search

OpenSourceMycetoma / Series-3-Phenothiazines

Project for the development of phenothiazine (and related tricyclic) anti-fungal drugs
0 stars 0 forks source link

Samples from NEU #6

Open MFernflower opened 1 year ago

MFernflower commented 1 year ago

I luckily came across a paper by the team at NEU about some tricyclic chlopromazine like compounds (based on carbazoles) that showed activity against Naegleria Folweri 10.3389/fmicb.2023.1149145

Since we as a team don't have the lab capacity to make novel phenothiazines at the moment this could be a good step forward!

P-Rayner commented 9 months ago

This looks really interesting data. Thanks @wwjvdsande! Hopefully some of the other tricycles will also be potent. @MFernflower we can certainly explore some analogues as a follow up. We will update asap.

MFernflower commented 7 months ago

image

@P-Rayner @lferrins since it seems like this particular tail is seeming useful - these are some possible head-swapped analogues to consider

MFernflower commented 7 months ago

I have also uploaded these as a CSV file that can be opened in a free tool called datawarrior

MFernflower commented 6 months ago

@MFernflower CID 61387607 is an analog of promethazine (des-methyl) and I recall that your original request for analogs featured the phenothiazine. Our focus has been on removing/modifying the acetyl groups on the CBL compounds as these could be problematic for a drug.

I have posted now the few possible scaffold hops of curaxin 137 (talked about in this issue) to the series 3 wiki https://github.com/OpenSourceMycetoma/Series-3-Phenothiazines/wiki/Desirable-Compounds-Not-Yet-Synthesised @lferrins

lferrins commented 3 months ago

Hi all, I recall that there was a request for additional material from the NU compounds but now I am unable to locate it again, can anyone point me to it, please?

MFernflower commented 3 months ago

https://github.com/OpenSourceMycetoma/Monthly-zoom-meetings/issues/23#issuecomment-2188657532 @lferrins

On Tue, Aug 6, 2024, 9:27 AM Lori Ferrins @.***> wrote:

Hi all, I recall that there was a request for additional material from the NU compounds but now I am unable to locate it again, can anyone point me to it, please?

— Reply to this email directly, view it on GitHub https://github.com/OpenSourceMycetoma/Series-3-Phenothiazines/issues/6#issuecomment-2271293576, or unsubscribe https://github.com/notifications/unsubscribe-auth/AAYEWDXMFLUH5U2HSLNIPOLZQDFLTAVCNFSM6AAAAAA2WJOYROVHI2DSMVQWIX3LMV43OSLTON2WKQ3PNVWWK3TUHMZDENZRGI4TGNJXGY . You are receiving this because you were mentioned.Message ID: @.*** com>

DouniaEMC commented 1 month ago

In vitro data + toxicity data in vivo

Compound No toxicity at IC50 IC90
MYOS_00626_00_00 20 uM 8.3 14.4
MYOS_00627_00_00 20 uM 1.4 1.9
MYOS_00628_00_00 20 uM 3.9 6.0
MYOS_00631_00_00 20 uM 2.5 3.7
MYOS_00632_00_00 20 uM 2.4 3.5