M. PÜskÜllÜ - Academia.edu (original) (raw)
Papers by M. PÜskÜllÜ
![Research paper thumbnail of Synthesis and potent antistaphylococcal activity of some new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines](https://a.academia-assets.com/images/blank-paper.jpg)
](Journal of Enzyme Inhibition and Medicinal Chemistry, 2014
A series of new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxami... more A series of new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines (23-33) have been synthesized and evaluated for their potential antistaphylococcal activity. Cytotoxic effects of the compounds were investigated by the neutral red uptake (NRU) cytotoxicity test. Most of the compounds exhibited good MICs values against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Compound 28 with N-cyclohexylcarboxamidine group at the 5-position was found to be the most potent agent, with the MIC value of 3.12 µg/mL.
Archiv der Pharmazie, 2009
A series of N-substituted-1H-benzimidazole-5(6)-sulfonamides and 3-(5,6-dichloro-1H-benzimidazol-... more A series of N-substituted-1H-benzimidazole-5(6)-sulfonamides and 3-(5,6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzensulfonamides were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Certain compounds inhibit bacterial growth with low MIC (lg/mL) values. The most active compounds 30, 31, and 32 have the lowest MIC values with 0.39 to 0.19 lg/mL. Among the compounds having sulfonamido moities, 16, 23, and 24 exhibited the strongest antibacterial activity with 1.56 lg/ mL MIC values.
Journal of Enzyme Inhibition and Medicinal Chemistry, 2006
New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized i... more New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized in the present study. The potential role of melatonin as an antioxidant by scavenging and detoxifying ROS raised the possibility that compounds that are analogous to melatonin can also be used for their antioxidant properties. Therefore the antioxidant effects of the newly synthesized compounds were investigated in vitro by means of their inhibitory effect on hydrogen peroxide-induced erythrocyte membrane lipid peroxidation (EMLP) and on various erythrocyte antioxidant enzymes viz. superoxide dismutase (SOD), catalase (CAT) and glucose-6-phosphate dehydrogenase (G6PD). The synthesized benzimidazole derivatives showed remarkable antioxidant activity in vitro in the H 2 O 2-induced EMLP system. Furthermore their effects on various antioxidant enzymes are discussed and evaluated from the perspective of structure-activity relationships.
Mini-Reviews in Medicinal Chemistry, 2013
Quinolinc dclivatives constitute an importatrt class of compounds for new drug development. As a ... more Quinolinc dclivatives constitute an importatrt class of compounds for new drug development. As a large number of experimental and thcorctical rdieshaveshopnahatth€quinolineringsystcmisanimporlantsbucluralunitrridelyexistinginatkaloids,therapeuticsandsynthcticanalogueswithexcitingbiologicalactivities.TheF€sentrcviewprcvidesrecentantioxidardies have shopn ahat th€ quinoline ring systcm is an imporlant sbuclural unit rridely existing in atkaloids, therapeutics and synthctic analogues with exciting biological activities. The F€sent rcview prcvides recent antioxidardieshaveshopnahatth€quinolineringsystcmisanimporlantsbucluralunitrridelyexistinginatkaloids,therapeuticsandsynthcticanalogueswithexcitingbiologicalactivities.TheF€sentrcviewprcvidesrecentantioxidat activities covering in vivo and in ritlo studies of natural and synihetic analogues, as well as the proposad mechanisms of acion and structure-activity relationships. Ke].rvordsi Antioxidant activity, free radical, quitroline, oxidativc stless. may promote water contamination. Luckily, quinoline is r€adily degadable by certain micloorgatisms, such as Rhodococcws species Stlain Ql, which can be isolated from soil [4]. Quinoline and tbeir derivatives play important roles for the sl.nthesis of nahlal products and as thenp€utic agents, an important class of compounds for new drug development. Thus, it has been synthesizing by many researchels as target compouds. They also evaluated with different pharmacological activities covering anti-cancer, anti-mycobacterial, antimicrobial, arti-convuls{|t, atti-infl amrnalory and cardiovascula activities [5-9]. Nitrogen including heterocycles are among the most commonly synthesized compounds as th€y show distinct biological activities. The anti-malarial activity of quinoline de vatives is well known from many decades. Apart from antimalarial activity, quinoline compounds wide variety of biologically signiflcant activities like, anti-inflammatory [l0], anti-malarial U l-131, anli-ncoplastic [14-15], anticancer and anti-oxidant [6-17], antileishmanial [18], anti-con\.ulsant [1 9], anti-microbial [20-21], vasorclaxing [22], anti-h).pertensive and platelet derived go$th factor receptor tlaosine kinase (PDGF-RTK) inhibiting agents 123,241, ^ntiproliferative [25] activity and anti-viral [26] activities. Praveen et al. [27] synthesized substituted quinolines and bis(indolyl)methane derivatives. Anti-bacterial efficary of the 2,4,6-substitut€d quinolines (Fig. 2) was sqeoncd against Staphylococcus aureus and Escherichia coli. Compounds having p{olyl (2) and 3-bromo (3) groups showed same activity with the standard drug Amoxiclav against S. a 'eus. 3-brorno (3) and compound posscssitrg 3-anisyl (5) group showed better activity than tbe refercnce drug Amphotericin' B. Altifungal activity of these compounds was performed against Candida arricars. Compounds 3-bromo (3) and 5-Cl, p-tolyl (4) sbowed higher activity than the standard drug Amphotericin-B against C. Albicans. 6 20t3 BeDth.rn Scienc. Publbhers
Journal of Enzyme Inhibition and Medicinal Chemistry, 2006
New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized i... more New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized in the present study. The potential role of melatonin as an antioxidant by scavenging and detoxifying ROS raised the possibility that compounds that are analogous to melatonin can also be used for their antioxidant properties. Therefore the antioxidant effects of the newly synthesized compounds were investigated in vitro by means of their inhibitory effect on hydrogen peroxide-induced erythrocyte membrane lipid peroxidation (EMLP) and on various erythrocyte antioxidant enzymes viz. superoxide dismutase (SOD), catalase (CAT) and glucose-6-phosphate dehydrogenase (G6PD). The synthesized benzimidazole derivatives showed remarkable antioxidant activity in vitro in the H 2 O 2 -induced EMLP system. Furthermore their effects on various antioxidant enzymes are discussed and evaluated from the perspective of structure-activity relationships.
Journal of Enzyme Inhibition and Medicinal Chemistry, 2014
A series of new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxami... more A series of new 2-[4-(3,4-dimethoxyphenoxy)phenyl]-1,N-disubstituted-1H-benzimidazole-5-carboxamidines (23-33) have been synthesized and evaluated for their potential antistaphylococcal activity. Cytotoxic effects of the compounds were investigated by the neutral red uptake (NRU) cytotoxicity test. Most of the compounds exhibited good MICs values against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Compound 28 with N-cyclohexylcarboxamidine group at the 5-position was found to be the most potent agent, with the MIC value of 3.12 µg/mL.
Archiv der Pharmazie, 2009
A series of N-substituted-1H-benzimidazole-5(6)-sulfonamides and 3-(5,6-dichloro-1H-benzimidazol-... more A series of N-substituted-1H-benzimidazole-5(6)-sulfonamides and 3-(5,6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzensulfonamides were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Certain compounds inhibit bacterial growth with low MIC (lg/mL) values. The most active compounds 30, 31, and 32 have the lowest MIC values with 0.39 to 0.19 lg/mL. Among the compounds having sulfonamido moities, 16, 23, and 24 exhibited the strongest antibacterial activity with 1.56 lg/ mL MIC values.
Journal of Enzyme Inhibition and Medicinal Chemistry, 2006
New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized i... more New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized in the present study. The potential role of melatonin as an antioxidant by scavenging and detoxifying ROS raised the possibility that compounds that are analogous to melatonin can also be used for their antioxidant properties. Therefore the antioxidant effects of the newly synthesized compounds were investigated in vitro by means of their inhibitory effect on hydrogen peroxide-induced erythrocyte membrane lipid peroxidation (EMLP) and on various erythrocyte antioxidant enzymes viz. superoxide dismutase (SOD), catalase (CAT) and glucose-6-phosphate dehydrogenase (G6PD). The synthesized benzimidazole derivatives showed remarkable antioxidant activity in vitro in the H 2 O 2-induced EMLP system. Furthermore their effects on various antioxidant enzymes are discussed and evaluated from the perspective of structure-activity relationships.
Mini-Reviews in Medicinal Chemistry, 2013
Quinolinc dclivatives constitute an importatrt class of compounds for new drug development. As a ... more Quinolinc dclivatives constitute an importatrt class of compounds for new drug development. As a large number of experimental and thcorctical rdieshaveshopnahatth€quinolineringsystcmisanimporlantsbucluralunitrridelyexistinginatkaloids,therapeuticsandsynthcticanalogueswithexcitingbiologicalactivities.TheF€sentrcviewprcvidesrecentantioxidardies have shopn ahat th€ quinoline ring systcm is an imporlant sbuclural unit rridely existing in atkaloids, therapeutics and synthctic analogues with exciting biological activities. The F€sent rcview prcvides recent antioxidardieshaveshopnahatth€quinolineringsystcmisanimporlantsbucluralunitrridelyexistinginatkaloids,therapeuticsandsynthcticanalogueswithexcitingbiologicalactivities.TheF€sentrcviewprcvidesrecentantioxidat activities covering in vivo and in ritlo studies of natural and synihetic analogues, as well as the proposad mechanisms of acion and structure-activity relationships. Ke].rvordsi Antioxidant activity, free radical, quitroline, oxidativc stless. may promote water contamination. Luckily, quinoline is r€adily degadable by certain micloorgatisms, such as Rhodococcws species Stlain Ql, which can be isolated from soil [4]. Quinoline and tbeir derivatives play important roles for the sl.nthesis of nahlal products and as thenp€utic agents, an important class of compounds for new drug development. Thus, it has been synthesizing by many researchels as target compouds. They also evaluated with different pharmacological activities covering anti-cancer, anti-mycobacterial, antimicrobial, arti-convuls{|t, atti-infl amrnalory and cardiovascula activities [5-9]. Nitrogen including heterocycles are among the most commonly synthesized compounds as th€y show distinct biological activities. The anti-malarial activity of quinoline de vatives is well known from many decades. Apart from antimalarial activity, quinoline compounds wide variety of biologically signiflcant activities like, anti-inflammatory [l0], anti-malarial U l-131, anli-ncoplastic [14-15], anticancer and anti-oxidant [6-17], antileishmanial [18], anti-con\.ulsant [1 9], anti-microbial [20-21], vasorclaxing [22], anti-h).pertensive and platelet derived go$th factor receptor tlaosine kinase (PDGF-RTK) inhibiting agents 123,241, ^ntiproliferative [25] activity and anti-viral [26] activities. Praveen et al. [27] synthesized substituted quinolines and bis(indolyl)methane derivatives. Anti-bacterial efficary of the 2,4,6-substitut€d quinolines (Fig. 2) was sqeoncd against Staphylococcus aureus and Escherichia coli. Compounds having p{olyl (2) and 3-bromo (3) groups showed same activity with the standard drug Amoxiclav against S. a 'eus. 3-brorno (3) and compound posscssitrg 3-anisyl (5) group showed better activity than tbe refercnce drug Amphotericin' B. Altifungal activity of these compounds was performed against Candida arricars. Compounds 3-bromo (3) and 5-Cl, p-tolyl (4) sbowed higher activity than the standard drug Amphotericin-B against C. Albicans. 6 20t3 BeDth.rn Scienc. Publbhers
Journal of Enzyme Inhibition and Medicinal Chemistry, 2006
New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized i... more New, except 1d, melatonin analogue benzimidazole derivatives were synthesized and characterized in the present study. The potential role of melatonin as an antioxidant by scavenging and detoxifying ROS raised the possibility that compounds that are analogous to melatonin can also be used for their antioxidant properties. Therefore the antioxidant effects of the newly synthesized compounds were investigated in vitro by means of their inhibitory effect on hydrogen peroxide-induced erythrocyte membrane lipid peroxidation (EMLP) and on various erythrocyte antioxidant enzymes viz. superoxide dismutase (SOD), catalase (CAT) and glucose-6-phosphate dehydrogenase (G6PD). The synthesized benzimidazole derivatives showed remarkable antioxidant activity in vitro in the H 2 O 2 -induced EMLP system. Furthermore their effects on various antioxidant enzymes are discussed and evaluated from the perspective of structure-activity relationships.