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1.
Pak J Pharm Sci ; 36(6): 1749-1757, 2023 Nov.
Article in English | MEDLINE | ID: mdl-38124415

ABSTRACT

Certain drugs have potential to affect and alter individual's behavior. On the other hand, pain is a complex phenomenon with various treatment options; analgesic medicines are the primary source. Therefore, this study was based on examining some of the benzimidazole analogues for their analgesic as well as behavioral potential following Tail immersion test and Open field test respectively. In addition, molecular docking was performed to find the interaction of these compounds with the active site using AutoDock Vina which was further visualized through Discovery Studio Visualizer. It was seen that the cyano-methyl benzimidazole derivatives (CMB1-CMB3) showed relief in pain as compared to benzimidazole derivatives (BI1-BI3), CMB2 demonstrated highly potent analgesic effect. Likewise, all structures except BI1 displayed increase locomotion during open field test and can be offered as anxiolytic compounds. Almost all derivatives showed improve binding energies for the tested proteins where the high analgesic action of CMB2 might be correlated to its high binding affinity and interaction at µOR. It was also noticed that all structures except BI showed possible binding interaction with GABAA receptor and hence possessed anxiolytic like potential. Thus, this study offered benzimidazole analogues for further drug development of analgesic and anxiolytic like compounds.


Subject(s)
Anti-Anxiety Agents , Humans , Anti-Anxiety Agents/pharmacology , Molecular Docking Simulation , Analgesics/pharmacology , Analgesics/chemistry , Pain/drug therapy , Benzimidazoles/pharmacology , Benzimidazoles/chemistry
2.
Pak J Pharm Sci ; 31(3): 827-833, 2018 May.
Article in English | MEDLINE | ID: mdl-29716862

ABSTRACT

Six novel analogues were prepared by reacting benzimidazole molecules (BM and CMB) propiophenone and benzoyl chlorides respectively. The structures of newly synthesized compounds were determined with the help of spectroscopic techniques. The compounds were subjected to in-vitro screening for their activity against nematodes. It was observed that the benzimidazole (BM) derivatives possessed more nematicidal activity as compared to that of cyanomethyl-benzimidazole (CMB) for Meloidogyne incognita. Among them, the propiophenone substituted benzimidazole derivative B3 was found to be the most active compound and can be further studied as lead molecule for development of anthelmintic drugs.


Subject(s)
Anthelmintics/chemical synthesis , Antinematodal Agents/chemical synthesis , Benzimidazoles/chemical synthesis , Tylenchoidea/drug effects , Animals , Anthelmintics/pharmacology , Antinematodal Agents/pharmacology , Benzimidazoles/pharmacology , Structure-Activity Relationship , Tylenchoidea/physiology
3.
Health Expect ; 20(5): 911-919, 2017 10.
Article in English | MEDLINE | ID: mdl-28294479

ABSTRACT

BACKGROUND: Advance care planning (ACP) is a process of reflection on and communication of a person's future health-care preferences. Evidence suggests visible minorities engage less in ACP. The South Asian ethnic group is the largest visible minority group in Canada, and information is needed to understand how ACP is perceived and how best to approach ACP within this diverse community. OBJECTIVE: To explore perspectives of South Asian community members towards ACP. DESIGN: Peer-to-peer inquiry. South Asian community members who graduated from the Patient and Community Engagement Research programme (PaCER) at the University of Calgary utilized the PaCER method (SET, COLLECT and REFLECT) to conduct a focus group, family interviews and a community forum. SETTING AND PARTICIPANTS: Fifty-seven community-dwelling men and women (22-86 years) who self-identified with the South Asian community in Calgary, Alberta, Canada. RESULTS: The concept of ACP was mostly foreign to this community and was often associated with other end-of-life issues such as organ donation and estate planning. Cultural aspects (e.g. trust in shared family decision making and taboos related to discussing death), religious beliefs (e.g. fatalism) and immigration challenges (e.g. essential priorities) emerged as barriers to participation in ACP. However, participants were eager to learn about ACP and recommended several engagement strategies (e.g. disseminate information through religious institutions and community centres, include families in ACP discussions, encourage family physicians to initiate discussions and translate materials). CONCLUSIONS: Use of a patient engagement research model proved highly successful in understanding South Asian community members' participation in ACP.


Subject(s)
Advance Care Planning , Asian People/psychology , Perception , Adult , Aged , Aged, 80 and over , Asia, Western/ethnology , Canada/epidemiology , Communication , Cultural Characteristics , Female , Focus Groups , Humans , Male , Middle Aged , Qualitative Research , Religion
4.
Pak J Pharm Sci ; 28(6): 2129-34, 2015 Nov.
Article in English | MEDLINE | ID: mdl-26639506

ABSTRACT

In this research program, the antibacterial, antifungal and antioxidant activities of six N'-substituted sulfonyl and benzoyl derivatives of lead molecule PCH were reported. Out of these compounds, sulphonyl derivatives 2,3 and benzoyl derivative 5 showed moderate to good activity against different strains of gram-positive and gram-negative bacteria including B. cereus, B. subtilis, B. thruingiensis and S. pyogenes, S. fecalis and E. coli ATCC 8739. Moreover, upon antifungal screening, the compound, N¢-[(2,4,6-trimethylbenzene) sulfonyl]pyridine-4-carbohydrazide possessed good antifungal activity against Candida species, a causative agent of systemic fungal infections. Antioxidant study demonstrated more than 50% inhibition in DPPH assay for sulphonyl derivative 2 indicating its potential as antioxidant while the other derivatives expressed low level of radical scavenging property.


Subject(s)
Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Antioxidants/pharmacology , Carboxylic Acids/pharmacology , Hydrazines/pharmacology , Pyridines/pharmacology , Anti-Bacterial Agents/chemical synthesis , Antifungal Agents/chemical synthesis , Antioxidants/chemical synthesis , Bacteria/drug effects , Bacteria/growth & development , Biphenyl Compounds/chemistry , Candida/drug effects , Candida/growth & development , Carboxylic Acids/chemical synthesis , Hydrazines/chemical synthesis , Microbial Sensitivity Tests , Molecular Structure , Picrates/chemistry , Pyridines/chemical synthesis , Structure-Activity Relationship
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