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1.
J Family Med Prim Care ; 13(6): 2237-2241, 2024 Jun.
Article in English | MEDLINE | ID: mdl-39027852

ABSTRACT

Objective: To determine the effectiveness of the telemedicine-based pulmonary rehabilitation programme in COVID-19 pneumonitis. Design: Prospective intervention study. Setting: Rehabilitation outpatient department, Tertiary-Care institute. Participants: Consecutive sample of patients (N = 50) in recovered COVID-19 infection. Intervention: Six weeks of telemedicine-based pulmonary rehabilitation in recovered patients of COVID-19 infection. Outcome Measures: All patients were clinically assessed by six minutes walk test (6MWT), Modified Medical Research Council Scale (mMRC), 30s-STS and SF 36 at zero week and six weeks post-intervention. Statistical Analysis: Difference in means of pre- and post-intervention was compared using paired t-test. A P value <0.05 was considered statistically significant. Results: The 6MWT, mMRC Scale, 30 seconds sit-to-stand test, and WHO QoL scale-SF 36 were assessed and post-rehabilitation sessions, all the patients' showed improvement in the prescribed parameters. After six weeks of respiratory rehabilitation, the distance covered in the 6MWT was significantly longer than that of before the intervention. There was a significant difference between zero and six weeks during the PR intervention. mMRC and 30s-STS results showed a significant difference between zero and six weeks (2.36 ± 0.598, 4.54 ± 1.94. Quality of life improved significantly after six weeks of pulmonary rehabilitation in eight domains of the SF-36. Conclusion: Six-week pulmonary rehabilitation programme delivered through telemedicine platform improves respiratory function, QoL and anxiety in patients with post-COVID-19 pneumonia during a recovery phase.

2.
Arch Pharm (Weinheim) ; 356(3): e2200444, 2023 Mar.
Article in English | MEDLINE | ID: mdl-36461683

ABSTRACT

In the present investigation, we devolved and synthesized a new series of pyrazole-embedded thiazolidin-4-one derivatives (9a-p) with the goal to produce promising antitubercular leads. The in vitro antimycobacterial activity of the synthesized compounds was tested against replicating and nonreplicating Mtb H37Rv strains. With MIC ranging from 3.03 to 22.55 µg/ml, five compounds (9a, 9c, 9d, 9e, and 9f) emerged as promising antitubercular agents. The active molecules were nontoxic to normal Vero cells. All the synthesized compounds were evaluated for in vitro anti-inflammatory studies. Compounds 9a, 9b, 9c, 9h, and 9i exhibited excellent anti-inflammatory efficacy. Docking study was performed to understand the binding pattern of the significantly active compound 9a with 1P44.


Subject(s)
Molecular Dynamics Simulation , Mycobacterium tuberculosis , Animals , Chlorocebus aethiops , Vero Cells , Structure-Activity Relationship , Antitubercular Agents/pharmacology , Antitubercular Agents/chemistry , Pyrazoles/pharmacology , Molecular Docking Simulation , Molecular Structure , Microbial Sensitivity Tests
3.
Med Chem ; 18(6): 629-654, 2022.
Article in English | MEDLINE | ID: mdl-34344295

ABSTRACT

BACKGROUND: From time immemorial, natural products have been used for the treatment of various diseases. Various natural products, their semisynthetic derivatives, and synthetic analogs have been explored for their anti-infective properties. One such group of natural compounds that has been widely explored is manzamine alkaloids. Manzamine alkaloids are complex natural compounds consisting of a ß-carboline nucleus attached to a pentacyclic ring system; they were first isolated from a marine sponge during the 1980s. OBJECTIVE: This review aims to provide a critical overview on the anti-infective potential of manzamine alkaloids. METHODS: A comprehensive and exhaustive review of the literature on manzamine alkaloids, and their isolation, anti-infective properties, and mechanism of action, is presented. RESULTS: Various manzamine alkaloids have been isolated and have been found to exhibit potent antiinfective activities like antibacterial, antimalarial, antiviral, antifungal, antileishmanial, among others. These manzamine alkaloids exhibit their anti-infective activity by inhibiting targets like GSK-3ß, MtSK. CONCLUSION: This present review along with structure-activity relationship study of manzamine alkaloids for their anti-infective activity will be useful for further development of semisynthetic manzamine analogs as potent anti-infective agents with better therapeutic potential and reduced toxicity.


Subject(s)
Alkaloids , Anti-Infective Agents , Biological Products , Porifera , Alkaloids/pharmacology , Animals , Anti-Infective Agents/pharmacology , Biological Products/pharmacology , Carbazoles/pharmacology , Glycogen Synthase Kinase 3 beta
4.
Future Med Chem ; 13(3): 269-286, 2021 02.
Article in English | MEDLINE | ID: mdl-33399497

ABSTRACT

Reverse transcriptase and integrase are key enzymes that play a pivotal role in HIV-1 viral maturation and replication. Reverse transcriptase consists of two active sites: RNA-dependent DNA polymerase and RNase H. The catalytic domains of integrase and RNase H share striking similarity, comprising two aspartates and one glutamate residue, also known as the catalytic DDE triad, and a Mg2+ pair. The simultaneous inhibition of reverse transcriptase and integrase can be a rational drug discovery approach for combating the emerging drug resistance problem. In the present review, the dual inhibition of RNase H and integrase is systematically discussed, including rationality of design, journey of development, advancement and future perspective.


Subject(s)
Anti-HIV Agents/chemistry , HIV Integrase/metabolism , HIV-1/enzymology , Ribonuclease H/metabolism , Anti-HIV Agents/metabolism , Anti-HIV Agents/therapeutic use , Catalytic Domain , Drug Design , HIV Infections/drug therapy , HIV Infections/metabolism , HIV Integrase/chemistry , HIV Reverse Transcriptase/antagonists & inhibitors , HIV Reverse Transcriptase/metabolism , Humans , Ribonuclease H/antagonists & inhibitors , Structure-Activity Relationship
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