SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL (2-OXO-3-(ARYLIMINO) INDOLIN-1-YL)-N-ARYL PROPANAMIDES AS ANTI-HUMAN IMMUNODEFICIENCY AGENTS

Objective: Acquired immunodeficiency syndrome (AIDS) was first identified in the Western world in 1981. Since then, AIDS has been increasingly wide spreading, its rapid worldwide dissemination brought about by modern mass tourism. Isatin (1 H-indole-2, 3-Dione), an endogenous compound identified in many organisms, shows a wide range of biological activities. In view of the above details, we wish to report the synthesis and evaluation of novel isatin analogs, as promising anti-human immunodeficiency (HIV) agents.Methods: A series of novel isatin analogs (3a-3p) were synthesized, and their chemical structures were confirmed by nuclear magnetic resonance:1H, 13C, ESI-MS spectral data, and CHNS.Results: The compounds were evaluated as inhibitors of HIV type-1 in MT-4 cell cultures. Of these sixteen compounds, only 5 compounds showed potent anti-HIV activity.Conclusion: Evaluation of compound properties in silico showed that they possess significant drug-like characteristics.

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1,4-Diazepines: A Review on Synthesis, Reactions and Biological Significance

Current Organic Synthesis ◽

10.2174/1570179416666190703113807 ◽

2019 ◽

Vol 16 (5) ◽

pp. 709-729 ◽

Cited By ~ 4

Author(s):

Muhammad A. Rashid ◽

Aisha Ashraf ◽

Sahibzada S. Rehman ◽

Shaukat A. Shahid ◽

Adeel Mahmood ◽

...

Keyword(s):

Biological Activities ◽

Biological Significance ◽

Biological Evaluation ◽

Wide Range ◽

Pharmaceutical Industries ◽

Biological Aspects ◽

Synthetic Routes ◽

Biological Attributes ◽

Synthesis Reactions ◽

Potential Use

Background:1,4-Diazepines are two nitrogen containing seven membered heterocyclic compounds and associated with a wide range of biological activities. Due to its medicinal importance, scientists are actively involved in the synthesis, reactions and biological evaluation of 1,4-diazepines since number of decades.Objective:The primary purpose of this review is to discuss the synthetic schemes and reactivity of 1,4- diazepines. This article also describes biological aspects of 1,4-diazepine derivatives, that can be usefully exploited for the pharmaceutical sector.Conclusion:This review summarizes the abundant literature on synthetic routes, chemical reactions and biological attributes of 1,4-diazepine derivatives. We concluded that 1,4-diazepines have significant importance due to their biological activities like antipsychotic, anxiolytic, anthelmintic, anticonvulsant, antibacterial, antifungal and anticancer. 1,4-diazepine derivatives with significant biological activities could be explored for potential use in the pharmaceutical industries.

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Effects of Atovaquone on the Ultrastructural Morphology of Pneumocystis Carinii

Microscopy and Microanalysis ◽

10.1017/s1431927600007297 ◽

1997 ◽

Vol 3 (S2) ◽

pp. 81-82

Author(s):

M.P. Goheen ◽

M.S. Bartlett ◽

M.M. Shaw ◽

S.R. Meshnick ◽

J.W. Smith

Keyword(s):

Adverse Reactions ◽

Pneumocystis Carinii ◽

Spinner Flask ◽

Short Term ◽

Human Embryonic Lung ◽

Transmission Electron ◽

Significant Incidence ◽

Wide Range ◽

Acquired Immunodeficiency ◽

Immunodeficiency Syndrome

Pneumocystis carinii pneumonia (PCP) occurs at some time in most patients with acquired immunodeficiency syndrome (AIDS). Trimethoprim/sulfamethoxazole or pentamidine isothionate are the traditional modes of therapy for treatment and prophylaxis of PCP. Unfortunately these drugs are associated with a significant incidence of adverse side effects particularly in patients with AIDS. Toxicity and a growing concern that P. carinii strains are becoming resistant to these compounds is providing the impetus for the search for additional drugs to combat P. carinii. Atovaquone, developed as an antimalarial agent, has activity against a wide range of other organisms, including Toxoplasma sp. and P. carinii, with a lower incidence of adverse reactions during clinical trials. Atovaquone inhibits mitochondrial respiration in P. falciparum and P. carinii. In this study transmission electron microscopy (TEM) was used to observe the effects of atovaquone on P. carinii organisms in short term spinner flask culture.Spinner flask cultures of human embryonic lung cells were inoculated with P. carinii from infected rat lung.

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A Case Report of Acute Severe Myelitis and Meningitis Secondary to Varicella Zoster Virus Reactivation in a Patient with Acquired Immunodeficiency Syndrome

International Journal of Medical Students ◽

10.5195/ijms.2021.863 ◽

2021 ◽

Author(s):

Victor A Novelo-Hernández ◽

Marco Cárdenas ◽

Claudia Torres-González ◽

Patricio Garcia-Espinosa ◽

Rómulo Ramirez ◽

...

Keyword(s):

Spinal Cord ◽

Varicella Zoster Virus ◽

Acquired Immunodeficiency Syndrome ◽

Clinical Manifestations ◽

Virus Reactivation ◽

Neck Stiffness ◽

Varicella Zoster ◽

Wide Range ◽

Acquired Immunodeficiency ◽

Immunodeficiency Syndrome

Background: Myelitis post Herpes-Zoster is a rare condition that is typically associated with immunocompromised states. It usually starts as an acute loss of sensory and motor functions below the affected spinal cord level. The condition can range in severity from a mild to a fatal presentation. Other neurological complications include meningitis, atypical presentations should encourage the search for undiagnosed immunosuppression states. The Case: We describe the case of a 42-year-old man, previously undiagnosed with HIV, who developed acute myelitis and meningitis after the appearance of the classic zoster lesions. On lumbar puncture and subsequent CSF analysis, the patient was found to have Froin’s Syndrome. The patient was initiated with ceftriaxone, vancomycin, and acyclovir regimen and prophylactic antiphymic treatment was also added. After 14 days in the hospital, the fever, headache, and neck stiffness subsided while the sphincter function and lower limb paraplegia did not improve. Conclusion: Varicella zoster virus reactivation suggests underlying immunosuppression. This case demonstrates the importance of being cognizant to the wide range of clinical manifestations that may suggest spinal cord involvement after clinical reactivation. Furthermore, physicians also need to be mindful that Acquired Immunodeficiency Syndrome (AIDS) and other immunodeficiency states could present with atypical clinical manifestations.

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Pathologic Features of Mycobacterium kansasii Infection in Patients With Acquired Immunodeficiency Syndrome

Archives of Pathology & Laboratory Medicine ◽

10.5858/2003-127-0554-pfomki ◽

2003 ◽

Vol 127 (5) ◽

pp. 554-560 ◽

Cited By ~ 7

Author(s):

Michael B. Smith ◽

Claudia P. Molina ◽

Vicki J. Schnadig ◽

Michael C. Boyars ◽

Judith F. Aronson

Keyword(s):

Lymph Node ◽

Acquired Immunodeficiency Syndrome ◽

Pulmonary Infection ◽

Mycobacterium Kansasii ◽

Abdominal Lymph Node ◽

Inflammatory Reactions ◽

Pathologic Features ◽

Wide Range ◽

Acquired Immunodeficiency ◽

Immunodeficiency Syndrome

Abstract Context.—Mycobacterium kansasii is a slow-growing photochromogenic mycobacterium that may infect patients with human immunodeficiency virus (HIV) late in the course of acquired immunodeficiency syndrome (AIDS). The clinical features of pulmonary and extrapulmonary infections have been described in the literature; however, the pathology of infection has not been adequately addressed. Objective.—This report describes the pathologic features of 12 cases of M kansasii infection in patients with AIDS. Design.—The medical records, autopsy protocols, cytologic material, and histologic material from patients with AIDS and concomitant M kansasii infection at a tertiary-care medical center during 1990–2001 were reviewed. Results.—Twelve cases were identified, 6 by autopsy, 5 of which were diagnosed postmortem. Four of the 12 cases had cytologic material and 4 cases had histologic biopsies available for review. Pulmonary infection was most common (9/12), and all patients in whom thoracic lymph nodes were assessed showed involvement (7/7). Abdominal infection was less frequent, with only 1 of 6, 2 of 6, and 2 of 6, demonstrating liver, spleen, and abdominal lymph node infection, respectively. Isolated infections without documented pulmonary infection included brain abscess (n = 1), ulnar osteomyelitis (n = 1), and paratracheal mass (n = 1). Cytologic and histologic material showed a wide range of inflammatory reactions, including granulomas with and without necrosis, neutrophilic abscesses, spindle-cell proliferations, and foci of granular eosinophilic necrosis. The M kansasii bacillus was characteristically long, coarsely beaded, and frequently showed folded, bent, or curved ends. Intracellular bacilli were randomly or haphazardly distributed within histiocytes. Conclusion.—Mycobacterium kansasii infection produces predominately pulmonary infection in late-stage AIDS with a high incidence of thoracic lymph node involvement and a much lower incidence of dissemination to other sites. Infection is manifest as a wide variety of inflammatory reactions on cytology and histology; however, the characteristic appearance of the bacillus on acid-fast bacilli stain and its intracellular arrangement in histiocytes can allow a presumptive identification.

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Biological Activity of Bicyclic and Tricyclic Diterpenoids from Salvia Species of Immediate Pharmacological and Pharmaceutical Interest

Natural Product Communications ◽

10.1177/1934578x1100600839 ◽

2011 ◽

Vol 6 (8) ◽

pp. 1934578X1100600 ◽

Cited By ~ 3

Author(s):

Maria Carmela Bonito ◽

Carla Cicala ◽

Maria Carla Marcotullio ◽

Francesco Maione ◽

Nicola Mascolo

Keyword(s):

Biological Activities ◽

Folk Medicine ◽

Plant Defence ◽

Experimental Studies ◽

Scientific Basis ◽

Chemical Structures ◽

Wide Range ◽

Real Value ◽

Antimicrobic Activity ◽

Cyclic Compounds

Diterpenoids are a class of compounds that derive from the condensation of four isoprene units that leads to a wide variety of complex chemical structures, including acyclic bi-, tri-and tetra-cyclic compounds; in Salvia species, only bi-, tri-and tetra-cyclic compounds have been found. This review covers a wide range of biological activities and mode of action of diterpenoids isolated from Salvia species that might raise some pharmacological and pharmaceutical interest. We have produced a synoptic table where the biological activities of the main active principles are summarized. Our analysis emphasizes that diterpenoids from Salvia species continue to be a plant defence system since their antimicrobic activity. Experimental studies show that most of diterpenoids considered have cytotoxic and / or antiproliferative activity. Some of them have also cardiovascular and central effects. In a less extended manner, diterpenoids from Salvia species show gastrointestinal, urinary, antinflammatory, antidiabetic, ipolipidemic and antiaggregating effects. In the last decade, several clinical trials have been developed in order to investigate the real value of Salvia extracts treatment; results obtained are promising and confer scientific basis in the use of medicinal plants from folk medicine.

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Development of Nimesulide Analogues as Dual Tubulin and HSP27 Inhibitor for Treating Female Cancers

10.20944/preprints202009.0523.v1 ◽

2020 ◽

Author(s):

Laila Jarragh Alhadad ◽

Fars Alanazi ◽

Gamaleldin Harisa

Keyword(s):

Breast Cancer ◽

Ovarian Cancer ◽

Cell Lines ◽

Biological Activities ◽

Critical Role ◽

Biological Evaluation ◽

Crystallographic Analysis ◽

Skbr3 Cell ◽

Chemical Structures ◽

Ic50 Values

Tubulin and heat shock protein 27 (HSP27) are up-regulated in cancer cells, and play a critical role in cell division, and proliferation. Therefore, they are targets for discovery of anticancer therapy. The objective of this study is to design, characterize, and biologically evaluate the nimesulide analogues to combat female cancer such as ovarian cancer, and breast cancer. Herein, the nimesulide analogues are designed to target both tubulin and HSP27 functions. Ovarian cancer (SKOV3) and breast cancer (SKBR3) cell lines were used as surrogate models to test the nimesulide analogs biological activities using MTT assay. In the present study, four nimesulide analogues were designed, synthesized and the chemical structures were with the biological evaluation were studied. The synthesized agents were characterized by 1H-NMR, 13C-NMR, the molecular weight was confirmed using GC-MS technique, and melting point. Besides, the agent L4 structure was confirmed using X-ray crystallographic analysis. The present data revealed that nimesulide analogs have potent anticancer activity against SKOV3and SKBR3 cell lines. The IC50 values for both SKOV3 and SKBR3 cell lines treated with the agents showed a potent cell growth inhibition range of 0.23-2.02 µM and 0.50-3.73 µM respectively. In conclusion, the designed nimesulide analogues can target both tubulins, and HSP27 concurrently, and they are promising agents as future chemotherapy female cancers.

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Marine Invertebrate Natural Products for Anti-Inflammatory and Chronic Diseases

Evidence-based Complementary and Alternative Medicine ◽

10.1155/2013/572859 ◽

2013 ◽

Vol 2013 ◽

pp. 1-10 ◽

Cited By ~ 29

Author(s):

Kalimuthu Senthilkumar ◽

Se-Kwon Kim

Keyword(s):

Chronic Diseases ◽

Marine Invertebrates ◽

Biological Activities ◽

Marine Invertebrate ◽

Neurological Diseases ◽

Multiple Cell ◽

Acquired Immunodeficiency ◽

Anti Inflammatory ◽

Hiv And Cancer ◽

Immunodeficiency Syndrome

The marine environment represents a relatively available source of functional ingredients that can be applied to various aspects of food processing, storage, and fortification. Moreover, numerous marine invertebrates based compounds have biological activities and also interfere with the pathogenesis of diseases. Isolated compounds from marine invertebrates have been shown to pharmacological activities and are helpful for the invention and discovery of bioactive compounds, primarily for deadly diseases like cancer, acquired immunodeficiency syndrome (AIDS), osteoporosis, and so forth. Extensive research within the last decade has revealed that most chronic illnesses such as cancer, neurological diseases, diabetes, and autoimmune diseases exhibit dysregulation of multiple cell signaling pathways that have been linked to inflammation. On the basis of their bioactive properties, this review focuses on the potential use of marine invertebrate derived compounds on anti-inflammatory and some chronic diseases such as cardiovascular disease, osteoporosis, diabetes, HIV, and cancer.

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Room Temperature Synthesis and Antibacterial Activity of New Sulfonamides Containing N,N-Diethyl-Substituted Amido Moieties

International Journal of Medicinal Chemistry ◽

10.1155/2012/367815 ◽

2012 ◽

Vol 2012 ◽

pp. 1-13 ◽

Cited By ~ 2

Author(s):

Olayinka O. Ajani ◽

Oluwole B. Familoni ◽

Feipeng Wu ◽

Johnbull O. Echeme ◽

Zheng Sujiang

Keyword(s):

Antibacterial Activity ◽

Mass Spectra ◽

Room Temperature ◽

Biological Activities ◽

Chemical Structures ◽

Wide Range ◽

Synthetic Routes ◽

Mic Value ◽

C Nmr

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1–11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12–22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1–22 were confirmed by analytical and spectral data such as IR, 1H- and 13C-NMR, and mass spectra. The in vitro antibacterial activity of these compounds along with standard clinical reference, streptomycin, was investigated on two key targeted organisms. It was observed that 1-(benzylsulfonyl)pyrrolidine-2-carboxylic acid, 2 emerged as the most active compound against Staphylococcus aureus at MIC value of 1.8 μg/mL while 4-(3-(diethylamino)-3-oxo-2-(phenylmethylsulfonamido) propyl)phenyl phenylmethanesulfonate, 22 was the most active sulfonamide scaffold on Escherichia coli at MIC value of 12.5 μg/mL.

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Acetylcholine esterase inhibitory activity of green synthesized nanosilver by naphthopyrones isolated from marine-derived Aspergillus niger

PLoS ONE ◽

10.1371/journal.pone.0257071 ◽

2021 ◽

Vol 16 (9) ◽

pp. e0257071

Author(s):

Ghada Mahmoud Abdelwahab ◽

Amira Mira ◽

Yuan-Bin Cheng ◽

Tarek A. Abdelaziz ◽

Mohamed Farid I. Lahloub ◽

...

Keyword(s):

Aspergillus Niger ◽

Inhibitory Activity ◽

Active Sites ◽

Biological Activities ◽

Biological Properties ◽

Biological Evaluation ◽

Acetylcholine Esterase ◽

Protective Effects ◽

Wide Range ◽

First Time

Aspergillus niger metabolites exhibited a wide range of biological properties including antioxidant and neuro-protective effects and some physical properties as green synthesis of silver nanoparticles AgNP. The present study presents a novel evidence for the various biological activities of green synthesized AgNPs. For the first time, some isolated naphtho-γ-pyrones from marine-derived Aspergillus niger, flavasperone (1), rubrofusarin B (2), aurasperone A (3), fonsecinone A (4) in addition to one alkaloid aspernigrin A (7) were invistigated for their inhibitory activity of acetylcholine esterase AChE, a hallmark of Alzheimer’s disease (AD). The ability to synthesize AgNPs by compounds 3, 4 and 7 has been also tested for the first time. Green synthesized AgNPs were well-dispersed, and their size was ranging from 8–30 nm in diameter, their morphology was obviously spherical capped with the organic compounds. Further biological evaluation of their AChE inhibitory activity was compared to the parent compounds. AgNps dramatically increased the inhibitory activity of Compounds 4, 3 and 7 by 84, 16 and 13 fold, respectively to be more potent than galanthamine as a positive control with IC50 value of 1.43 compared to 0.089, 0.311 and 1.53 of AgNPs of Compounds 4, 3 and 7, respectively. Also compound 2 showed moderate inhibitory activity. This is could be probably explained by closer fitting to the active sites or the synergistic effect of the stabilized AgNPs by the organic compouds. These results, in addition to other intrinsic chemical and biological properties of naphtho-γ-pyrones, suggest that the latter could be further explored with a view towards other neuroprotective studies for alleviating AD.

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New Scabimycins A-C Isolated from Streptomyces acidiscabies (Lu19992)

Molecules ◽

10.3390/molecules26195922 ◽

2021 ◽

Vol 26 (19) ◽

pp. 5922

Author(s):

Constanze Paulus ◽

Josef Zapp ◽

Andriy Luzhetskyy

Keyword(s):

Natural Products ◽

Bioactive Peptides ◽

Biological Activities ◽

Powerful Source ◽

Drug Candidates ◽

Chemical Structures ◽

Wide Range ◽

Streptomyces Acidiscabies ◽

New Compounds ◽

Important Drug

Peptide natural products displaying a wide range of biological activities have become important drug candidates over the years. Microorganisms have been a powerful source of such bioactive peptides, and Streptomyces have yielded many novel natural products thus far. In an effort to uncover such new, meaningful compounds, the metabolome of Streptomyces acidiscabies was analyzed thoroughly. Three new compounds, scabimycins A–C (1–3), were discovered, and their chemical structures were elucidated by NMR spectroscopy. The relative and absolute configurations were determined using ROESY NMR experiments and advanced Marfey’s method.

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