α9α10 receptor subtypes draw attention in terms of pain modulation. The fact that different receptor subtypes involve in different processes of different pain conditions leads to provide beneficial results from the agonism of α7, α4β2 and antagonism of α9α10. The major restraint of the usage of nAChR agonists is their adverse effects. However, nowadays, the side effects are reduced by the clinical developments. Additionally, positive allosteric modulators that amplify the effectiveness of nAChR ligands are in demand.

2020-01-30T00:00:00Z