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1.
Future Med Chem ; 16(8): 737-749, 2024.
Artigo em Inglês | MEDLINE | ID: mdl-38456272

RESUMO

Aim: To synthesize novel chloroquine analogues and evaluate them for antimicrobial and cytotoxic potential. Methods: Novel analogues were synthesized from chloroquine by nucleophilic substitution reaction at the 4-amino position. Results: Analogue CS1 showed maximum antimicrobial potential (30.3 ± 0.15 mm zone) against Pseudomonas aeruginosa and produced a 19.2 ± 0.21 mm zone against Candida albicans, while CS0 produced no zone at the same concentration. Analogue CS9 has excellent cytotoxic potential (HeLa cell line), showing 100% inhibition (IC50 = 8.9 ± 1.2 µg/ml), compared with CS0 (61.9% inhibition at 30 µg/ml). Conclusion: These synthesized chloroquine analogues have excellent activity against different microbial strains and cervical cancer cell lines (HeLa) compared with their parent molecule.


[Box: see text].


Assuntos
Antineoplásicos , Candida albicans , Cloroquina , Testes de Sensibilidade Microbiana , Pseudomonas aeruginosa , Humanos , Candida albicans/efeitos dos fármacos , Cloroquina/farmacologia , Cloroquina/química , Pseudomonas aeruginosa/efeitos dos fármacos , Células HeLa , Antineoplásicos/farmacologia , Antineoplásicos/química , Antineoplásicos/síntese química , Antibacterianos/farmacologia , Antibacterianos/química , Antibacterianos/síntese química , Relação Estrutura-Atividade , Antifúngicos/farmacologia , Antifúngicos/química , Antifúngicos/síntese química , Estrutura Molecular , Ensaios de Seleção de Medicamentos Antitumorais , Proliferação de Células/efeitos dos fármacos , Anti-Infecciosos/farmacologia , Anti-Infecciosos/química , Anti-Infecciosos/síntese química
2.
J Oncol Pharm Pract ; 27(3): 570-578, 2021 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-32437225

RESUMO

OBJECTIVES: Thyroid Cancer is one of the rarest cancers but its prevalence has been increasing worldwide for the last couple of decades. METHODS: The data collection tool was designed to assess knowledge, awareness, perception, and attitude towards preventive practices of thyroid cancer in Pakistani university students. The data were collected over a duration of six months and a total number of 3722 students participated. RESULTS: The knowledge of risk factors of thyroid cancer was an important parameter of this study. The students who knew all the early signs of thyroid cancer were 28.7%. In this study, the independent variables such as age, gender, demographic location, and financial status were found to be highly significant with knowledge, attitude towards warning signs of cancer, and the perception of students about developing thyroid cancer. CONCLUSIONS: The participants were found to have poor knowledge about early signs of thyroid cancer. The study participants perception, behavior, and attitude towards preventive practices of thyroid cancer were found inadequate and appropriate measures on a National level should be taken to enhance the knowledge about preventive practices of thyroid cancer. Increasing knowledge and awareness shall help decrease the overall morbidity and mortality linked with thyroid carcinomas and thyroid diseases.


Assuntos
Estudantes de Medicina , Estudantes , Neoplasias da Glândula Tireoide/prevenção & controle , Adolescente , Adulto , Fatores Etários , Atitude , Estudos Transversais , Feminino , Conhecimentos, Atitudes e Prática em Saúde , Humanos , Masculino , Paquistão , Fatores de Risco , Fatores Sexuais , Fatores Socioeconômicos , Inquéritos e Questionários , Neoplasias da Glândula Tireoide/epidemiologia , Universidades , Adulto Jovem
3.
Curr Drug Deliv ; 15(8): 1100-1111, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29366416

RESUMO

Androgenetic alopecia, generally recognized as male pattern baldness, is a gradually developing medical and physiological change, which is manifested by continuous hair-loss from scalp. Finasteride (4-aza-3-oxosteroid) is a potent anti-baldness compound that selectively and competitively inhibits the 5α-reductase isoenzymes. Prolonged oral use of finasteride leads to the emergence of sexual disorders including decrease in libido, gynecomastia, erectile dysfunction, ejaculation disorder, orgasm disorders and mood disturbances. Since, hair follicles widely home in 5α-reductase, topical formulations of finasteride in comparison to its oral formulations are expected to potentially reduce its systemic adverse effects. The analysis of literature has revealed some delivery systems developed for the enhanced and localized penetration of finasteride into the skin. These finasteride delivery systems include polymersomes, vesicular nanocarriers, vesicular ethosomal carriers, liposomes and niosomes, liquid crystalline nanoparticles, topical solutions and gels. The aim of this review article is to briefly amass all literature on topical delivery of finasteride to elaborate best dosage form, i.e. formulation having maximum permeation rate. This study will serve as a future perspective regarding topical delivery of finasteride. The literature analysis has exhibited that most of the previous investigators have used propylene glycol in their finasteride-loaded topical formulations, while poloxamer P407, monoolein, transcutol P and choline was used in few formulations. Moreover, among all drug delivery systems, finasteride liposomal gel system consisting of 2% methyl cellulose and gel system containing poloxamer P407 exhibited the highest flux with a value of 28.4 ± 1.3 µg/cm2h and 23.1 ± 1.4 µg/cm2h, respectively. Several topical drug delivery techniques such as topical microneedles, aerosol foams, nanoemulsions, microsponges, and emulsifier free formulations, fullerenes, ointments, pastes, creams, gel and lotions are still to be worthy regarding finasteride topical delivery in future.


Assuntos
Inibidores de 5-alfa Redutase/administração & dosagem , Alopecia/tratamento farmacológico , Sistemas de Liberação de Medicamentos , Finasterida/administração & dosagem , Administração Tópica , Animais , Humanos
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