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1.
South Asian J Cancer ; 12(1): 17-22, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36851927

RESUMO

Shamaila ShamaunBackground Cervical cancer is the third most prevalent female cancer in Pakistan; nearly 70% present at a very advanced stage of malignancy due to lack of awareness, proper screening, and vaccination. Therefore, we aimed to assess the knowledge and attitude toward screening, vaccination, and risk factors of cervical cancer in sexually active women of Pakistan. Methods This cross-sectional study was conducted at the gynecology outpatient clinic of a public sector hospital in Karachi, Pakistan, from December 2021 to March 2022. We included sexually active women with exception of diagnosed cases of cervical cancer, pregnancy, vaginal bleeding, and psychological disorder. Collected data were regarding demographic characteristics, awareness regarding cervical cancer, screening, human papillomavirus (HPV) vaccine, and risk factors, history of cervical screening, and wiliness to opt-in for cervical screening. Results We included 226 women with a mean age of 41.25 ± 10.54 years. The mean parity level was observed to be 3.8 ± 1.95. A majority of women were housewives by profession (88.9%) and uneducated (61.9%). Only 41.2% (93) of women were aware of cervical cancer, 33.6% (76) were aware of cervical screening, and only 15.9% (36) had a history of cervical screening. Only four women (1.8%) were aware of the HPV vaccine and 31% (70) showed intention to opt-in for cervical screening. A vast majority of women (96.9%) were not aware of the risk factors of cervical cancer. Conclusion(s) We have observed poor awareness regarding cervical cancer, HPV vaccination, and cervical screening among women in our population. Lack of awareness was not restricted to a certain segment but it prevails all across the demographic in our population.

2.
Molecules ; 21(3): 266, 2016 Feb 25.
Artigo em Inglês | MEDLINE | ID: mdl-26927044

RESUMO

A new series of N-(6-arylbenzo[d]thiazol-2-yl)acetamides were synthesized by C-C coupling methodology in the presence of Pd(0) using various aryl boronic pinacol ester/acids. The newly synthesized compounds were evaluated for various biological activities like antioxidant, haemolytic, antibacterial and urease inhibition. In bioassays these compounds were found to have moderate to good activities. Among the tested biological activities screened these compounds displayed the most significant activity for urease inhibition. In urease inhibition, all compounds were found more active than the standard used. The compound N-(6-(p-tolyl)benzo[d]thiazol-2-yl)acetamide was found to be the most active. To understand this urease inhibition, molecular docking studies were performed. The in silico studies showed that these acetamide derivatives bind to the non-metallic active site of the urease enzyme. Structure-activity studies revealed that H-bonding of compounds with the enzyme is important for its inhibition.


Assuntos
Acetamidas/síntese química , Antibacterianos/síntese química , Antioxidantes/síntese química , Benzotiazóis/síntese química , Inibidores Enzimáticos/síntese química , Urease/antagonistas & inibidores , Acetamidas/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Benzotiazóis/farmacologia , Células Cultivadas , Inibidores Enzimáticos/farmacologia , Eritrócitos/citologia , Eritrócitos/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Bactérias Gram-Negativas/crescimento & desenvolvimento , Bactérias Gram-Positivas/efeitos dos fármacos , Bactérias Gram-Positivas/crescimento & desenvolvimento , Hemólise/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Óxido Nítrico/antagonistas & inibidores , Phaseolus/química , Phaseolus/enzimologia , Proteínas de Plantas/antagonistas & inibidores , Proteínas de Plantas/química , Urease/química
3.
Molecules ; 20(11): 19914-28, 2015 Nov 05.
Artigo em Inglês | MEDLINE | ID: mdl-26556326

RESUMO

A variety of novel 5-aryl thiophenes 4a-g containing sulphonylacetamide (sulfacetamide) groups were synthesized in appreciable yields via Pd[0] Suzuki cross coupling reactions. The structures of these newly synthesized compounds were determined using spectral data and elemental analysis. Density functional theory (DFT) studies were performed using the B3LYP/6-31G (d, p) basis set to gain insight into their structural properties. Frontier molecular orbital (FMOs) analysis of all compounds 4a-g was computed at the same level of theory to get an idea about their kinetic stability. The molecular electrostatic potential (MEP) mapping over the entire stabilized geometries of the molecules indicated the reactive sites. First hyperpolarizability analysis (nonlinear optical response) were simulated at the B3LYP/6-31G (d, p) level of theory as well. The compounds were further evaluated for their promising antibacterial and anti-urease activities. In this case, the antibacterial activities were estimated by the agar well diffusion method, whereas the anti-urease activities of these compounds were determined using the indophenol method by quantifying the evolved ammonia produced. The results revealed that all the sulfacetamide derivatives displayed antibacterial activity against Bacillus subtiles, Escherichia coli, Staphylococcus aureus, Shigella dysenteriae, Salmonella typhae, Pseudomonas aeruginosa at various concentrations. Furthermore, the compound 4g N-((5-(4-chlorophenyl)thiophen-2-yl)sulfonyl) acetamide showed excellent urease inhibition with percentage inhibition activity ~46.23 ± 0.11 at 15 µg/mL with IC50 17.1 µg/mL. Moreover, some other compounds 4a-f also exhibited very good inhibition against urease enzyme.


Assuntos
Acetamidas/química , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Tiofenos/química , Tiofenos/farmacologia , Urease/antagonistas & inibidores , Antibacterianos/química , Antibacterianos/farmacologia , Anti-Infecciosos/síntese química , Testes de Sensibilidade Microbiana , Modelos Moleculares , Eletricidade Estática , Tiofenos/síntese química
4.
PLoS One ; 9(12): e115457, 2014.
Artigo em Inglês | MEDLINE | ID: mdl-25545159

RESUMO

A highly convenient method has been developed for the synthesis of (prop-2-ynyloxy) benzene and its derivatives. Differently substituted phenol and aniline derivatives were allowed to react with propargyl bromide in the presence of K2CO3 base and acetone as solvent. The compounds were synthesized in good yields (53-85%). Low cost, high yields and easy availability of compounds helped in the synthesis. Electron withdrawing groups favor the formation of stable phenoxide ion thus in turn favors the formation of product while electron donating groups do not favor the reaction. Phenol derivatives gave good yields as compared to that of aniline. As aprotic polar solvents favor SN2 type reactions so acetone provided best solvation for the reactions. K2CO3 was proved to be good for the synthesis. Antibacterial, Antiurease and NO scavenging activity of synthesized compounds were also examined. 4-bromo-2-chloro-1-(prop-2-ynyloxy)benzene 2a was found most active compound against urease enzyme with a percentage inhibition of 82.00±0.09 at 100 µg/mL with IC50 value of 60.2. 2-bromo-4-methyl-1-(prop-2-ynyloxy)benzene 2d was found potent antibacterial against Bacillus subtillus showing excellent inhibitory action with percentage inhibition of 55.67±0.26 at 100 µg/ml wih IC50 value of 79.9. Based on results, it can be concluded that some of the synthesized compounds may have potential antiurease and antibacterial effects against several harmful substances.


Assuntos
Alcinos/síntese química , Antioxidantes/síntese química , Sequestradores de Radicais Livres/síntese química , Éteres Fenílicos/síntese química , Alcinos/farmacologia , Antioxidantes/farmacologia , Bacillus subtilis/efeitos dos fármacos , Técnicas de Química Sintética/métodos , Sequestradores de Radicais Livres/farmacologia , Pargilina/análogos & derivados , Pargilina/química , Éteres Fenílicos/farmacologia
5.
Molecules ; 18(8): 8845-57, 2013 Jul 25.
Artigo em Inglês | MEDLINE | ID: mdl-23892631

RESUMO

In general, benzothiazole derivatives have attracted great interest due to thier pharmaceutical and biological importance. New 2-amino-6-arylbenzothiazoles were synthesized in moderate to excellent yields via Suzuki cross coupling reactions using various aryl boronic acids and aryl boronic acid pinacol esters and the antiurease and nitric oxide (NO) scavenging activity of the products were also examined. The most active compound concerning urease enzyme inhibition was 6-phenylbenzo[d]thiazole-2-amine 3e, with an IC50 value of 26.35 µg/mL. Compound 3c, 6-(4-methoxyphenyl) benzo[d]thiazole-2-amine, exhibited the highest nitric oxide percentage scavenging at 100 µg/mL.


Assuntos
Benzotiazóis/síntese química , Paládio/química , Urease/química , Aminas , Benzotiazóis/química , Ácidos Borônicos/química , Catálise , Sequestradores de Radicais Livres/química , Estrutura Molecular , Óxido Nítrico/química , Urease/antagonistas & inibidores
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