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Papers by Syeda Malaika ejaz

Research paper thumbnail of Prevalence and Antibiotic Susceptibility Pattern of Isolates from Patients with Urinary Tract Infection in Karachi

The prevalence of urinary tract infections (UTIs) can vary significantly in males and females amo... more The prevalence of urinary tract infections (UTIs) can vary significantly in males and females among different age groups. With the increased use of antibiotics, UTIs have now become more challenging to treat and a major healthcare issue in developing countries. Therefore, this retrospective study was designed to recognize the resistance profile of isolates from samples of UTI patients in Karachi, Pakistan, so that a proper treatment plan against the infection can be prescribed. One thousand seven hundred hundred urine samples were processed to isolate pathogens at the One Health Diagnostics Microbiology department, Karachi, for 6 months in 2020. Results were analyzed to determine the age group affected, gender affected, the correlation of age group and gender, the most frequent to least frequent isolates found, and the susceptibility patterns of isolates. Pearson Chi-square test was applied to identify whether an association existed between the different variables. The degree of association between the risk factors and UTI was determined by calculating Cramer's V and Odds Ratio (OR). Out of 1700 samples, 1130 (66.5%) were positive samples for UTI, with 910 (80.5%) females and 220 (19.5%) males. The most frequent isolates were E. coli (50.44%), Klebsiella spp. (21.23%), and Coagulase Negative Staphylococcus (7.52%). It was found that the patients between the age group 18-30 and above 60 were the most susceptible, 37% and 32% of the total cases, respectively. Piperacillin-Tazobactam was observed as the most effective drug, as 52.24% of isolates were sensitive to it. Similarly, Doxycycline was found to be the least effective, as 57.75% of isolates were resistant. The most effective antibiotic regime against the most prevalent organism, i.e., E. coli was Imipenem (93.75% sensitive), Amikacin (90.63%), and Fosfomycin (91.28%). A statistically significant association was found between gender and UTI (P<0.01, OR=0.416 (0.326-0.532)) and the most prevalent organism and UTI (P<0.01).

Research paper thumbnail of Diarylsulfonamides and their bioisosteres as dual inhibitors of alkaline phosphatase and carbonic anhydrase: Structure activity relationship and molecular modelling studies

Bioorganic & Medicinal Chemistry, 2015

The effect of bioisosteric replacement of carboxamide linking group with sulfonamide linking grou... more The effect of bioisosteric replacement of carboxamide linking group with sulfonamide linking group, on alkaline phosphatase (AP) and carbonic anhydrase (CA) inhibition activity of aromatic benzenesulfonamides was investigated. A series of carboxamide linked aromatic benzenesulfonamides 1a-1c, 2a-2d and their sulfonamide linked bioisosteres 3a-3d, 4a-4d was synthesized and evaluated for inhibitory activity against bovine tissue non-specific alkaline phosphatase (TNAP), intestinal alkaline phosphatase (IAP) and bCA II. A significant increase in CA inhibition activity was observed upon bioisosteric replacement of carboxamide linking group with a sulfonamide group. Some of these compounds were identified as highly potent and selective AP inhibitors. Compounds 1b, 2b, 3d, 4d 5b and 5c were found to be selective bTNAP inhibitors, whereas compounds 1a, 1c, 2a, 2c, 2d, 3a, 3c, 4a, 4b, 4c, 5a were found to be selective bIAP inhibitors. For most active AP inhibitor 3b, detailed kinetic studies indicated a competitive mode of inhibition against tissue non-specific alkaline phosphatase (TNAP) and non-competitive mode of inhibition against intestinal alkaline phosphatase (IAP). Molecular docking studies were carried out to rationalize important binding site interactions.

Research paper thumbnail of Synthesis, Characterization and Enzyme Inhibition Activity of Organophosphorus Trichalcones Containing Core-Phosphate Moiety

Asian Journal of Chemistry, 2019

Facile synthesis of various organophosphorus trichalcones, possessing substantial insecticidal ac... more Facile synthesis of various organophosphorus trichalcones, possessing substantial insecticidal activity, by using tris(4-acetylphenyl)-phosphate (3) and substituted benzaldehydes as a precursor has been reported. Key precursor 3 has been prepared under mild conditions in presence of tetrabutylammonium bromide (TBAB) as a phase transfer catalyst. All the synthesized compounds (5a-h) were screened for their antibacterial activity and inhibition of α-amylase of insect pest, Tribolium castaneum (Herbst) (Coleoptera: Tenebrionadeae). Biological activity evaluation study revealed that among all the compounds screened, compound 5g found to have promising inhibition of α-amylase of insect pest, Tribolium castaneum. All the synthesized compounds revealed insignificant antimicrobial activity against pathogenic bacteria even at 500 μg/mL.

Research paper thumbnail of Bioactive Phenolics from Launaea intybacea

Phytochemical investigations on the methanolic extract of Launaea intybacea yielded eleven compou... more Phytochemical investigations on the methanolic extract of Launaea intybacea yielded eleven compounds namely, octadecyl (E)-p-coumarate (1), 4-hydroxy-3-methoxybenzaldehyde (2), 4-hydroxybenzoic acid (3), 4-hydroxy-3-methoxybenzoic acid (4), coumaric acid (5), methyl gallate (6), 3,4-dihydroxybenzoic acid (7), 4',5,7-trihydroxyflavone (8), 3',4',5,7-tetrahydroxyflavone (9), 3,3',5,7-tetrahydroxy-4'-methoxyflavone (10) and apigenin 7-O-(4''-O-p-E-coumaroyl)-β-D-glucopyranoside (11). Their structures were determined by using 1D-NMR (1 H, 13 C), mass spectrometry (EIMS, HREIMS, FABMS, HRFABMS) and comparison with the reported data. These compounds (1-11) showed DPPH radical scavenging and enzyme inhibitory activities.

Research paper thumbnail of (15). BJPS 2-Phenitidine

Research paper thumbnail of Prevalence and Antibiotic Susceptibility Pattern of Isolates from Patients with Urinary Tract Infection in Karachi

The prevalence of urinary tract infections (UTIs) can vary significantly in males and females amo... more The prevalence of urinary tract infections (UTIs) can vary significantly in males and females among different age groups. With the increased use of antibiotics, UTIs have now become more challenging to treat and a major healthcare issue in developing countries. Therefore, this retrospective study was designed to recognize the resistance profile of isolates from samples of UTI patients in Karachi, Pakistan, so that a proper treatment plan against the infection can be prescribed. One thousand seven hundred hundred urine samples were processed to isolate pathogens at the One Health Diagnostics Microbiology department, Karachi, for 6 months in 2020. Results were analyzed to determine the age group affected, gender affected, the correlation of age group and gender, the most frequent to least frequent isolates found, and the susceptibility patterns of isolates. Pearson Chi-square test was applied to identify whether an association existed between the different variables. The degree of association between the risk factors and UTI was determined by calculating Cramer's V and Odds Ratio (OR). Out of 1700 samples, 1130 (66.5%) were positive samples for UTI, with 910 (80.5%) females and 220 (19.5%) males. The most frequent isolates were E. coli (50.44%), Klebsiella spp. (21.23%), and Coagulase Negative Staphylococcus (7.52%). It was found that the patients between the age group 18-30 and above 60 were the most susceptible, 37% and 32% of the total cases, respectively. Piperacillin-Tazobactam was observed as the most effective drug, as 52.24% of isolates were sensitive to it. Similarly, Doxycycline was found to be the least effective, as 57.75% of isolates were resistant. The most effective antibiotic regime against the most prevalent organism, i.e., E. coli was Imipenem (93.75% sensitive), Amikacin (90.63%), and Fosfomycin (91.28%). A statistically significant association was found between gender and UTI (P<0.01, OR=0.416 (0.326-0.532)) and the most prevalent organism and UTI (P<0.01).

Research paper thumbnail of Diarylsulfonamides and their bioisosteres as dual inhibitors of alkaline phosphatase and carbonic anhydrase: Structure activity relationship and molecular modelling studies

Bioorganic & Medicinal Chemistry, 2015

The effect of bioisosteric replacement of carboxamide linking group with sulfonamide linking grou... more The effect of bioisosteric replacement of carboxamide linking group with sulfonamide linking group, on alkaline phosphatase (AP) and carbonic anhydrase (CA) inhibition activity of aromatic benzenesulfonamides was investigated. A series of carboxamide linked aromatic benzenesulfonamides 1a-1c, 2a-2d and their sulfonamide linked bioisosteres 3a-3d, 4a-4d was synthesized and evaluated for inhibitory activity against bovine tissue non-specific alkaline phosphatase (TNAP), intestinal alkaline phosphatase (IAP) and bCA II. A significant increase in CA inhibition activity was observed upon bioisosteric replacement of carboxamide linking group with a sulfonamide group. Some of these compounds were identified as highly potent and selective AP inhibitors. Compounds 1b, 2b, 3d, 4d 5b and 5c were found to be selective bTNAP inhibitors, whereas compounds 1a, 1c, 2a, 2c, 2d, 3a, 3c, 4a, 4b, 4c, 5a were found to be selective bIAP inhibitors. For most active AP inhibitor 3b, detailed kinetic studies indicated a competitive mode of inhibition against tissue non-specific alkaline phosphatase (TNAP) and non-competitive mode of inhibition against intestinal alkaline phosphatase (IAP). Molecular docking studies were carried out to rationalize important binding site interactions.

Research paper thumbnail of Synthesis, Characterization and Enzyme Inhibition Activity of Organophosphorus Trichalcones Containing Core-Phosphate Moiety

Asian Journal of Chemistry, 2019

Facile synthesis of various organophosphorus trichalcones, possessing substantial insecticidal ac... more Facile synthesis of various organophosphorus trichalcones, possessing substantial insecticidal activity, by using tris(4-acetylphenyl)-phosphate (3) and substituted benzaldehydes as a precursor has been reported. Key precursor 3 has been prepared under mild conditions in presence of tetrabutylammonium bromide (TBAB) as a phase transfer catalyst. All the synthesized compounds (5a-h) were screened for their antibacterial activity and inhibition of α-amylase of insect pest, Tribolium castaneum (Herbst) (Coleoptera: Tenebrionadeae). Biological activity evaluation study revealed that among all the compounds screened, compound 5g found to have promising inhibition of α-amylase of insect pest, Tribolium castaneum. All the synthesized compounds revealed insignificant antimicrobial activity against pathogenic bacteria even at 500 μg/mL.

Research paper thumbnail of Bioactive Phenolics from Launaea intybacea

Phytochemical investigations on the methanolic extract of Launaea intybacea yielded eleven compou... more Phytochemical investigations on the methanolic extract of Launaea intybacea yielded eleven compounds namely, octadecyl (E)-p-coumarate (1), 4-hydroxy-3-methoxybenzaldehyde (2), 4-hydroxybenzoic acid (3), 4-hydroxy-3-methoxybenzoic acid (4), coumaric acid (5), methyl gallate (6), 3,4-dihydroxybenzoic acid (7), 4',5,7-trihydroxyflavone (8), 3',4',5,7-tetrahydroxyflavone (9), 3,3',5,7-tetrahydroxy-4'-methoxyflavone (10) and apigenin 7-O-(4''-O-p-E-coumaroyl)-β-D-glucopyranoside (11). Their structures were determined by using 1D-NMR (1 H, 13 C), mass spectrometry (EIMS, HREIMS, FABMS, HRFABMS) and comparison with the reported data. These compounds (1-11) showed DPPH radical scavenging and enzyme inhibitory activities.

Research paper thumbnail of (15). BJPS 2-Phenitidine